Target Information
Target General Infomation | |||||
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Target ID |
T29500
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Former ID |
TTDS00029
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Target Name |
Alpha-1B adrenergic receptor
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Gene Name |
ADRA1B
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Synonyms |
Alpha 1B-adrenoceptor; Alpha 1B-adrenoreceptor; ADRA1B
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Target Type |
Successful
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Disease | Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90] | ||||
Exogenous obesity [ICD10: E66] | |||||
Hypertension [ICD9: 401; ICD10: I10-I16] | |||||
Heart arrhythmia [ICD10: I47-I49] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Psychiatric disorder [ICD9: 290-319; ICD10: F01-F99] | |||||
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32] | |||||
Unspecified [ICD code not available] | |||||
Function |
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine (PE)-stimulated ERK signaling in cardiac myocytes.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T29500
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UniProt ID | |||||
Sequence |
MNPDLDTGHNTSAPAHWGELKNANFTGPNQTSSNSTLPQLDITRAISVGLVLGAFILFAI
VGNILVILSVACNRHLRTPTNYFIVNLAMADLLLSFTVLPFSAALEVLGYWVLGRIFCDI WAAVDVLCCTASILSLCAISIDRYIGVRYSLQYPTLVTRRKAILALLSVWVLSTVISIGP LLGWKEPAPNDDKECGVTEEPFYALFSSLGSFYIPLAVILVMYCRVYIVAKRTTKNLEAG VMKEMSNSKELTLRIHSKNFHEDTLSSTKAKGHNPRSSIAVKLFKFSREKKAAKTLGIVV GMFILCWLPFFIALPLGSLFSTLKPPDAVFKVVFWLGYFNSCLNPIIYPCSSKEFKRAFV RILGCQCRGRGRRRRRRRRRLGGCAYTYRPWTRGGSLERSQSRKDSLDDSGSCLSGSQRT LPSASPSPGYLGRGAPPPVELCAFPEWKAPGALLSLPAPEPPGRRGRHDSGPLFTFKLLT EPESPGTDGGASNGGCEAAADVANGQPGFKSNMPLAPGQF |
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Drugs and Mode of Action | |||||
Drug(s) | Methamphetamine | Drug Info | Approved | Attention deficit hyperactivity disorder | [468034], [538186] |
Methoxamine | Drug Info | Approved | Hypertension | [468062], [550776] | |
Phendimetrazine | Drug Info | Approved | Exogenous obesity | [551871] | |
Propericiazine | Drug Info | Approved | Psychiatric disorder | [533807], [537783], [551439] | |
MEDETOMIDINE | Drug Info | Phase 2 | Pain | [529347] | |
Sunepitron | Drug Info | Discontinued in Phase 3 | Discovery agent | [545699] | |
TIOSPIRONE | Drug Info | Discontinued in Phase 3 | Discovery agent | [538617], [544679] | |
MAZAPERTINE | Drug Info | Discontinued in Phase 2 | Discovery agent | [545274] | |
SOU-001 | Drug Info | Discontinued in Phase 2 | Urinary incontinence | [547251] | |
ABANOQUIL | Drug Info | Terminated | Discovery agent | [544556] | |
AGN-193080 | Drug Info | Terminated | Discovery agent | [546437] | |
BMY-7378 | Drug Info | Terminated | Discovery agent | [543289], [544847] | |
NIGULDIPINE | Drug Info | Terminated | Discovery agent | [468083], [545183] | |
Siramesine | Drug Info | Terminated | Discovery agent | [545008] | |
SK&F-104078 | Drug Info | Terminated | Discovery agent | [544626] | |
SK&F-104856 | Drug Info | Terminated | Discovery agent | [544924] | |
SNAP-5089 | Drug Info | Terminated | Heart arrhythmia | [468115], [546179] | |
WB-4101 | Drug Info | Terminated | Discovery agent | [468117], [545656] | |
Sunepitron | Drug Info | Investigative | Unspecified | [528210] | |
Inhibitor | (+/-)-nantenine | Drug Info | [530558] | ||
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine | Drug Info | [534315] | |||
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine | Drug Info | [534315] | |||
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [526618] | |||
4-((E)-1-Naphthalen-1-yl-propenyl)-1H-imidazole | Drug Info | [534160] | |||
4-((Z)-1-Naphthalen-1-yl-propenyl)-1H-imidazole | Drug Info | [534160] | |||
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole | Drug Info | [533805] | |||
4-(1-Naphthalen-1-yl-propyl)-1H-imidazole | Drug Info | [534160] | |||
4-(1-Naphthalen-1-yl-vinyl)-1H-imidazole | Drug Info | [534160] | |||
4-(2,3-Dihydro-1H-phenalen-1-yl)-1H-imidazole | Drug Info | [534160] | |||
4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline | Drug Info | [526618] | |||
4-(3-Hydroxy-piperidin-3-yl)-benzene-1,2-diol | Drug Info | [526729] | |||
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [531079] | |||
4-(4-Isopropyl-morpholin-2-yl)-benzene-1,2-diol | Drug Info | [526729] | |||
4-(4-Methyl-indan-1-yl)-1H-imidazole | Drug Info | [534467] | |||
4-Benzo[b]thiophen-4-yl-1H-imidazole | Drug Info | [525720] | |||
4-Morpholin-2-yl-benzene-1,2-diol | Drug Info | [526729] | |||
6-fluoronorepinehprine | Drug Info | [530478] | |||
A-119637 | Drug Info | [526051] | |||
A-123189 | Drug Info | [526051] | |||
ABANOQUIL | Drug Info | [533682] | |||
AGN-192172 | Drug Info | [551280] | |||
AGN-193080 | Drug Info | [551280] | |||
BMY-7378 | Drug Info | [527512] | |||
CORYNANTHEINE | Drug Info | [533638] | |||
FLUANISONE | Drug Info | [533378] | |||
Imidazolidin-2-ylidene-o-tolyl-amine | Drug Info | [551280] | |||
Imidazolidin-2-ylidene-quinoxalin-6-yl-amine | Drug Info | [551280] | |||
ISOCLOZAPINE | Drug Info | [534532] | |||
LEVONORDEFRIN | Drug Info | [534160] | |||
MAZAPERTINE | Drug Info | [533800] | |||
MEDETOMIDINE | Drug Info | [533805] | |||
N-(5-Bromo-quinoxalin-6-yl)-guanidine | Drug Info | [551280] | |||
NIGULDIPINE | Drug Info | [533638] | |||
OCTOCLOTHEPIN | Drug Info | [531171] | |||
RWJ-68157 | Drug Info | [525785] | |||
RWJ-69736 | Drug Info | [525785] | |||
RX-821002 | Drug Info | [533375] | |||
Siramesine | Drug Info | [533739] | |||
SK&F-104078 | Drug Info | [533638] | |||
SK&F-104856 | Drug Info | [533638] | |||
SK&F-105854 | Drug Info | [533638] | |||
SK&F-106686 | Drug Info | [533638] | |||
SK&F-86466 | Drug Info | [533638] | |||
SNAP-5089 | Drug Info | [533638] | |||
SNAP-8719 | Drug Info | [527512] | |||
Sunepitron | Drug Info | [528210] | |||
TIOSPIRONE | Drug Info | [534093] | |||
UH-301 | Drug Info | [534363] | |||
WB-4101 | Drug Info | [533682] | |||
Antagonist | 5-methylurapidil | Drug Info | [526102] | ||
AH 11110 | Drug Info | [534189] | |||
Cyclazosin | Drug Info | [536955] | |||
Methamphetamine | Drug Info | [536897] | |||
Phendimetrazine | Drug Info | [536284] | |||
Rec 15/2615 | Drug Info | [534403] | |||
spiroxatrine | Drug Info | [526102] | |||
[125I]BE-2254 | Drug Info | [533751] | |||
Stimulator | Methoxamine | Drug Info | [537237] | ||
Binder | Propericiazine | Drug Info | [537783] | ||
Modulator | SOU-001 | Drug Info | [527154] | ||
Agonist | [125I]HEAT | Drug Info | [533679] | ||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
cGMP-PKG signaling pathway | |||||
Neuroactive ligand-receptor interaction | |||||
Adrenergic signaling in cardiomyocytes | |||||
Vascular smooth muscle contraction | |||||
Salivary secretion | |||||
NetPath Pathway | IL2 Signaling Pathway | ||||
PANTHER Pathway | Alpha adrenergic receptor signaling pathway | ||||
Pathway Interaction Database | LPA receptor mediated events | ||||
Reactome | Adrenoceptors | ||||
G alpha (q) signalling events | |||||
G alpha (12/13) signalling events | |||||
WikiPathways | Monoamine GPCRs | ||||
Calcium Regulation in the Cardiac Cell | |||||
GPCRs, Class A Rhodopsin-like | |||||
Vitamin D Receptor Pathway | |||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
AMPK Signaling | |||||
References | |||||
Ref 468034 | (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: 4803). | ||||
Ref 468062 | (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: 483). | ||||
Ref 468083 | (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: 487). | ||||
Ref 468115 | (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: 498). | ||||
Ref 468117 | (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: 499). | ||||
Ref 528210 | J Med Chem. 2006 Jun 1;49(11):3116-35.An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. | ||||
Ref 529347 | Sedative and cardiopulmonary effects of medetomidine hydrochloride and xylazine hydrochloride and their reversal with atipamezole hydrochloride in calves. Am J Vet Res. 2008 Mar;69(3):319-29. | ||||
Ref 533807 | Affinity of neuroleptics for D1 receptor of human brain striatum. J Psychiatry Neurosci. 1994 Jul;19(4):265-9. | ||||
Ref 537783 | Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action. Biol Psychiatry. 1984 Sep;19(9):1283-91. | ||||
Ref 538186 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040529. | ||||
Ref 538617 | (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: 101). | ||||
Ref 543289 | (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: 9). | ||||
Ref 544556 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000128) | ||||
Ref 544626 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000354) | ||||
Ref 544679 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000562) | ||||
Ref 544847 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001317) | ||||
Ref 544924 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001560) | ||||
Ref 545008 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001859) | ||||
Ref 545183 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002398) | ||||
Ref 545274 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002662) | ||||
Ref 545656 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004048) | ||||
Ref 545699 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004255) | ||||
Ref 546179 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006771) | ||||
Ref 546437 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008130) | ||||
Ref 525720 | J Med Chem. 2000 Mar 9;43(5):765-8.alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene [corrected] as a high-affinity ligand for the alpha(2D) adrenergic receptor. | ||||
Ref 525785 | Bioorg Med Chem Lett. 2000 May 15;10(10):1093-6.Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists. | ||||
Ref 526051 | Bioorg Med Chem Lett. 2001 May 7;11(9):1119-21.Two novel and potent 3-[(o-methoxyphenyl)piperazinylethyl]-5-phenylthien. | ||||
Ref 526102 | Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes. Jpn J Pharmacol. 2001 Jun;86(2):189-95. | ||||
Ref 526618 | Bioorg Med Chem Lett. 2003 May 19;13(10):1759-62.4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists. | ||||
Ref 526729 | J Med Chem. 1992 Mar 20;35(6):1009-18.Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic receptors. | ||||
Ref 527154 | Drug repositioning: identifying and developing new uses for existing drugs. Nat Rev Drug Discov. 2004 Aug;3(8):673-83. | ||||
Ref 527512 | J Med Chem. 2005 Apr 21;48(8):3076-9.Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists. | ||||
Ref 528210 | J Med Chem. 2006 Jun 1;49(11):3116-35.An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. | ||||
Ref 530478 | Bioorg Med Chem. 2009 Dec 1;17(23):7987-92. Epub 2009 Oct 13.Structural basis of the selectivity of the beta(2)-adrenergic receptor for fluorinated catecholamines. | ||||
Ref 530558 | Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. | ||||
Ref 531079 | J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. | ||||
Ref 531171 | J Med Chem. 2010 Oct 14;53(19):7021-34.Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for |A(1)-adrenoceptors. | ||||
Ref 533375 | J Med Chem. 1986 Oct;29(10):2000-3.Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists. | ||||
Ref 533378 | J Med Chem. 1987 Nov;30(11):2099-104.2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1. | ||||
Ref 533638 | J Med Chem. 1995 Sep 15;38(19):3681-716.Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. | ||||
Ref 533679 | KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues. Mol Pharmacol. 1995 Aug;48(2):250-8. | ||||
Ref 533682 | J Med Chem. 1995 Sep 1;38(18):3415-44.Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. | ||||
Ref 533739 | J Med Chem. 1995 May 26;38(11):1998-2008.Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. | ||||
Ref 533751 | Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues. J Pharmacol Exp Ther. 1995 Jan;272(1):134-42. | ||||
Ref 533800 | J Med Chem. 1994 Apr 15;37(8):1060-2.A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects. | ||||
Ref 533805 | J Med Chem. 1994 Jul 22;37(15):2328-33.A structure-activity relationship study of benzylic modifications of 4-[1-(1-naphthyl)ethyl]-1H-imidazoles on alpha 1- and alpha 2-adrenergic receptors. | ||||
Ref 534093 | J Med Chem. 1996 Jan 5;39(1):143-8.3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents. | ||||
Ref 534160 | J Med Chem. 1996 Jul 19;39(15):3001-13.Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine. | ||||
Ref 534189 | Structure activity relationships of a series of buspirone analogs at alpha-1 adrenoceptors: further evidence that rat aorta alpha-1 adrenoceptors are of the alpha-1D-subtype. J Pharmacol Exp Ther. 1996 Jul;278(1):136-44. | ||||
Ref 534315 | J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists. | ||||
Ref 534363 | J Med Chem. 1997 Apr 11;40(8):1252-7.N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor. | ||||
Ref 534403 | Pharmacological characterization of the uroselective alpha-1 antagonist Rec 15/2739 (SB 216469): role of the alpha-1L adrenoceptor in tissue selectivity, part II. J Pharmacol Exp Ther. 1997 Jun;281(3):1284-93. | ||||
Ref 534467 | J Med Chem. 1997 Sep 12;40(19):3014-24.Medetomidine analogs as alpha 2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with alpha 2-adrenoceptors involving a "methyl pocket". | ||||
Ref 534532 | J Med Chem. 1997 Dec 5;40(25):4146-53.Synthesis and pharmacological evaluation of triflate-substituted analogues of clozapine: identification of a novel atypical neuroleptic. | ||||
Ref 536284 | Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. | ||||
Ref 536897 | Mirtazapine treatment after conditioning with methamphetamine alters subsequent expression of place preference. Drug Alcohol Depend. 2009 Jan 1;99(1-3):231-9. Epub 2008 Oct 21. | ||||
Ref 536955 | Identification of alpha1-adrenoceptor subtypes involved in contraction of young CD rat epididymal vas deferens. Eur J Pharmacol. 2009 Jan 14;602(2-3):388-94. Epub 2008 Nov 14. | ||||
Ref 537237 | Activation of alpha1-adrenoceptors Inhibits Growth Hormone Secretion in Humans. Exp Clin Endocrinol Diabetes. 2009 Apr 16. |
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