Target Information

Target General Infomation
Target ID
T81183
Former ID
TTDS00027
Target Name
Alpha-1 adrenergic receptor
Synonyms
Alpha1-adrenoceptor
Target Type
Successful
Disease Cardiotonic [ICD10: I50]
Congestive heart failure [ICD9: 428; ICD10: I50]
Hypertension; Symptomatic benign prostatic hyperplasia; Severe congestive heart failure [ICD10: I10-I16]
Hypertension [ICD9: 401; ICD10: I10-I16]
Headache [ICD9: 339, 784.0; ICD10: G43-G44, R51]
Obesity [ICD9: 278; ICD10: E66]
Orthostatic hypotension [ICD9: 458; ICD10: I95.1]
BioChemical Class
GPCR rhodopsin
Target Validation
T81183
Drugs and Mode of Action
Drug(s) Carvedilol Drug Info Approved Congestive heart failure [536361], [540906]
Ergotamine Drug Info Approved Headache [536832], [538937]
Labetalol Drug Info Approved Hypertension [538284], [542221]
Midodrine Drug Info Approved Orthostatic hypotension [536650], [542257]
Prazosin Drug Info Approved Hypertension; Symptomatic benign prostatic hyperplasia; Severe congestive heart failure [551871]
Urapidil Drug Info Approved Hypertension [551871]
Phenylpropanolamine Drug Info Withdrawn from market Obesity [536103]
Metazosin Drug Info Discontinued in Phase 3 Cardiotonic [545078]
DC-015 Drug Info Terminated Discovery agent [546169]
Antagonist Carvedilol Drug Info [537409]
DC-015 Drug Info [535307]
Labetalol Drug Info [537409]
Metazosin Drug Info [537827]
Prazosin Drug Info [535260], [537558]
Urapidil Drug Info [538139]
Agonist Ergotamine Drug Info [536832]
Midodrine Drug Info [535227]
Phenylpropanolamine Drug Info [535972]
References
Ref 536103Pharmacotherapy for obesity. Drugs. 2005;65(10):1391-418.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 536650Emerging drugs for complications of end-stage liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):159-74.
Ref 536832Reversal of ergotamine-induced vasospasm following methylprednisolone. Clin Toxicol (Phila). 2008 Dec;46(10):1074-6.
Ref 538284FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074787.
Ref 538937(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 149).
Ref 540906(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 551).
Ref 542221(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7207).
Ref 542257(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7240).
Ref 545078Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002056)
Ref 546169Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006738)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 535227Orthostatic hypotension in patients with Parkinson's disease: pathophysiology and management. Drugs Aging. 2001;18(7):495-505.
Ref 535260Characterization of alpha-adrenoceptor subtypes in smooth muscle of equine ileum. Am J Vet Res. 2001 Sep;62(9):1370-4.
Ref 535307Antihypertensive and Hypolipidemic Effects of DC-015, a Novel, Potent and Specific alpha(1)-Adrenoceptor Antagonist: Comparison with Prazosin in Spontaneously Hypertensive Rats. J Biomed Sci. 1996 Apr;3(2):108-116.
Ref 535972Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist. J Med Chem. 2004 Jun 3;47(12):3220-35.
Ref 536832Reversal of ergotamine-induced vasospasm following methylprednisolone. Clin Toxicol (Phila). 2008 Dec;46(10):1074-6.
Ref 537409Beta-blockers in the treatment of hypertension: are there clinically relevant differences? Postgrad Med. 2009 May;121(3):90-8.
Ref 537558Adventitia removal does not modify the alphaID-adrenoceptors response in aorta during hypertension and ageing. Auton Autacoid Pharmacol. 2009 Jul;29(3):117-33.
Ref 537827Metazosin tablets (Kenosin) in the treatment of chronic congestive heart failure. Cas Lek Cesk. 1995 Sep 20;134(18):590-3.
Ref 538139Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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