Target Information
| Target General Information | Top | |||||
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| Target ID |
T81183
(Former ID: TTDS00027)
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| Target Name |
Adrenergic receptor Alpha-1 (ADRA1)
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| Synonyms |
Alpha1-adrenoceptor; Alpha(1)-adrenoceptor
Click to Show/Hide
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 5 Target-related Diseases | + | ||||
| 1 | Headache [ICD-11: 8A80-8A84] | |||||
| 2 | Heart failure [ICD-11: BD10-BD1Z] | |||||
| 3 | Hypertension [ICD-11: BA00-BA04] | |||||
| 4 | Orthostatic hypotension [ICD-11: BA21] | |||||
| 5 | Prostate hyperplasia [ICD-11: GA90] | |||||
| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 6 Approved Drugs | + | ||||
| 1 | Carvedilol | Drug Info | Approved | Congestive heart failure | [2], [3] | |
| 2 | Ergotamine | Drug Info | Approved | Headache | [4], [5] | |
| 3 | Labetalol | Drug Info | Approved | Hypertension | [6], [7] | |
| 4 | Midodrine | Drug Info | Approved | Orthostatic hypotension | [8], [9] | |
| 5 | Prazosin | Drug Info | Approved | Congestive heart failure | [10] | |
| 6 | Urapidil | Drug Info | Approved | Hypertension | [10] | |
| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | Phenylpropanolamine | Drug Info | Withdrawn from market | Obesity | [11] | |
| 2 | Metazosin | Drug Info | Discontinued in Phase 3 | Cardiac disease | [12] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Antagonist | [+] 6 Antagonist drugs | + | ||||
| 1 | Carvedilol | Drug Info | [13] | |||
| 2 | Labetalol | Drug Info | [13] | |||
| 3 | Prazosin | Drug Info | [1], [15] | |||
| 4 | Urapidil | Drug Info | [16] | |||
| 5 | Metazosin | Drug Info | [18] | |||
| 6 | DC-015 | Drug Info | [19] | |||
| Agonist | [+] 3 Agonist drugs | + | ||||
| 1 | Ergotamine | Drug Info | [5] | |||
| 2 | Midodrine | Drug Info | [14] | |||
| 3 | Phenylpropanolamine | Drug Info | [17] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
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| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
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| REF 1 | 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 2 | URL: 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 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | |||||
| REF 4 | URL: 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 | Reversal of ergotamine-induced vasospasm following methylprednisolone. Clin Toxicol (Phila). 2008 Dec;46(10):1074-6. | |||||
| REF 6 | URL: 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 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074787. | |||||
| REF 8 | URL: 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 | Emerging drugs for complications of end-stage liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):159-74. | |||||
| REF 10 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 11 | Pharmacotherapy for obesity. Drugs. 2005;65(10):1391-418. | |||||
| 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 800002056) | |||||
| REF 13 | Beta-blockers in the treatment of hypertension: are there clinically relevant differences Postgrad Med. 2009 May;121(3):90-8. | |||||
| REF 14 | Orthostatic hypotension in patients with Parkinson's disease: pathophysiology and management. Drugs Aging. 2001;18(7):495-505. | |||||
| REF 15 | Characterization of alpha-adrenoceptor subtypes in smooth muscle of equine ileum. Am J Vet Res. 2001 Sep;62(9):1370-4. | |||||
| REF 16 | Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55. | |||||
| REF 17 | 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. | |||||
| REF 18 | Metazosin tablets (Kenosin) in the treatment of chronic congestive heart failure. Cas Lek Cesk. 1995 Sep 20;134(18):590-3. | |||||
| REF 19 | 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. | |||||
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