Target Information

Target General Infomation
Target ID
T29500
Former ID
TTDS00029
Target Name
Alpha-1B adrenergic receptor
Gene Name
ADRA1B
Synonyms
Alpha 1B-adrenoceptor; Alpha 1B-adrenoreceptor; ADRA1B
Target Type
Successful
Disease Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90]
Exogenous obesity [ICD10: E66]
Heart arrhythmia [ICD10: I47-I49]
Hypertension [ICD9: 401; ICD10: I10-I16]
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T29500
UniProt ID
P35368
Sequence
MNPDLDTGHNTSAPAHWGELKNANFTGPNQTSSNSTLPQLDITRAISVGLVLGAFILFAI
VGNILVILSVACNRHLRTPTNYFIVNLAMADLLLSFTVLPFSAALEVLGYWVLGRIFCDI
WAAVDVLCCTASILSLCAISIDRYIGVRYSLQYPTLVTRRKAILALLSVWVLSTVISIGP
LLGWKEPAPNDDKECGVTEEPFYALFSSLGSFYIPLAVILVMYCRVYIVAKRTTKNLEAG
VMKEMSNSKELTLRIHSKNFHEDTLSSTKAKGHNPRSSIAVKLFKFSREKKAAKTLGIVV
GMFILCWLPFFIALPLGSLFSTLKPPDAVFKVVFWLGYFNSCLNPIIYPCSSKEFKRAFV
RILGCQCRGRGRRRRRRRRRLGGCAYTYRPWTRGGSLERSQSRKDSLDDSGSCLSGSQRT
LPSASPSPGYLGRGAPPPVELCAFPEWKAPGALLSLPAPEPPGRRGRHDSGPLFTFKLLT
EPESPGTDGGASNGGCEAAADVANGQPGFKSNMPLAPGQF
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 528210J 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 529347Sedative 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 533807Affinity of neuroleptics for D1 receptor of human brain striatum. J Psychiatry Neurosci. 1994 Jul;19(4):265-9.
Ref 537783Interaction 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 538186FDA 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 544556Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000128)
Ref 544626Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000354)
Ref 544679Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000562)
Ref 544847Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001317)
Ref 544924Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001560)
Ref 545008Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001859)
Ref 545183Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002398)
Ref 545274Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002662)
Ref 545656Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004048)
Ref 545699Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004255)
Ref 546179Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006771)
Ref 546437Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008130)
Ref 547251Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014478)
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Ref 525720J 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.
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Ref 526102Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes. Jpn J Pharmacol. 2001 Jun;86(2):189-95.
Ref 526618Bioorg 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 526729J 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 527154Drug repositioning: identifying and developing new uses for existing drugs. Nat Rev Drug Discov. 2004 Aug;3(8):673-83.
Ref 527512J 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 528210J 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 530478Bioorg 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 530558Bioorg 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 531079J 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 531171J 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 533375J Med Chem. 1986 Oct;29(10):2000-3.Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists.
Ref 533378J Med Chem. 1987 Nov;30(11):2099-104.2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.
Ref 533638J 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 533679KMD-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 533682J 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 533739J 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 533751Cloning 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 533800J 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 533805J 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 534093J Med Chem. 1996 Jan 5;39(1):143-8.3-Benzisothiazolylpiperazine derivatives as potential atypical antipsychotic agents.
Ref 534160J 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 534189Structure 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 534315J Med Chem. 1997 Jan 3;40(1):18-23.Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.
Ref 534363J 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 534403Pharmacological 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 534467J 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 534532J 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 536284Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34.
Ref 536897Mirtazapine 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 536955Identification 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 537237Activation of alpha1-adrenoceptors Inhibits Growth Hormone Secretion in Humans. Exp Clin Endocrinol Diabetes. 2009 Apr 16.
Ref 537783Interaction 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 551280Analogs of UK 14,304: Structural features responsible for alpha2 adrenoceptor activity, Bioorg. Med. Chem. Lett. 5(15):1745-1750 (1995).

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