Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T81183
|
||||
| Former ID |
TTDS00027
|
||||
| Target Name |
Alpha-1 adrenergic receptor
|
||||
| Synonyms |
Alpha1-adrenoceptor
|
||||
| Target Type |
Successful
|
||||
| Disease | Congestive heart failure [ICD9: 428; ICD10: I50] | ||||
| Cardiotonic [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] | |||||
| Orthostatic hypotension [ICD9: 458; ICD10: I95.1] | |||||
| Obesity [ICD9: 278; ICD10: E66] | |||||
| BioChemical Class |
GPCR rhodopsin
|
||||
| Target Validation |
T81183
|
||||
| Drugs and Mode of Action | |||||
| Drug(s) | Carvedilol | Drug Info | Approved | Congestive heart failure | [1], [2] |
| Ergotamine | Drug Info | Approved | Headache | [3], [4] | |
| Labetalol | Drug Info | Approved | Hypertension | [5], [6] | |
| Midodrine | Drug Info | Approved | Orthostatic hypotension | [7], [8] | |
| Prazosin | Drug Info | Approved | Hypertension; Symptomatic benign prostatic hyperplasia; Severe congestive heart failure | [9] | |
| Urapidil | Drug Info | Approved | Hypertension | [9] | |
| Phenylpropanolamine | Drug Info | Withdrawn from market | Obesity | [10] | |
| Metazosin | Drug Info | Discontinued in Phase 3 | Cardiotonic | [11] | |
| DC-015 | Drug Info | Terminated | Discovery agent | [12] | |
| Antagonist | Carvedilol | Drug Info | [13] | ||
| DC-015 | Drug Info | [14] | |||
| Labetalol | Drug Info | [13] | |||
| Metazosin | Drug Info | [15] | |||
| Prazosin | Drug Info | [16], [17] | |||
| Urapidil | Drug Info | [18] | |||
| Agonist | Ergotamine | Drug Info | [3] | ||
| Midodrine | Drug Info | [19] | |||
| Phenylpropanolamine | Drug Info | [20] | |||
| References | |||||
| REF 1 | Natural 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 2 | (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 3 | Reversal of ergotamine-induced vasospasm following methylprednisolone. Clin Toxicol (Phila). 2008 Dec;46(10):1074-6. | ||||
| REF 4 | (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 5 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074787. | ||||
| REF 6 | (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 7 | Emerging drugs for complications of end-stage liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):159-74. | ||||
| REF 8 | (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 9 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
| REF 10 | Pharmacotherapy for obesity. Drugs. 2005;65(10):1391-418. | ||||
| REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002056) | ||||
| REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006738) | ||||
| REF 13 | Beta-blockers in the treatment of hypertension: are there clinically relevant differences? Postgrad Med. 2009 May;121(3):90-8. | ||||
| REF 14 | Antihypertensive 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 15 | Metazosin tablets (Kenosin) in the treatment of chronic congestive heart failure. Cas Lek Cesk. 1995 Sep 20;134(18):590-3. | ||||
| REF 16 | Characterization of alpha-adrenoceptor subtypes in smooth muscle of equine ileum. Am J Vet Res. 2001 Sep;62(9):1370-4. | ||||
| REF 17 | Adventitia removal does not modify the alphaID-adrenoceptors response in aorta during hypertension and ageing. Auton Autacoid Pharmacol. 2009 Jul;29(3):117-33. | ||||
| REF 18 | Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55. | ||||
| REF 19 | Orthostatic hypotension in patients with Parkinson's disease: pathophysiology and management. Drugs Aging. 2001;18(7):495-505. | ||||
| REF 20 | Synthesis 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. | ||||
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