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Available MolScreen Hybrid Model (dfa) |
| model | name | nof_ligand | auc | R2pkd | tag | Tissue | ADR | category | Disease | Function | Drug_Mechanism |
|---|---|---|---|---|---|---|---|---|---|---|---|
| dfaABCG2 | ATP-binding cassette sub-family G member 2 | 361 | 95.43 | 0.8033 | Anaemia Thrombocytopenia | ABC transporter | |||||
| dfaMDR1 | Multidrug resistance protein 1 | 1166 | 94.67 | 0.4495 | Expressed in liver, kidney, small intestine and brain. | Alopecia Angioedema Azoospermia Bone marrow failure Hyperlipidaemia Mucosal inflammation Oligomenorrhoea Stomatitis | ABC transporter | Cancer, unspecific | Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells. | ||
| dfa5HT1A | 5-hydroxytryptamine receptor 1A | 6870 | 96.15 | 0.3264 | Nature11159 | Detected in lymph nodes, thymus and spleen. Detected in activated T cells, but not in resting T cells. <a class="attribution" href="P08908#ref1" onclick="ensureReferenceVisible('ref1')">Ref.1</a> <a class="attribution" href="P08908#ref8" onclick="ensureReferenceVisible('ref8')">Ref.8</a> | Asthenia Cardiac failure congestive Dry eye Dry mouth Insomnia Orthostatic hypotension Peripheral coldness Priapism Psychotic disorder Raynaud's phenomenon | G-protein coupled receptor 1 | Anxiety disorder, unspecified
Brain ischemia Cocaine dependence Depression Detrusor hyperreflexia Mood [affective] disorders Skeletal muscle associated spasticity Urinary incontinence | This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase. | Serotonin 1a (5-HT1a) receptor agonist: Ergoloid Serotonin 1a (5-HT1a) receptor partial agonist: Aripiprazole, Buspirone, Methysergide, Vilazodone |
| dfa5HT2A | 5-hydroxytryptamine receptor 2A | 4473 | 89.56 | 0.4198 | Nature11159 | Detected in brain cortex (at protein level). Detected in blood platelets. <a class="attribution" href="P28223#ref15" onclick="ensureReferenceVisible('ref15')">Ref.15</a> | Akathisia Anticholinergic syndrome Corneal pigmentation Dermatitis allergic Dry mouth Dystonia Ejaculation disorder Electrocardiogram change Erectile dysfunction Extrapyramidal disorder Fibrocystic breast disease Galactorrhoea Gynaecomastia Hypercholesterolaemia Hyperprolactinaemia Hyperthermia Insomnia Lenticular opacities Lipid metabolism disorder Mania Miosis Mydriasis Nasal congestion Neuroleptic malignant syndrome Orthostatic hypotension Parkinsonism Tachycardia Tardive dyskinesia Weight increased | G-protein coupled receptor 1 | Acute ureteric colic
Anxiety disorder, unspecified Arterial embolism and thrombosis Cocaine dependence Depression Diabetic nephropathy Diabetic neuropathy Essential (primary) hypertension Migraine Schizophrenia | This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor mediates its action by association with G proteins. | Serotonin 2a (5-HT2a) receptor antagonist: Aripiprazole, Asenapine, Carphenazine, Chlorpromazine, Chlorprothixene, Clozapine, Cyclobenzaprine, Droperidol, Haloperidol, Haloperidol Decanoate, Iloperidone, Loxapine, Lurasidone, Mesoridazine, Mirtazapine, Molindone, Nefazodone, Olanzapine, Paliperidone, Pimozide, Promazine, Quetiapine, Risperidone, Thioridazine, Thiothixene, Trazodone, Trifluoperazine, Trimipramine, Ziprasidone |
| dfa5HT2B | 5-hydroxytryptamine receptor 2B | 1330 | 88.28 | 0.3304 | Nature11159 | Ubiquitous. Detected in liver, kidney, heart, pulmonary artery, and intestine. Detected at lower levels in blood, placenta and brain, especially in cerebellum, occipital cortex and frontal cortex. <a class="attribution" href="P41595#ref1" onclick="ensureReferenceVisible('ref1')">Ref.1</a> <a class="attribution" href="P41595#ref2" onclick="ensureReferenceVisible('ref2')">Ref.2</a> <a class="attribution" href="P41595#ref3" onclick="ensureReferenceVisible('ref3')">Ref.3</a> <a class="attribution" href="P41595#ref10" onclick="ensureReferenceVisible('ref10')">Ref.10</a> <a class="attribution" href="P41595#ref15" onclick="ensureReferenceVisible('ref15')">Ref.15</a> | Dry mouth Dyskinesia Extrapyramidal disorder Insomnia Nasal congestion Orthostatic hypotension | G-protein coupled receptor 1 | Anxiety disorder, unspecified
Migraine P-chloroamphetamine-induced hyperglycemia | This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor mediates its action by association with G proteins. | Serotonin 2b (5-HT2b) receptor antagonist: Methysergide Serotonin 2b (5-HT2b) receptor partial agonist: Methylergonovine |
| dfa5HT2C | 5-hydroxytryptamine receptor 2C | 3080 | 91.43 | 0.4913 | Nature11159 | Detected in brain. <a class="attribution" href="P28335#ref3" onclick="ensureReferenceVisible('ref3')">Ref.3</a> | Akathisia Dermatitis allergic Dry mouth Dystonia Ejaculation disorder Extrapyramidal disorder Galactorrhoea Hypercholesterolaemia Hyperthermia Insomnia Lipid metabolism disorder Neuroleptic malignant syndrome Orthostatic hypotension Parkinsonism Psychotic disorder Tachycardia Tardive dyskinesia | G-protein coupled receptor 1 | Acute ureteric colic
Cocaine dependence Motor disorder Schizophrenia | This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor mediates its action by association with G proteins. | Serotonin 2c (5-HT2c) receptor agonist: Lorcaserin Serotonin 2c (5-HT2c) receptor antagonist: Carphenazine, Chlorprothixene, Cyclobenzaprine, Loxapine, Methixene, Methysergide, Mirtazapine, Nefazodone, Olanzapine, Quetiapine, Risperidone, Thioridazine, Trazodone, Trifluoperazine, Trimipramine, Ziprasidone |
| dfaAA1R | Adenosine receptor A1 | 6538 | 96.76 | 0.4106 | Nature11159 | G-protein coupled receptor 1 | Analgesics
Asthma Cardiac arrhythmias Chronic ileitis Inflammation Inflammatory bowel disease Insulin resistance (obesity-related) Noninsulin-dependent diabetes mellitus Pain Renal failure | Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. | Adenosine A1 receptor antagonist: Theophylline | ||
| dfaAA2AR | Adenosine receptor A2a | 5340 | 93.68 | 0.3371 | Nature11159 | Angina pectoris Flushing Palpitations | G-protein coupled receptor 1 | Analgesics
Brain injury Depression Dyskinesia Inflammation Ischemia reperfusion injuries Neurodegenerative diseases Neuropsychiatric disorders Oxygen-induced retinopathy Pain Parkinson's disease Renal diseases | Receptor for adenosine, and the activity of this receptor is mediated by G proteins which activate adenylyl cyclase. | Adenosine A2 receptor antagonist: Pentoxifylline Adenosine A2a receptor agonist: Regadenoson |
|
| dfaAA2BR | Adenosine receptor A2b | 2336 | 93.74 | 0.5893 | Palpitations | G-protein coupled receptor 1 | Asthma | Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. | Adenosine A2b receptor antagonist: Theophylline Adenosine receptor agonist: Adenosine Adenosine receptor antagonist: Caffeine, Theophylline, Theophylline Glycinate |
||
| dfaAA3R | Adenosine receptor A3 | 3505 | 92.32 | 0.515 | Nature11159 | G-protein coupled receptor 1 | Cancer, unspecific
Chronic ileitis Depression Inflammatory bowel disease Myocardial ischemia and reperfusion injury | Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase. possible role in reproduction. | |||
| dfaACM1 | Muscarinic acetylcholine receptor M1 | 2443 | 87.73 | 0.5634 | Nature11159 | Anticholinergic syndrome Constipation Cycloplegia Diabetic eye disease Dry mouth Dry skin Dysphagia Dysuria Extrapyramidal disorder Hyperpyrexia Hyperthermia Hyperventilation Hypohidrosis Intraocular pressure increased Mydriasis Neuroleptic malignant syndrome Photophobia Suppressed lactation Tachycardia Urinary retention Vision blurred | G-protein coupled receptor 1 | Alzheimer's disease
Bronchospasm (histamine induced) Cognitive deficits Schizophrenia | The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. | Muscarinic acetylcholine receptor M1 agonist: Cevimeline Muscarinic acetylcholine receptor M1 antagonist: Anisotropine, Atropine, Benztropine, Biperiden, Clidinium, Cycrimine, Dicyclomine, Diphemanil, Diphenidol, Ethopropazine, Glycopyrrolate, Hexocyclium, Isopropamide, Mepenzolate, Methixene, Methscopolamine, Oxyphencyclimine, Oxyphenonium, Procyclidine, Propantheline, Scopolamine, Tridihexethyl, Trihexyphenidyl |
|
| dfaACM2 | Muscarinic acetylcholine receptor M2 | 2143 | 90.08 | 0.5293 | Nature11159 | Anticholinergic syndrome Constipation Cycloplegia Diabetic eye disease Dry mouth Dry skin Extrapyramidal disorder Gastric hypomotility Hyperpyrexia Intraocular pressure increased Mydriasis Salivary hypersecretion Tachycardia Urinary incontinence Urinary retention Vision blurred | G-protein coupled receptor 1 | Alzheimer's disease
Analgesics Autoimmune cardiomyopathy Bronchoconstriction (cold air-induced) Chronic obstructive pulmonary disease, unspecified Hypothermia Neurogenic bladder Pain, unspecified Tremor, unspecified | The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. | Muscarinic acetylcholine receptor M2 agonist: Bethanechol Muscarinic acetylcholine receptor M2 antagonist: Atropine, Darifenacin, Fesoterodine, Oxybutynin, Propantheline, Solifenacin, Tolterodine, Trospium |
|
| dfaACM3 | Muscarinic acetylcholine receptor M3 | 1692 | 89.9 | 0.6991 | Nature11159 | Anticholinergic syndrome Constipation Cycloplegia Diabetic eye disease Dry mouth Dry skin Dysphagia Extrapyramidal disorder Hyperpyrexia Intraocular pressure increased Mydriasis Salivary hypersecretion Tachycardia Urinary retention Vision blurred | G-protein coupled receptor 1 | Airway hyperreactivity
Urge incontinence | The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. | Muscarinic acetylcholine receptor M3 agonist: Acetylcholine, Bethanechol, Carbachol, Cevimeline, Methacholine, Pilocarpine Muscarinic acetylcholine receptor M3 antagonist: Aclidinium, Anisotropine, Atropine, Clidinium, Cyclopentolate, Darifenacin, Dicyclomine, Diphemanil, Fesoterodine, Glycopyrrolate, Hexocyclium, Ipratropium, Isopropamide, Mepenzolate, Methscopolamine, Oxybutynin, Oxyphencyclimine, Oxyphenonium, Propantheline, Solifenacin, Tiotropium, Tolterodine, Tridihexethyl, Tropicamide, Trospium |
|
| dfaADA1A | Alpha-1A adrenergic receptor | 1887 | 93.96 | 0.5874 | Nature11159 | Expressed in heart, brain, liver and prostate, but not in kidney, lung, adrenal, aorta and pituitary. Within the prostate, expressed in the apex, base, periurethral and lateral lobe. Isoform <a href="#P35348-4" onclick="ensureIsoformSequenceVisible('P35348-4'); return true;">4</a> is the most abundant isoform expressed in the prostate with high levels also detected in liver and heart. <a class="attribution" href="P35348#ref5" onclick="ensureReferenceVisible('ref5')">Ref.5</a> <a class="attribution" href="P35348#ref7" onclick="ensureReferenceVisible('ref7')">Ref.7</a> <a class="attribution" href="P35348#ref15" onclick="ensureReferenceVisible('ref15')">Ref.15</a> | Anxiety Bradycardia Carbohydrate metabolism disorder Cerebral haemorrhage Dyskinesia Dysuria Ejaculation disorder Fear Gangrene Gestational hypertension Hyperhidrosis Hypertension Insomnia Intranasal paraesthesia Irritability Nasal congestion Nasal discomfort Nasal dryness Nervous system disorder Orthostatic hypotension Pallor Palpitations Psychotic disorder Pulmonary oedema Restlessness Sleep disorder Sneezing Sudden death Tachycardia Vasoconstriction Ventricular arrhythmia | G-protein coupled receptor 1 | Benign prostate hyperplasia
Hypertrophic vascular disease | This alpha-adrenergic receptor mediates its action by association with g proteins that activate a phosphatidylinositol- calcium second messenger system, and its effect is mediated by G(q) and G(11) proteins. | Adrenergic receptor alpha-1 agonist: Alfuzosin, Metaraminol, Methoxamine, Midodrine, Phenylephrine Adrenergic receptor alpha-1 antagonist: Carvedilol, Doxazosin, Prazosin, Tamsulosin, Terazosin, Trimipramine Alpha-1a adrenergic receptor agonist: Phenylpropanolamine, Phenylpropanolamine Polistirex Alpha-1a adrenergic receptor antagonist: Dapiprazole, Silodosin |
| dfaADA1B | Alpha-1B adrenergic receptor | 4419 | 92.55 | 0.4398 | Anxiety Bradycardia Cerebral haemorrhage Depressed level of consciousness Dyskinesia Ejaculation disorder Fear Gangrene Gestational hypertension Hyperhidrosis Intranasal paraesthesia Nasal congestion Nasal discomfort Nasal dryness Nervous system disorder Orthostatic hypotension Pallor Palpitations Pulmonary oedema Respiration abnormal Sneezing Tachycardia Vasoconstriction | G-protein coupled receptor 1 | Shy-Drager syndrome | This alpha-adrenergic receptor mediates its action by association with g proteins that activate a phosphatidylinositol-calcium second messenger system. | |||
| dfaADA1D | Alpha-1D adrenergic receptor | 2055 | 95.14 | 0.5331 | Anxiety Bradycardia Cerebral haemorrhage Dyskinesia Fear Gestational hypertension Hyperhidrosis Intranasal paraesthesia Nasal congestion Nasal dryness Neurosis Orthostatic hypotension Pallor Palpitations Tachycardia Vasoconstriction | G-protein coupled receptor 1 | Hypertension | This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium. | |||
| dfaADA2A | Alpha-2A adrenergic receptor | 923 | 84 | 0.6225 | Nature11159 | Bradycardia Cerebral haemorrhage Depressed level of consciousness Dyskinesia Ejaculation disorder Fear Gangrene Gestational hypertension Hallucination Intranasal paraesthesia Nasal congestion Nasal discomfort Nasal dryness Nervous system disorder Neurosis Orthostatic hypotension Pallor Palpitations Priapism Respiration abnormal Sneezing Somnolence Urinary incontinence Vasoconstriction | G-protein coupled receptor 1 | Heart failure
Hypertension Ischemic heart disease | Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine. | Adrenergic receptor alpha-2 agonist: Apraclonidine, Brimonidine, Clonidine, Dexmedetomidine, Guanabenz, Guanfacine, Levonordefrin, Methyldopa, Methyldopate, Tizanidine Adrenergic receptor alpha-2 antagonist: Mirtazapine |
|
| dfaADA2B | Alpha-2B adrenergic receptor | 462 | 87.85 | 0.553 | Nature11159 | Bradycardia Cerebral haemorrhage Depressed level of consciousness Dyskinesia Fear Gestational hypertension Hallucination Intranasal paraesthesia Nasal congestion Nasal dryness Neurosis Orthostatic hypotension Pallor Respiration abnormal Sneezing Urinary incontinence Vasoconstriction | G-protein coupled receptor 1 | Heart failure
Hypertension Ischemic heart disease | Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline. | Adrenergic receptor alpha agonist: Ergotamine, Naphazoline, Oxymetazoline, Tetrahydrozoline Adrenergic receptor alpha antagonist: Alseroxylon, Ergoloid, Phenoxybenzamine, Phentolamine, Rauwolfia Serpentina, Tolazoline |
|
| dfaADA2C | Alpha-2C adrenergic receptor | 542 | 91.8 | 0.6121 | Nature11159 | Bradycardia Cerebral haemorrhage Depressed level of consciousness Dyskinesia Fear Gestational hypertension Hallucination Intranasal paraesthesia Nasal congestion Nasal dryness Neurosis Orthostatic hypotension Pallor Priapism Respiration abnormal Sneezing Somnolence Urinary incontinence Vasoconstriction | G-protein coupled receptor 1 | Neuropsychiatric disorders
Raynaud's syndrome | Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. | ||
| dfaADRB1 | Beta-1 adrenergic receptor | 1425 | 98.17 | 0.5492 | Nature11159 | Angina pectoris Anxiety Arrhythmia Asthenia Atrioventricular block Bradycardia Bronchospasm Cardiac failure Cardiac failure congestive Deafness transitory Dry eye Fear Hallucination Lung disorder Metabolic disorder Neurotoxicity Palpitations Peripheral coldness Psychotic disorder Raynaud's phenomenon Sleep disorder | G-protein coupled receptor 1 | Anxiety disorder, unspecified
Asthma Cardiac arrhythmias Cardiovascular disease, unspecified Coronary heart disease Dilated cardiomyopathy Glaucoma Hypertension | Beta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximatively equal affinity. | Beta-1 adrenergic receptor agonist: Dobutamine, Dopamine Beta-1 adrenergic receptor antagonist: Acebutolol, Atenolol, Betaxolol, Bisoprolol, Esmolol, Levobetaxolol, Levobunolol, Metipranolol, Metoprolol, Nadolol, Nebivolol, Oxprenolol, Penbutolol, Propafenone, Propranolol, Sotalol, Timolol Beta-1 adrenergic receptor partial agonist: Pindolol |
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| dfaADRB2 | Beta-2 adrenergic receptor | 1617 | 94.91 | 0.4622 | Nature11159 | Angina pectoris Anxiety Arrhythmia Atrioventricular block Bradycardia Bronchospasm Cardiac arrest Cardiac failure Cardiac failure congestive Dry eye Fear Myocardial infarction Neurotoxicity Palpitations Peripheral coldness Raynaud's phenomenon Sleep disorder Tachycardia Tension Tremor Vasodilatation Ventricular arrhythmia | G-protein coupled receptor 1 | Anxiety disorder, unspecified
Asthma Cardiac arrhythmias Chronic obstructive pulmonary disease, unspecified Depression Glaucoma Hypertension Inflammation Multiple sclerosis Obstructive airway disease Respiratory distress syndrome Skeletal muscle wasting Skeletal muscle weakness | Beta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine. | Beta-2 adrenergic receptor agonist: Albuterol, Arformoterol, Bitolterol, Dobutamine, Formoterol, Indacaterol, Isoetharine, Levosalbutamol, Metaproterenol, Pirbuterol, Protokylol, Ritodrine, Salmeterol, Terbutaline, Vilanterol Beta-2 adrenergic receptor antagonist: Esmolol, Levobunolol, Metipranolol, Nadolol, Nebivolol, Oxprenolol, Penbutolol, Propafenone, Propranolol, Sotalol, Timolol Beta-2 adrenergic receptor partial agonist: Pindolol |
|
| dfaADRB3 | Beta-3 adrenergic receptor | 1184 | 99.28 | 0.6375 | Nature11159 | Expressed mainly in adipose tissues. | Angina pectoris Arrhythmia Atrioventricular block Bradycardia Bronchospasm Cardiac failure Cardiac failure congestive Dry eye Hallucination Palpitations Peripheral coldness Psychotic disorder Raynaud's phenomenon Sleep disorder | G-protein coupled receptor 1 | Cardiac arrhythmias
Erectile dysfunction Gain weight in patients with morbid obesity Hypertension Hypertonicity of bladder Noninsulin-dependent diabetes mellitus Obesity Overactive bladder disorder | Beta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. Beta-3 is involved in the regulation of lipolysis and thermogenesis. | Adrenergic receptor beta agonist: Isoproterenol Adrenergic receptor beta antagonist: Carteolol, Carvedilol, Dronedarone Beta-3 adrenergic receptor agonist: Mirabegron |
| dfaAGTR1 | Type-1 angiotensin II receptor | 2049 | 99.73 | 0.7122 | Nature11159 | Liver, lung, adrenal and adrenocortical adenomas. | Dizziness | G-protein coupled receptor 1 | Cardiovascular disease, unspecified
Heart failure Hypertension Ischemic stroke Parkinson's disease | Receptor for angiotensin II. Mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. | Type-1 angiotensin II receptor antagonist: Azilsartan Medoxomil, Candesartan Cilexetil, Eprosartan, Irbesartan, Losartan, Olmesartan Medoxomil, Saralasin, Telmisartan, Valsartan |
| dfaBKRB1 | B1 bradykinin receptor | 779 | 98.98 | 0.6326 | Nature11159 | G-protein coupled receptor 1 | Diabetic nephropathy
Inflammatory diseases Ischemic vascular disease Prostate cancer | This is a receptor for bradykinin. Could be a factor in chronic pain and inflammation. | |||
| dfaBKRB2 | B2 bradykinin receptor | 567 | 90.01 | 0.693 | Nature11159 | Ubiquitous. Widespread in normal smooth muscle tissue and neurons. <a class="attribution" href="P30411#ref5" onclick="ensureReferenceVisible('ref5')">Ref.5</a> | G-protein coupled receptor 1 | Alzheimer's disease
Analgesics Arthritis Asthma Brain Cancer Cardiac hypertrophy Cardiovascular disease, unspecified Cerebral edema Chronic rhinitis Colitis Diabetic disorders Diabetic nephropathy Hepatorenal syndrome Hereditary Angioedema (HAE) Hypertension Liver Disease Lung cancer Myocardial infarction Pancreatitis Pediatric Restenosis Sepsis Tissue injury Traumatic brain injuries Visceral pain | Receptor for bradykinin. It is associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. | Bradykinin B2 receptor antagonist: Icatibant | |
| dfaCCKAR | Cholecystokinin receptor type A | 1992 | 99.68 | 0.4272 | Nature11159 | G-protein coupled receptor 1 | Acid-related diseases
Alcoholism Gastroesophageal Reflux Disease (GERD) Gastrointestinal Diseases and Disorders, miscellaneous Gastrointestinal motility disorders Irritable Bowel Syndrome (IBS) Obesity Pancreatic Cancer | Receptor for cholecystokinin. Has a 1000-fold higher affinity for cck rather than for gastrin. It modulates feeding and dopamine-induced behavior in the central and peripheral nervous system. This receptor mediates its action by association with G protein. | Cholecystokinin A receptor agonist: Ceruletide | ||
| dfaCNR1 | Cannabinoid receptor 1 | 5164 | 96.46 | 0.5241 | Nature11159 | Widely expressed. <a class="attribution" href="P21554#ref4" onclick="ensureReferenceVisible('ref4')">Ref.4</a> | G-protein coupled receptor 1 | Analgesics
Inflammatory bowel disease Migraine Pain, unspecified | Involved in cannabinoid-induced cns effects. Acts by inhibiting adenylate cyclase. Could be a receptor for anandamide. | Cannabinoid CB1 receptor agonist: Dronabinol, Nabilone | |
| dfaDRD1 | D(1A) dopamine receptor | 2145 | 86.42 | 0.5801 | Nature11159 | Detected in caudate, nucleus accumbens and in the olfactory tubercle. <a class="attribution" href="P21728#ref1" onclick="ensureReferenceVisible('ref1')">Ref.1</a> | Agranulocytosis Akathisia Amenorrhoea Cataract Cholestasis Corneal opacity Corneal pigmentation Dermatitis allergic Dermatitis exfoliative Dry mouth Dyskinesia Dystonia Ejaculation disorder Electrocardiogram change Endocrine disorder Extrapyramidal disorder Eyelash discolouration Fibrocystic breast disease Galactorrhoea Gynaecomastia Hypercholesterolaemia Hyperprolactinaemia Hyperthermia Hypothermia Insomnia Lenticular opacities Lipid metabolism disorder Menstrual disorder Miosis Mydriasis Nasal congestion Neuroleptic malignant syndrome Neutropenia Orthostatic hypotension Parkinsonism Photosensitivity reaction Tachycardia Tardive dyskinesia Weight increased | G-protein coupled receptor 1 | Parkinson's disease | This is one of the five types (D1 to D5) of receptors for dopamine, and the activity of this receptor is mediated by g proteins which activate adenylyl cyclase. | Dopamine D1 receptor agonist: Fenoldopam Dopamine D1 receptor antagonist: Methylergonovine |
| dfaDRD2 | D(2) dopamine receptor | 9214 | 93.42 | 0.3498 | Nature11159 | Akathisia Amenorrhoea Cataract Cholestasis Constipation Convulsion Corneal opacity Corneal pigmentation Dermatitis allergic Dermatitis exfoliative Dry mouth Dyskinesia Dystonia Ejaculation disorder Electrocardiogram change Endocrine disorder Erectile dysfunction Extrapyramidal disorder Eyelash discolouration Fibrocystic breast disease Galactorrhoea Gynaecomastia Hypercholesterolaemia Hyperprolactinaemia Hyperthermia Hypothermia Insomnia Lenticular opacities Lipid metabolism disorder Menstrual disorder Miosis Mydriasis Nasal congestion Neuroleptic malignant syndrome Orthostatic hypotension Parkinsonism Sexual dysfunction Tachycardia Tardive dyskinesia Urinary retention Vision blurred Weight increased | G-protein coupled receptor 1 | Anxiety disorder, unspecified
Attention deficit hyperactivity disorder Cocaine dependence Cognitive deficits Delusional disorder Depression Disabling peak-dose dyskinesias Erectile dysfunction Gastric emptying disorders Gilles de la Tourette's disorder Nausea and vomiting Neuroleptic malignant syndrome Neurological diseases Parkinson's disease Psychiatric illness Respiratory diseases Schizophrenia Vomiting | This is one of the five types (D1 to D5) of receptors for dopamine, and the activity of this receptor is mediated by g proteins which activate adenylyl cyclase. | Dopamine D2 receptor agonist: Cabergoline Dopamine D2 receptor antagonist: Acetophenazine, Asenapine, Chlorprothixene, Fluphenazine, Fluphenazine Decanoate, Fluphenazine Enanthate, Iloperidone, Mesoridazine, Metoclopramide, Molindone, Paliperidone, Perphenazine, Prochlorperazine, Thiethylperazine, Thiothixene, Triflupromazine, Trimipramine Dopamine D2 receptor modulator: Benzquinamide Dopamine D2 receptor partial agonist: Aripiprazole |
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| dfaDRD3 | D(3) dopamine receptor | 3627 | 95.12 | 0.4312 | Nature11159 | Brain. | Akathisia Amenorrhoea Dyskinesia Dystonia Ejaculation disorder Electrocardiogram change Extrapyramidal disorder Galactorrhoea Gynaecomastia Hyperprolactinaemia Hyperthermia Hypothermia Menstrual disorder Nasal congestion Neuroleptic malignant syndrome Orthostatic hypotension Parkinsonism Tardive dyskinesia Weight increased | G-protein coupled receptor 1 | Drug dependence
Neurological diseases Psychiatric illness Respiratory diseases Schizophrenia | This is one of the five types (D1 to D5) of receptors for dopamine, and the activity of this receptor is mediated by g proteins which activate adenylyl cyclase. | Dopamine D3 receptor agonist: Levodopa Dopamine D3 receptor antagonist: Chlorprothixene |
| dfaDRD4 | D(4) dopamine receptor | 1963 | 94.62 | 0.3951 | Nature11159 | Akathisia Amenorrhoea Dyskinesia Dystonia Ejaculation disorder Electrocardiogram change Extrapyramidal disorder Galactorrhoea Hypercholesterolaemia Hyperprolactinaemia Hyperthermia Hypothermia Lipid metabolism disorder Menstrual disorder Mydriasis Nasal congestion Neuroleptic malignant syndrome Orthostatic hypotension Parkinsonism Tardive dyskinesia | G-protein coupled receptor 1 | Parkinson's disease
Psychiatric illness Respiratory diseases | This is one of the five types (D1 to D5) of receptors for dopamine, and the activity of this receptor is mediated by g proteins which activate adenylyl cyclase. | Dopamine receptor agonist: Ergoloid, Pergolide Dopamine receptor antagonist: Amoxapine, Pimozide |
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| dfaEDNRA | Endothelin-1 receptor | 2329 | 96.12 | 0.5925 | Nature11159 | Isoform <a href="#P25101" onclick="ensureIsoformSequenceVisible('P25101'); return true;">1</a>, isoform <a href="#P25101-3" onclick="ensureIsoformSequenceVisible('P25101-3'); return true;">3</a> and isoform <a href="#P25101-4" onclick="ensureIsoformSequenceVisible('P25101-4'); return true;">4</a> are expressed in a variety of tissues, with highest levels in the aorta and cerebellum, followed by lung, atrium and cerebral cortex, lower levels in the placenta, kidney, adrenal gland, duodenum, colon, ventricle and liver but no expression in umbilical vein endothelial cells. Within the placenta, isoform <a href="#P25101" onclick="ensureIsoformSequenceVisible('P25101'); return true;">1</a>, isoform <a href="#P25101-2" onclick="ensureIsoformSequenceVisible('P25101-2'); return true;">2</a>, isoform <a href="#P25101-3" onclick="ensureIsoformSequenceVisible('P25101-3'); return true;">3</a> and isoform <a href="#P25101-4" onclick="ensureIsoformSequenceVisible('P25101-4'); return true;">4</a> are expressed in the villi and stem villi vessels. <a class="attribution" href="P25101#ref8" onclick="ensureReferenceVisible('ref8')">Ref.8</a> <a class="attribution" href="P25101#ref16" onclick="ensureReferenceVisible('ref16')">Ref.16</a> | G-protein coupled receptor 1 | Atopic asthma
Cardiovascular disease, unspecified Chronic renal failure Hypertension Ovarian cancer | Receptor for endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. The rank order of binding affinities for ET-A is: ET1 > ET2 >> ET3. | ||
| dfaEDNRB | Endothelin B receptor | 1698 | 96.56 | 0.7162 | Nature11159 | Expressed in placental stem villi vessels, but not in cultured placental villi smooth muscle cells. <a class="attribution" href="P24530#ref19" onclick="ensureReferenceVisible('ref19')">Ref.19</a> | G-protein coupled receptor 1 | Atopic asthma
Glial proliferation Melanoma Neuronal injury | Non-specific receptor for endothelin 1, 2, and 3. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. | Endothelin receptor, ET-A/ET-B antagonist: Ambrisentan, Bosentan | |
| dfaGASR | Gastrin/cholecystokinin type B receptor | 2198 | 96.9 | 0.5357 | Nature11159 | Isoform <a href="#P32239" onclick="ensureIsoformSequenceVisible('P32239'); return true;">1</a> is expressed in brain, pancreas, stomach, the colon cancer cell line LoVo and the T-lymphoblastoma Jurkat, but not in heart, placenta, liver, lung, skeletal muscle, kidney or the stomach cancer cell line AGS. Expressed at high levels in the small cell lung cancer cell line NCI-H510, at lower levels in NCI-H345, NCI-H69 and GLC-28 cell lines, not expressed in GLC-19 cell line. Within the stomach, expressed at high levels in the mucosa of the gastric fundus and at low levels in the antrum and duodenum. Isoform <a href="#P32239-2" onclick="ensureIsoformSequenceVisible('P32239-2'); return true;">2</a> is present in pancreatic cancer cells and colorectal cancer cells, but not in normal pancreas or colonic mucosa. Isoform <a href="#P32239-3" onclick="ensureIsoformSequenceVisible('P32239-3'); return true;">3</a> is expressed in brain, pancreas, stomach, the stomach cancer cell line AGS and the colon cancer cell line LoVo. <a class="attribution" href="P32239#ref3" onclick="ensureReferenceVisible('ref3')">Ref.3</a> <a class="attribution" href="P32239#ref5" onclick="ensureReferenceVisible('ref5')">Ref.5</a> <a class="attribution" href="P32239#ref6" onclick="ensureReferenceVisible('ref6')">Ref.6</a> <a class="attribution" href="P32239#ref7" onclick="ensureReferenceVisible('ref7')">Ref.7</a> <a class="attribution" href="P32239#ref8" onclick="ensureReferenceVisible('ref8')">Ref.8</a> <a class="attribution" href="P32239#ref10" onclick="ensureReferenceVisible('ref10')">Ref.10</a> | G-protein coupled receptor 1 | Acid-related diseases
Anxiety disorder, unspecified Cocaine dependence Gastrin sensitive tumours Gastrointestinal adenocarcinomas Gastrointestinal motility disorders Malignant gliomas Medullary thyroid cancer Neuroendocrine tumors Small cell lung cancer Stromal ovarian tumors | Receptor for gastrin and cholecystokinin, and the ckk-b receptors occur throughout the central nervous system where they modulate anxiety, analgesia, arousal, and neuroleptic activity. this receptor mediates its action by association with G proteins. | ||
| dfaGHSR | Growth hormone secretagogue receptor type 1 | 1170 | 96.95 | 0.4326 | Nature11159 | Pituitary and hypothalamus. | G-protein coupled receptor 1 | Anorexia
Cachexia Cardiovascular disease, unspecified Gastrointestinal Diseases and Disorders, miscellaneous Gastroparesis Ileus Noninsulin-dependent diabetes mellitus | Receptor for ghrelin, coupled to g-alpha-11 proteins. Stimulates growth hormone secretion. Binds also other growth hormone releasing peptides (ghrp) (e.g. Met-enkephalin and ghrp-6) as well as non-peptide, low molecular weight secretagogues. | ||
| dfaHRH1 | Histamine H1 receptor | 1878 | 95.15 | 0.5741 | Nature11159 | Agranulocytosis Akathisia Anticholinergic syndrome Ataxia Bladder disorder Bone marrow disorder Central nervous system stimulation Chest discomfort Conduction disorder Constipation Convulsion Cycloplegia Dermatitis allergic Diabetic eye disease Dry mouth Dystonia Dysuria Euphoric mood Extrapyramidal disorder Galactorrhoea Haemolytic anaemia Hypercholesterolaemia Hyperthermia Hyporeflexia Increased appetite Increased viscosity of bronchial secretion Insomnia Muscular weakness Myopathy Nervousness Parkinsonism Photosensitivity reaction Sedation Skin sensitisation Somnolence Tachycardia Tardive dyskinesia Tinnitus Tremor Urinary retention Urinary tract disorder Vision blurred Weight increased | G-protein coupled receptor 1 | Acute lymphoblastic leukaemia (therapy-refractory)
Allergic diseases Allergic rhinitis, unspecified Anxiety disorder, unspecified Chronic rhinitis Chronic urticaria Epidermal hyperplasia Epilepsy Hypotension Intimal hyperplasia Ischemia Motion sickness Nausea and vomiting Seasonal allergic rhinitis Systemic arterial vasodilation | In peripheral tissues, the h1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neuro. | Histamine H1 receptor agonist: Histamine, Tolazoline Histamine H1 receptor antagonist: Acrivastine, Alcaftadine, Antazoline, Azatadine, Azelastine, Bepotastine, Bromodiphenhydramine, Brompheniramine, Buclizine, Carbinoxamine, Cetirizine, Chlorpheniramine, Chlorpheniramine Polistirex, Clemastine, Cyclizine, Cyproheptadine, Desloratadine, Dexbrompheniramine, Dexchlorpheniramine, Dimenhydrinate, Diphenhydramine, Diphenylpyraline, Doxylamine, Emedastine, Epinastine, Fexofenadine, Hydroxyzine, Ketotifen, Levocabastine, Levocetirizine, Loratadine, Meclizine, Methdilazine, Methylpromazine, Olopatadine, Orphenadrine, Pheniramine, Promethazine, Propiomazine, Pyrilamine, Trimipramine, Tripelennamine, Triprolidine |
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| dfaHRH2 | Histamine H2 receptor | 602 | 82.82 | 0.4221 | Nature11159 | Anticholinergic syndrome Cycloplegia | G-protein coupled receptor 1 | Epidermal hyperplasia
Lasting tachycardia Peptic ulcer Systemic arterial vasodilation Zollinger-Ellison syndrome | The H2 subclass of histamine receptors mediates gastric acid secretion and also appears to regulate gastrointestinal motility and intestinal secretion., and it plays possible role in regulating cell growth and differentiation. | Histamine H2 receptor agonist: Betazole, Tolazoline Histamine H2 receptor antagonist: Cimetidine, Famotidine, Methantheline, Nizatidine, Ranitidine |
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| dfaHRH3 | Histamine H3 receptor | 3756 | 92.81 | 0.2662 | Nature11159 | Expressed predominantly in the CNS, with the greatest expression in the thalamus and caudate nucleus. The various isoforms are mainly coexpressed in brain, but their relative expression level varies in a region-specific manner. Isoform <a href="#Q9Y5N1-3" onclick="ensureIsoformSequenceVisible('Q9Y5N1-3'); return true;">3</a> and isoform <a href="#Q9Y5N1-7" onclick="ensureIsoformSequenceVisible('Q9Y5N1-7'); return true;">7</a> are highly expressed in the thalamus, caudate nucleus and cerebellum while isoform <a href="#Q9Y5N1-5" onclick="ensureIsoformSequenceVisible('Q9Y5N1-5'); return true;">5</a> and isoform <a href="#Q9Y5N1-6" onclick="ensureIsoformSequenceVisible('Q9Y5N1-6'); return true;">6</a> show a poor expression. Isoform <a href="#Q9Y5N1-5" onclick="ensureIsoformSequenceVisible('Q9Y5N1-5'); return true;">5</a> and isoform <a href="#Q9Y5N1-6" onclick="ensureIsoformSequenceVisible('Q9Y5N1-6'); return true;">6</a> show a high expression in the amygdala, substantia nigra, cerebral cortex and hypothalamus. Isoform <a href="#Q9Y5N1-7" onclick="ensureIsoformSequenceVisible('Q9Y5N1-7'); return true;">7</a> is not found in hypothalamus or substantia nigra. | G-protein coupled receptor 1 | Acid-related diseases
Allergic rhinitis, unspecified Alzheimer's disease Attention-deficit hyperactivity disorder Central nervous system diseases Inflammatory diseases Schizophrenia | The h3 subclass of histamine receptors could mediate the histamine signals in cns and peripheral nervous system. Signals through the inhibition of adenylate cyclase and displays high constitutive activity (spontaneous activity in the absence of agonist). | ||
| dfaMC3R | Melanocortin receptor 3 | 708 | 99.4 | 0.6285 | Nature11159 | Brain, placental, and gut tissues. | G-protein coupled receptor 1 | Chronic inflammatory diseases
Gouty arthritis Obesity | Receptor for msh (alpha, beta and gamma) and acth. This receptor is mediated by G proteins which activate adenylate cyclase. | ||
| dfaMC4R | Melanocortin receptor 4 | 2399 | 98.04 | 0.662 | Nature11159 | Brain, placental, and gut tissues. | G-protein coupled receptor 1 | Erectile Dysfunction
Obesity Sexual Dysfunction, Female | Receptor specific to the heptapeptide core common to adrenocorticotropic hormone and alpha-, beta-, and gamma-msh. This receptor is mediated by G proteins that stimulates adenylate cyclase. | ||
| dfaNK1R | Substance-P receptor | 2510 | 96.65 | 0.5334 | Nature11159 | G-protein coupled receptor 1 | Analgesics
Asthma Mood [affective] disorders Neuropathic pain Visceral pain | This is a receptor for the tachykinin neuropeptide substance p. It is probably associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. | Neurokinin 1 receptor antagonist: Aprepitant, Fosaprepitant | ||
| dfaNPY1R | Neuropeptide Y receptor type 1 | 865 | 96.31 | 0.6826 | Nature11159 | G-protein coupled receptor 1 | Analgesics
Anxiety disorder, unspecified Cardiovascular disease, unspecified Convulsions Drug dependence Metabolic disorder, unspecified Obesity Pain, unspecified Rhinitis | Receptor for neuropeptide y and peptide yy. The rank order of affinity of this receptor for pancreatic polypeptides is npy > [pro-34] pyy, pyy and [leu-31, pro-34] npy > npy (2-36) > [ile-31, gln-34] pp and pyy (3-36) > pp > npy free acid. | |||
| dfaNPY2R | Neuropeptide Y receptor type 2 | 560 | 99.51 | 0.6526 | Nature11159 | High levels in amygdala, corpus callosum, hippocampus and subthalamic nucleus. Also detectable in caudate nucleus, hypothalamus and substantia nigra. | G-protein coupled receptor 1 | Obesity | |||
| dfaNTR1 | Neurotensin receptor type 1 | 320 | 100 | 0.8462 | Nature11159 | Expressed in prostate (at protein level). Detected in colon and peripheral blood mononuclear cells. Detected at very low levels in brain. <a class="attribution" href="P30989#ref1" onclick="ensureReferenceVisible('ref1')">Ref.1</a> <a class="attribution" href="P30989#ref4" onclick="ensureReferenceVisible('ref4')">Ref.4</a> | G-protein coupled receptor 1 | Analgesics
Colorectal Cancer Depression Lung Cancer NTR-positive tumors Pain, Acute or Chronic Pancreatic cancer Prostate cancer Psychosis Schizophrenia and Schizoaffective Disorders | Receptor for the tridecapeptide neurotensin. It is associated with G proteins that activate a phosphatidylinositol- calcium second messenger system. | ||
| dfaOPRD | Delta-type opioid receptor | 5430 | 94.07 | 0.3382 | Nature11159 | Biliary colic Bladder disorder Bradycardia Cerebrovascular disorder Constipation Death Dependence Dermatitis contact Drug tolerance Dysuria Euphoric mood Hyperhidrosis Hypothermia Injection site irritation Injection site pain Intracranial pressure increased Mental disorder Miosis Mood altered Muscle spasms Oliguria Orthostatic hypotension Pruritus Respiratory depression Restlessness Shock Somnolence Ureteral spasm Urticaria Withdrawal syndrome | G-protein coupled receptor 1 | Analgesics
Cough Dyspnea Ischemia Pain, unspecified Parkinson's disease | Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Highly stereoselective and receptor for enkephalins. | Opioid receptors; mu/kappa/delta agonist: Codeine, Codeine Polistirex, Hydrocodone, Hydrocodone Polistirex, Nalbuphine, Oxymorphone Opioid receptors; mu/kappa/delta antagonist: Nalmefene, Naloxone, Naltrexone |
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| dfaOPRK | Kappa-type opioid receptor | 4974 | 92.99 | 0.4268 | Nature11159 | Detected in brain and placenta. <a class="attribution" href="P41145#ref1" onclick="ensureReferenceVisible('ref1')">Ref.1</a> <a class="attribution" href="P41145#ref2" onclick="ensureReferenceVisible('ref2')">Ref.2</a> | Biliary colic Bladder disorder Bradycardia Cerebrovascular disorder Coma Constipation Death Dependence Dermatitis contact Drug tolerance Dysphoria Dysuria Euphoric mood Hyperhidrosis Hypothermia Injection site irritation Injection site pain Intracranial pressure increased Mental disorder Miosis Mood altered Muscle spasms Oliguria Orthostatic hypotension Pruritus Respiratory depression Respiratory disorder Restlessness Shock Somnolence Ureteral spasm Withdrawal syndrome | G-protein coupled receptor 1 | Alcohol dependence
Analgesics Behcet's disease Diarrhea Dyspnea Focal ischemia Immune disease Neurodegenerative diseases Pain, unspecified | Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. The receptor for dynorphins and may play a role in arousal and regulation of autonomic and neuroendocrine functions. | Kappa opioid receptor agonist: Anileridine, Buprenorphine Kappa opioid receptor antagonist: Dezocine Kappa opioid receptor partial agonist: Butorphanol, Levallorphan |
| dfaOPRM | Mu-type opioid receptor | 5231 | 89.22 | 0.4073 | Nature11159 | Expressed in brain. Isoform <a href="#P35372-16" onclick="ensureIsoformSequenceVisible('P35372-16'); return true;">16</a> and isoform <a href="#P35372-17" onclick="ensureIsoformSequenceVisible('P35372-17'); return true;">17</a> are detected in brain. <a class="attribution" href="P35372#ref32" onclick="ensureReferenceVisible('ref32')">Ref.32</a> | Biliary colic Biliary tract disorder Bladder disorder Bradycardia Cerebrovascular disorder Coma Constipation Death Dependence Dermatitis contact Disorientation Drug tolerance Dry mouth Dysphoria Dysuria Euphoric mood Hyperhidrosis Hypothermia Injection site irritation Injection site pain Intracranial pressure increased Mental disorder Miosis Mood altered Muscle rigidity Muscle spasms Oliguria Orthostatic hypotension Pruritus Respiratory depression Respiratory disorder Restlessness Shock Somnolence Ureteral spasm Urticaria Withdrawal syndrome | G-protein coupled receptor 1 | Analgesics
Cough Diarrhea Dyspnea Opioid-induced bowel dysfunction Pain, unspecified | Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. The receptor for beta-endorphin. | Mu opioid receptor agonist: Alfentanil, Anileridine, Buprenorphine, Difenoxin, Dihydrocodeine, Diphenoxylate, Fentanyl, Hydromorphone, Levomethadyl Acetate, Levorphanol, Loperamide, Meperidine, Methadone, Morphine, Oxycodone, Propoxyphene, Remifentanil, Sufentanil, Tapentadol, Tramadol Mu opioid receptor antagonist: Alvimopan, Levallorphan, Methylnaltrexone Mu opioid receptor partial agonist: Butorphanol, Dezocine |
| dfaTA2R | Thromboxane A2 receptor | 1154 | 96.31 | 0.6635 | Nature11159 | G-protein coupled receptor 1 | Platelet adhesion | Receptor for thromboxane a2 (txa2), a potent stimulator of platelet aggregation. The activity of this receptor is mediated by a g-protein that activate a phosphatidylinositol-calcium second messenger system. In the kidney, the binding of txa2 to glomerula. | |||
| dfaV1AR | Vasopressin V1a receptor | 960 | 97.16 | 0.5894 | Nature11159 | G-protein coupled receptor 1 | Congestive heart failure
Dysmenorrhea, unspecified Hypertension Raynaud's syndrome Renal diseases Vasoconstriction Water-retaining diseases | Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate a phosphatidyl- inositol-calcium second messenger system. | Vasopressin V1a receptor agonist: Vasopressin Tannate Vasopressin V1a receptor antagonist: Conivaptan |
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| dfaV2R | Vasopressin V2 receptor | 976 | 98.16 | 0.7994 | Nature11159 | Kidney. | G-protein coupled receptor 1 | Cerebral edema
Congestive heart failure Diabetes insipidus Glaucoma Hydronephrosis Hyponatremia Liver cirrhosis Nephrogenic diabetes insipidus Ocular hypertension Renal colic Renal diseases Syndrome of inappropriate secretion of antidiuretic hormone Von Willebrand's disease Water-retaining diseases | Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. | Vasopressin V2 receptor agonist: Vasopressin Tannate Vasopressin V2 receptor antagonist: Conivaptan, Tolvaptan |
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| dfaCRFR1 | Corticotropin-releasing factor receptor 1 | 2124 | 99.88 | 0.4245 | Nature11159 | Predominantly expressed in the cerebellum, pituitary, cerebral cortex and olfactory lobe. <a class="attribution" href="P34998#ref2" onclick="ensureReferenceVisible('ref2')">Ref.2</a> | G-protein coupled receptor 2 | Anxiety Disorders
Depression Innate anxiety Irritable Bowel Syndrome (IBS) Obesity Stress-related disorders | This is a receptor for corticotropin releasing factor. Shows high-affinity crf binding. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. | ||
| dfaS29A1 | Equilibrative nucleoside transporter 1 | 242 | 99.76 | 0.7524 | Nature11159 | SLC29A/ENT transporter | Malaria | Mediates both influx and efflux of nucleosides across the membrane (equilibrative transporter). It is sensitive to low concentrations of the inhibitor nitrobenzylmercaptopurine riboside (nbmpr) and is sodium-independent. | |||
| dfaCAC1B | Voltage-dependent N-type calcium channel subunit alpha-1B | 337 | 92.09 | 0.7725 | Nature11159 | Isoform Alpha-1b-1 and isoform Alpha-1b-2 are expressed in the central nervous system, but not in skeletal muscle or aorta. | Flushing Oedema peripheral | calcium channel alpha-1 subunit | Analgesics
Cardiovascular disease, unspecified Cerebral ischemia Malignant pain Neuropathic pain | Voltage-sensitive calcium channels (vscc) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release and gene expression. | Voltage-gated N-type calcium channel alpha-1B subunit blocker: Levetiracetam, Ziconotide, Ziconotide Acetate |
| dfaCAC1C | Voltage-dependent L-type calcium channel subunit alpha-1C | 532 | 97.59 | 0.6715 | Nature11159 | Expressed in brain, heart, jejunum, ovary, pancreatic beta-cells and vascular smooth muscle. Overall expression is reduced in atherosclerotic vascular smooth muscle. <a class="attribution" href="Q13936#ref2" onclick="ensureReferenceVisible('ref2')">Ref.2</a> <a class="attribution" href="Q13936#ref8" onclick="ensureReferenceVisible('ref8')">Ref.8</a> <a class="attribution" href="Q13936#ref9" onclick="ensureReferenceVisible('ref9')">Ref.9</a> | Arrhythmia Flushing Gingival hyperplasia Oedema peripheral | calcium channel alpha-1 subunit | Heart Disease
Heart transplant | ||
| dfaPDE3A | cGMP-inhibited 3',5'-cyclic phosphodiesterase A | 296 | 97.98 | 0.7446 | Nature11159 | Dyspepsia Palpitations | cyclic nucleotide phosphodiesterase | Bronchial asthma
Chronic myeloid leukemia Vascular disease | Hydrolyzes both cyclic amp (camp) and cyclic gmp (cgmp) (by similarity). | Phosphodiesterase 3A inhibitor: Cilostazol, Dyphylline, Inamrinone, Milrinone, Theophylline | |
| dfaPDE4D | cAMP-specific 3',5'-cyclic phosphodiesterase 4D | 519 | 97.9 | 0.7753 | Nature11159 | Widespread; most abundant in skeletal muscle. Isoform <a href="#Q08499-8" onclick="ensureIsoformSequenceVisible('Q08499-8'); return true;">6</a> is detected in brain. Isoform <a href="#Q08499-9" onclick="ensureIsoformSequenceVisible('Q08499-9'); return true;">8</a> is detected in brain, placenta, lung and kidney. Isoform <a href="#Q08499-11" onclick="ensureIsoformSequenceVisible('Q08499-11'); return true;">7</a> is detected in heart and skeletal muscle. <a class="attribution" href="Q08499#ref6" onclick="ensureReferenceVisible('ref6')">Ref.6</a> | Dyspepsia Flushing | cyclic nucleotide phosphodiesterase | Asthma | Regulates the levels of camp in the cell. | |
| dfaCP2D6 | Cytochrome P450 2D6 | 2980 | 82.88 | 0.3325 | VirtualToxLab | cytochrome P450 | Insomnia | Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants. | |||
| dfaCP3A4 | Cytochrome P450 3A4 | 3975 | 84.75 | 0.3609 | VirtualToxLab | Expressed in prostate and liver. According to some authors, it is not expressed in brain (<a class="attribution" href="#ref19" onclick="ensureReferenceVisible('ref19');">Ref.19</a>). According to others, weak levels of expression are measured in some brain locations (<a class="attribution" href="#ref22" onclick="ensureReferenceVisible('ref22');">Ref.22</a> and <a class="attribution" href="#ref20" onclick="ensureReferenceVisible('ref20');">Ref.20</a>). Also expressed in epithelium of the small intestine and large intestine, bile duct, nasal mucosa, kidney, adrenal cortex, epithelium of the gastric mucosa with intestinal metaplasia, gallbladder, intercalated ducts of the pancreas, chief cells of the parathyroid and the corpus luteum of the ovary (at protein level). <a class="attribution" href="P08684#ref12" onclick="ensureReferenceVisible('ref12')">Ref.12</a> <a class="attribution" href="P08684#ref13" onclick="ensureReferenceVisible('ref13')">Ref.13</a> <a class="attribution" href="P08684#ref14" onclick="ensureReferenceVisible('ref14')">Ref.14</a> <a class="attribution" href="P08684#ref19" onclick="ensureReferenceVisible('ref19')">Ref.19</a> <a class="attribution" href="P08684#ref20" onclick="ensureReferenceVisible('ref20')">Ref.20</a> <a class="attribution" href="P08684#ref22" onclick="ensureReferenceVisible('ref22')">Ref.22</a> | Abdominal pain upper Diabetes mellitus Headache Hyperlipidaemia Lipodystrophy acquired Oedema peripheral | cytochrome P450 | Hypothalamic-pituitary ACTH function | ||
| dfaAOFA | Amine oxidase [flavin-containing] A | 1898 | 81.54 | 0.522 | Nature11159 | Heart, liver, duodenum, blood vessels and kidney. | Dry mouth Hyperhidrosis Irritability Mania Psychotic disorder | flavin monoamine oxidase | Depression
Mood [affective] disorders Social phobias | Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. Mao-A preferentially oxidizes biogenic amines. | |
| dfa5HT3A | 5-hydroxytryptamine receptor 3A | 618 | 90.67 | 0.6388 | Nature11159 | Expressed in cerebral cortex, amygdala, hippocampus, and testis. Detected in monocytes of the spleen and tonsil, in small and large intestine, uterus, prostate, ovary and placenta. <a class="attribution" href="P46098#ref13" onclick="ensureReferenceVisible('ref13')">Ref.13</a> | ligand-gated ion channel | Alcohol dependence
Alcoholism Irritable bowel syndrome Nausea and vomiting Pruritus | This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel. | Serotonin 3a (5-HT3a) receptor antagonist: Alosetron, Dolasetron, Granisetron, Metoclopramide, Ondansetron, Palonosetron | |
| dfaGBRA1 | Gamma-aminobutyric acid receptor subunit alpha-1 | 705 | 95.8 | 0.6357 | Nature11159 | Agitation Amnesia Apnoea Ataxia Cholestasis Confusional state Dependence Dermatitis exfoliative Dysarthria Erythema multiforme Folate deficiency Gangrene Hiccups Hypoprothrombinaemia Hypotension Incontinence Irritability Jaundice Laryngospasm Libido disorder Necrosis Nystagmus Respiratory depression Respiratory disorder Salivary gland disorder Somnolence Speech disorder Thrombophlebitis Urinary retention | ligand-gated ion channel | Anxiety disorders
Insomnia | |||
| dfaANDR | Androgen receptor | 1728 | 92.18 | 0.4444 | Nature11159 VirtualToxLab | Isoform <a href="#P10275-2" onclick="ensureIsoformSequenceVisible('P10275-2'); return true;">2</a> is mainly expressed in heart and skeletal muscle. <a class="attribution" href="P10275#ref7" onclick="ensureReferenceVisible('ref7')">Ref.7</a> | Acne Amenorrhoea Azoospermia Bone disorder Breast pain Cushingoid Depression Electrolyte imbalance Endocrine disorder Epiphyses premature fusion Gynaecomastia Hepatic function abnormal Hirsutism Hypercalcaemia Infertility Jaundice cholestatic Libido decreased Menstrual disorder Metrorrhagia Oedema Osteoporosis Priapism Virilism Weight increased | nuclear hormone receptor | Prostate cancer
Spinal and bulbar muscular atrophy | The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. | Androgen Receptor agonist: Danazol, Dromostanolone Propionate, Ethylestrenol, Fluoxymesterone, Methyltestosterone, Nandrolone Decanoate, Nandrolone Phenpropionate, Oxandrolone, Oxymetholone, Stanozolol, Testosterone, Testosterone Cypionate, Testosterone Enanthate, Testosterone Propionate Androgen Receptor antagonist: Bicalutamide, Enzalutamide, Flutamide, Nilutamide |
| dfaESR1 | Estrogen receptor alpha | 2157 | 99.13 | 0.6769 | Nature11159 VirtualToxLab | Acne Blood urea increased Bone disorder Breast pain Chloasma Depression Electrolyte imbalance Embolism arterial Endometrial cancer Endometrial hyperplasia Epiphyses premature fusion Erythema multiforme Fibrocystic breast disease Gynaecomastia Hepatic function abnormal Hypercalcaemia Jaundice Menstrual disorder Metrorrhagia Neoplasm Oedema Porphyria non-acute Sodium retention Urticaria Uterine inflammation Weight increased | nuclear hormone receptor | Brain injury
Breast cancer Cardiovascular disease, unspecified Coronary atherosclerosis Endocrine independent cancer Neurodegenerative diseases Osteoporosis, unspecified Postmenopausal symptoms | Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. | ||
| dfaESR2 | Estrogen receptor beta | 1897 | 93.82 | 0.6581 | Nature11159 VirtualToxLab | Isoform beta-1 is expressed in testis and ovary, and at a lower level in heart, brain, placenta, liver, skeletal muscle, spleen, thymus, prostate, colon, bone marrow, mammary gland and uterus. Also found in uterine bone, breast, and ovarian tumor cell lines, but not in colon and liver tumors. Isoform beta-2 is expressed in spleen, thymus, testis and ovary and at a lower level in skeletal muscle, prostate, colon, small intestine, leukocytes, bone marrow, mammary gland and uterus. Isoform beta-3 is found in testis. Isoform beta-4 is expressed in testis, and at a lower level in spleen, thymus, ovary, mammary gland and uterus. Isoform beta-5 is expressed in testis, placenta, skeletal muscle, spleen and leukocytes, and at a lower level in heart, lung, liver, kidney, pancreas, thymus, prostate, colon, small intestine, bone marrow, mammary gland and uterus. Not expressed in brain. | Acne Blood urea increased Bone disorder Breast pain Chloasma Depression Electrolyte imbalance Endometrial cancer Endometrial hyperplasia Epiphyses premature fusion Erythema multiforme Fibrocystic breast disease Gynaecomastia Hepatic function abnormal Hypercalcaemia Jaundice Menstrual disorder Metrorrhagia Neoplasm Oedema Porphyria non-acute Sodium retention Urticaria Uterine inflammation Weight increased | nuclear hormone receptor | Breast cancer
Cardiovascular disease, unspecified ER beta-positive prostate tumors Neurodegenerative diseases Vascular injury response | Nuclear hormone receptor. binds estrogens with an affinity similar to that of esr1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability. | Estrogen receptor beta: Estramustine Phosphate Estrogen receptor beta modulator: Chlorotrianisene, Raloxifene |
| dfaGCR | Glucocorticoid receptor | 1555 | 97.91 | 0.6225 | Nature11159 VirtualToxLab | Widely expressed. In the heart, detected in left and right atria, left and right ventricles, aorta, apex, intraventricular septum, and atrioventricular node as well as whole adult and fetal heart. <a class="attribution" href="P04150#ref21" onclick="ensureReferenceVisible('ref21')">Ref.21</a> | Acne Adrenal disorder Adrenal insufficiency Adrenal suppression Amenorrhoea Bone disorder Calcium metabolism disorder Cataract Cushingoid Depression Dysphonia Embolism arterial Endocrine disorder Epidural lipomatosis Epistaxis Euphoric mood Fluid retention Foot and mouth disease Fracture Fungal infection Glaucoma Growth retardation Hyperglycaemia Hypertension Hypertrichosis Hypokalaemia Impaired healing Increased appetite Intracranial pressure increased Menstrual disorder Muscular weakness Nitrogen balance negative Oedema Oral candidiasis Osteonecrosis Osteoporosis Pancreatic disorder Pancreatitis acute Peptic ulcer Phosphorus metabolism disorder Sepsis Skin atrophy Skin striae Superinfection Telangiectasia | nuclear hormone receptor | Cocaine dependence
Drug dependence Major depressive disorder | Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (gre) and as a modulator of other transcription factors. Affects inflammatory responses and cellular proliferation. | Glucocorticoid receptor agonist: Alclometasone Dipropionate, Amcinonide, Beclomethasone Dipropionate, Betamethasone, Betamethasone Acetate, Betamethasone Benzoate, Betamethasone Dipropionate, Betamethasone Phosphoric Acid, Betamethasone Valerate, Budesonide, Ciclesonide, Clobetasol Propionate, Clocortolone Pivalate, Cortisone Acetate, Desonide, Desoximetasone, Dexamethasone, Dexamethasone Acetate, Dexamethasone Phosphoric Acid, Diflorasone Diacetate, Difluprednate, Flumethasone Pivalate, Flunisolide, Fluocinolone Acetonide, Fluocinonide, Fluorometholone, Fluorometholone Acetate, Fluprednisolone, Flurandrenolide, Fluticasone Furoate, Fluticasone Propionate, Halcinonide, Halobetasol Propionate, Hydrocortamate, Hydrocortisone, Hydrocortisone Acetate, Hydrocortisone Butyrate, Hydrocortisone Cypionate, Hydrocortisone Hemisuccinate, Hydrocortisone Phosphoric Acid, Hydrocortisone Probutate, Hydrocortisone Valerate, Loteprednol Etabonate, Medrysone, Meprednisone, Methylprednisolone, Methylprednisolone Hemisuccinate, Mometasone Furoate, Paramethasone Acetate, Prednicarbate, Prednisolone, Prednisolone Acetate, Prednisolone Phosphoric Acid, Prednisolone Tebutate, Prednisone, Rimexolone, Triamcinolone, Triamcinolone Acetonide, Triamcinolone Diacetate, Triamcinolone Hexacetonide Glucocorticoid receptor antagonist: Mifepristone |
| dfaMCR | Mineralocorticoid receptor | 598 | 88.09 | 0.5528 | VirtualToxLab | Ubiquitous. Highly expressed in distal tubules, convoluted tubules and cortical collecting duct in kidney, and in sweat glands. Detected at lower levels in cardiomyocytes, in epidermis and in colon enterocytes. <a class="attribution" href="P08235#ref2" onclick="ensureReferenceVisible('ref2')">Ref.2</a> <a class="attribution" href="P08235#ref10" onclick="ensureReferenceVisible('ref10')">Ref.10</a> | Acne Adrenal insufficiency Amenorrhoea Cushingoid Depression Embolism arterial Endocrine disorder Euphoric mood Hyperglycaemia Hypokalaemia Menstrual disorder Muscular weakness Oedema Osteoporosis Peptic ulcer | nuclear hormone receptor | Autoimmune and sudden sensorineural hearing loss
Brain injury | Receptor for both mineralocorticoids (MC) such as aldosterone and glucocorticoids (GC) such as corticosterone or cortisol. binds to mineralocorticoid response elements (MRE) and transactivates target genes. The effect of MC is to increase ion. | Mineralocorticoid receptor agonist: Desoxycorticosterone Acetate, Desoxycorticosterone Pivalate, Fludrocortisone Acetate Mineralocorticoid receptor antagonist: Drospirenone, Eplerenone, Felodipine, Nimodipine, Spironolactone |
| dfaNR1H2 | Oxysterols receptor LXR-beta | 544 | 98.31 | 0.7432 | VirtualToxLab | Ubiquitous. | nuclear hormone receptor | Atherosclerosis
Dyslipidemia | Orphan receptor. Binds preferentially to double-stranded oligonucleotide direct repeats having the consensus half-site sequence 5'-aggtca-3' and 4-nt spacing (dr-4). | ||
| dfaNR1H3 | Oxysterols receptor LXR-alpha | 507 | 99.09 | 0.6632 | VirtualToxLab | Visceral organs specific expression. Strong expression was found in liver, kidney and intestine followed by spleen and to a lesser extent the adrenals. | nuclear hormone receptor | Atherosclerosis
Cancer, unspecific | Orphan receptor. Interaction with rxr shifts rxr from its role as a silent dna-binding partner to an active ligand- binding subunit in mediating retinoid responses through target genes defined by lxres. Lxres are dr4-type response elements. | ||
| dfaNR1I2 | Nuclear receptor subfamily 1 group I member 2 | 164 | 97.97 | 0.8234 | Nature11159 | Expressed in liver, colon and small intestine. | Hepatitis | nuclear hormone receptor | Anxiety disorder, unspecified
Depression Eye inflammation Multiple Sclerosis | Orphan receptor; Its natural ligand is probably pregnane. Binds to a response element in the cyp3a4 gene promoter. activates its expression in response to a wide variety of endobiotics and xenobiotics. | |
| dfaPPARA | Peroxisome proliferator-activated receptor alpha | 2182 | 98.75 | 0.4846 | Skeletal muscle, liver, heart and kidney. <a class="attribution" href="Q07869#ref2" onclick="ensureReferenceVisible('ref2')">Ref.2</a> <a class="attribution" href="Q07869#ref3" onclick="ensureReferenceVisible('ref3')">Ref.3</a> | Myalgia | nuclear hormone receptor | Hyperglycemia
Hyperinsulinemia Insulin resistance Lipid metabolic disorders Obesity | Receptor that bind peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the receptor binds to a promoter element in the gene for acyl-coa oxidase and activates its transcription. It therefore controls the perox[UniProt] | Peroxisome proliferator-activated receptor alpha agonist: Clofibrate, Fenofibrate, Fenofibric Acid, Gemfibrozil | |
| dfaPPARD | Peroxisome proliferator-activated receptor delta | 1328 | 97.42 | 0.5955 | Ubiquitous with maximal levels in placenta and skeletal muscle. | nuclear hormone receptor | Atherosclerosis
Hyperlipidemia Inflammation Metabolic Disease Metabolic syndrome X Noninsulin-dependent diabetes mellitus Obesity Skin diseases | Receptor that bind peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the receptor binds to a promoter element in the gene for acyl-coa oxidase and activates its transcription. | |||
| dfaPPARG | Peroxisome proliferator-activated receptor gamma | 2654 | 95.68 | 0.5443 | VirtualToxLab | Highest expression in adipose tissue. Lower in skeletal muscle, spleen, heart and liver. Also detectable in placenta, lung and ovary. <a class="attribution" href="P37231#ref1" onclick="ensureReferenceVisible('ref1')">Ref.1</a> | Dyspepsia | nuclear hormone receptor | Not Available | Peroxisome proliferator-activated receptor gamma agonist: Balsalazide, Mesalamine, Olsalazine, Pioglitazone, Rosiglitazone, Troglitazone | |
| dfaPRGR | Progesterone receptor | 1387 | 93.86 | 0.6158 | Nature11159 VirtualToxLab | Acne Amenorrhoea Biliary tract disorder Breast pain Depression Fibrocystic breast disease Gynaecomastia Hirsutism Jaundice cholestatic Libido disorder Menstrual disorder Metrorrhagia Migraine Oedema Urticaria Weight increased | nuclear hormone receptor | Breast cancer | The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. | Progesterone receptor agonist: Danazol, Desogestrel, Drospirenone, Dydrogesterone, Ethynodiol Diacetate, Etonogestrel, Fluticasone Propionate, Hydroxyprogesterone Caproate, Levonorgestrel, Medroxyprogesterone Acetate, Megestrol Acetate, Norelgestromin, Norethindrone, Norethindrone Acetate, Norethynodrel, Norgestimate, Norgestrel, Progesterone Progesterone receptor antagonist: Mifepristone Progesterone receptor modulator: Ulipristal Acetate |
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| dfaTHA | Thyroid hormone receptor alpha | 429 | 98.66 | 0.715 | VirtualToxLab | nuclear hormone receptor | Thyrotoxicosis [hyperthyroidism] | Nuclear hormone receptor. High affinity receptor for triiodothyronine. | Thyroid hormone receptor agonist: Dextrothyroxine, Levothyroxine, Liothyronine | ||
| dfaTHB | Thyroid hormone receptor beta | 541 | 99.81 | 0.8658 | VirtualToxLab | nuclear hormone receptor | Hyperlipidemia
Obesity Thyroid hormone resistance syndrome Thyrotoxicosis [hyperthyroidism] | High affinity receptor for triiodothyronine. | |||
| dfaACE | Angiotensin-converting enzyme | 1364 | 95.51 | 0.4488 | Angioedema Cough Dysgeusia Palpitations Pancreatitis | peptidase M2 | Chronic obstructive pulmonary disease, unspecified
Heart failure Hypertension Vascular disease | Converts angiotensin i to angiotensin ii by release of the terminal his-leu, this results in an increase of the vasoconstrictor activity of angiotensin. Also able to inactivate bradykinin, a potent vasodilatator. | |||
| dfaTHRB | Prothrombin | 6150 | 96.22 | 0.4523 | Expressed by the liver and secreted in plasma. | peptidase S1 | Coagulative disorders
Coronary atherosclerosis Gliomas Heparin-induced thrombocytopenia type II Multiple organ failure Thromboembolic disorders Thrombosis Thrombotic disease | Thrombin, which cleaves bonds after arg and lys, converts fibrinogen to fibrin and activates factors v, vii, viii, xiii, and, in complex with thrombomodulin, protein c. | Thrombin inhibitor: Argatroban, Bivalirudin, Dabigatran Etexilate, Desirudin, Lepirudin | ||
| dfaKCNH2 | HERG | 6071 | 90.79 | 0.3258 | Nature11159 VirtualToxLab | Highly expressed in heart and brain. Isoforms USO are frequently overexpressed in cancer cells. <a class="attribution" href="Q12809#ref6" onclick="ensureReferenceVisible('ref6')">Ref.6</a> | Electrocardiogram QT prolonged | potassium channel | Cardiac arrhythmias | Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. channel properties are modulated by camp and subunit assembly. Mediates the rapidly activating component of the delayed rectifying potassium current in heart (ikr). | HERG blocker: Amiodarone, Dofetilide, Dronedarone, Ibutilide, Sotalol |
| dfaPGH1 | Prostaglandin G/H synthase 1 | 3238 | 77.66 | 0.303 | Nature11159 | Abdominal pain upper Aplastic anaemia Asthma Dyspepsia Erythema multiforme Gastrointestinal haemorrhage Haematuria Haemorrhagic diathesis Hepatitis Nephropathy Oedema Peptic ulcer Pruritus Rash Renal failure Renal tubular disorder Thrombocytopenia Tinnitus Toxic epidermal necrolysis | prostaglandin G/H synthase | Cardiovascular disease, unspecified
Chronic inflammatory diseases | May play an important role in regulating or promoting cell proliferation in some normal and neoplastically transformed cells. | ||
| dfaPGH2 | Prostaglandin G/H synthase 2 | 3521 | 91.54 | 0.3445 | Nature11159 | Abdominal pain upper Aplastic anaemia Dyspepsia Erythema multiforme Flatulence Gastrointestinal haemorrhage Haematuria Haemorrhagic diathesis Hepatitis Nephropathy Oedema Oliguria Peptic ulcer Pruritus Renal failure Thrombocytopenia Tinnitus | prostaglandin G/H synthase | Abdominal aortic aneurysm
Adenomatous polyposis Alzheimer's disease Analgesics Arthritis Bladder cancer Breast cancer Cancer, unspecific Carcinoma in situ, unspecified Carpal tunnel syndrome Colorectal cancer Dysmenorrhea, unspecified Endometriosis Genitourinary tumors Gestational hypertension Inflammation Inflammatory diseases Lung cancer Malignant mesothelioma Meningioma Myocardial infarction Oropharyngeal squamous cell carcinoma Osteoarthritis Pain, unspecified Pathological angiogenesis Peutz-Jeghers syndrome Prostate cancer Pyresis Renal cell carcinoma Rheumatoid arthritis, unspecified Stroke Vascular lesion regression | May have a role as a major mediator of inflammation and/or a role for prostanoid signaling in activity-dependent plasticity. | Cyclooxygenase inhibitor: Acetaminophen, Aminosalicylic Acid, Aspirin, Balsalazide, Bismuth Subsalicylate, Bromfenac, Diclofenac, Diflunisal, Fenoprofen, Flurbiprofen, Ibuprofen, Indomethacin, Ketoprofen, Ketorolac, Meclofenamic Acid, Mefenamic Acid, Mesalamine, Naproxen, Nepafenac, Olsalazine, Oxaprozin, Oxyphenbutazone, Phenylbutazone, Piroxicam, Sulfasalazine, Sulindac, Suprofen, Tolmetin Cyclooxygenase-2 inhibitor: Carprofen, Celecoxib, Etodolac, Meloxicam, Nabumetone, Rofecoxib, Valdecoxib |
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| dfaSCN5A | Sodium channel protein type 5 subunit alpha | 428 | 99.59 | 0.4059 | Nature11159 | Found in jejunal circular smooth muscle cells (at protein level). Expressed in human atrial and ventricular cardiac muscle but not in adult skeletal muscle, brain, myometrium, liver, or spleen. Isoform <a href="#Q14524-4" onclick="ensureIsoformSequenceVisible('Q14524-4'); return true;">4</a> is expressed in brain. <a class="attribution" href="Q14524#ref2" onclick="ensureReferenceVisible('ref2')">Ref.2</a> <a class="attribution" href="Q14524#ref15" onclick="ensureReferenceVisible('ref15')">Ref.15</a> | Apnoea Cardiac arrest Central nervous system stimulation Coma Corneal disorder Death Diplopia Dysarthria Foetal damage Hypoaesthesia oral Impaired healing Keratitis Loss of consciousness Methaemoglobinaemia Muscle twitching Myocardial depression Nervousness Nystagmus Presyncope Respiratory failure Sensitisation Tinnitus Tremor Ventricular fibrillation Vision blurred | sodium channel | Analgesics
Cardiac dysrhythmias Epileptic seizures Pain Refractory partial epilepsy Sustained ventricular tachycardia | Sodium channel protein type V alpha subunit blocker: Dibucaine, Flecainide, Ranolazine | |
| dfaSC6A2 | Sodium-dependent noradrenaline transporter | 2679 | 95.41 | 0.5393 | Nature11159 | Anticholinergic syndrome Blood glucose abnormal Conduction disorder Cycloplegia Dry mouth Ejaculation disorder Erectile dysfunction Hyperhidrosis Hypomania Insomnia Mania Orthostatic hypotension Palpitations Psychotic disorder Schizophrenia Sexual dysfunction Sleep disorder Tremor Weight decreased | sodium:neurotransmitter symporter | Depression | Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals. | Norepinephrine transporter inhibitor: Amitriptyline, Amoxapine, Atomoxetine, Bupropion, Desipramine, Desvenlafaxine, Dexmethylphenidate, Diethylpropion, Doxepin, Duloxetine, Imipramine, Maprotiline, Methylphenidate, Milnacipran, Nefazodone, Nortriptyline, Orphenadrine, Phendimetrazine, Phenmetrazine, Protriptyline, Tapentadol, Trimipramine, Venlafaxine Norepinephrine transporter releasing agent: Amphetamine, Benzphetamine, Dextroamphetamine, Lisdexamfetamine, Phentermine, Phenylpropanolamine, Phenylpropanolamine Polistirex, Pseudoephedrine, Pseudoephedrine Polistirex Norepinephrine transporter substrate: Bethanidine, Bretylium, Guanadrel, Guanethidine |
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| dfaSC6A3 | Sodium-dependent dopamine transporter | 5191 | 96.46 | 0.5681 | Nature11159 | Dry mouth Ejaculation disorder Hyperhidrosis Insomnia Mydriasis Nervousness Palpitations Restlessness Tachycardia Tremor | sodium:neurotransmitter symporter | Parkinson's disease | Amine transporter, terminating the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals. | Dopamine transporter inhibitor: Armodafinil, Bupropion, Dexmethylphenidate, Diethylpropion, Methylphenidate, Modafinil, Phendimetrazine, Phenmetrazine Dopamine transporter releasing agent: Amphetamine, Dextroamphetamine, Lisdexamfetamine |
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| dfaSC6A4 | Sodium-dependent serotonin transporter | 6903 | 95.43 | 0.4076 | Nature11159 | Expressed in platelets (at protein level). <a class="attribution" href="P31645#ref11" onclick="ensureReferenceVisible('ref11')">Ref.11</a> | Anticholinergic syndrome Blood glucose abnormal Conduction disorder Cycloplegia Dependence Dry mouth Erectile dysfunction Extrapyramidal disorder Galactorrhoea Hyperhidrosis Hypomania Insomnia Libido disorder Mania Nervousness Orthostatic hypotension Palpitations Psychotic disorder Schizophrenia Sexual dysfunction Sleep disorder Tachycardia Tremor Urinary retention Weight decreased | sodium:neurotransmitter symporter | Schizophrenia | Terminates the action of serotonin by its high affinity sodium-dependent reuptake into presynaptic terminals. | Serotonin transporter inhibitor: Amitriptyline, Amoxapine, Citalopram, Clomipramine, Desvenlafaxine, Duloxetine, Escitalopram, Fluoxetine, Fluvoxamine, Imipramine, Milnacipran, Nefazodone, Nortriptyline, Paroxetine, Protriptyline, Sertraline, Trazodone, Venlafaxine, Vilazodone Serotonin transporter substrate: Chlorphentermine |
| dfaACES | Acetylcholinesterase | 3978 | 86.13 | 0.4493 | Isoform <a href="#P22303-2" onclick="ensureIsoformSequenceVisible('P22303-2'); return true;">H</a> is highly expressed in erythrocytes. <a class="attribution" href="P22303#ref11" onclick="ensureReferenceVisible('ref11')">Ref.11</a> | Diarrhoea Nausea Salivary hypersecretion | type-B carboxylesterase/lipase | Alzheimer's disease
Cognitive deficits Hypoxic-ischemic encephalopathy Motor neurone disease Parkinson's disease | Rapidly hydrolyzes choline released into the synapse. | Acetylcholinesterase activator: Pralidoxime Acetylcholinesterase inhibitor: Ambenonium, Demecarium, Donepezil, Echothiophate, Edrophonium, Galantamine, Hexafluorenium, Isoflurophate, Neostigmine, Pyridostigmine |
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