Target Information

Target General Infomation
Target ID
T53381
Former ID
TTDS00030
Target Name
Alpha-1D adrenergic receptor
Gene Name
ADRA1D
Synonyms
Alpha 1D-adrenoceptor; Alpha 1D-adrenoreceptor; Alpha adrenergic receptor 1a; Alpha-1A adrenergic receptor; ADRA1D
Target Type
Successful
Disease Benign prostatic hyperplasia [ICD9: 600; ICD10: N40]
Congestive heart failure [ICD9: 428; ICD10: I50]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Erectile dysfunction [ICD9: 302.72, 607.84; ICD10: F52.2, N48.4]
Fecal incontinence [ICD10: R15]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Hypertension [ICD9: 401; ICD10: I10-I16]
Heart arrhythmia [ICD10: I47-I49]
Prostate disease [ICD10: N42.9]
Peripheral vascular disease [ICD9: 443.9; ICD10: I73.9]
Prostate hyperplasia [ICD10: N40]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Pediatric cancer [ICD9: 140-229; ICD10: C00-C96]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Unspecified [ICD code not available]
Function
This alpha-adrenergic receptor mediatesits effect through the influx of extracellular calcium.
BioChemical Class
GPCR rhodopsin
Target Validation
T53381
UniProt ID
P25100
Sequence
MTFRDLLSVSFEGPRPDSSAGGSSAGGGGGSAGGAAPSEGPAVGGVPGGAGGGGGVVGAG
SGEDNRSSAGEPGSAGAGGDVNGTAAVGGLVVSAQGVGVGVFLAAFILMAVAGNLLVILS
VACNRHLQTVTNYFIVNLAVADLLLSATVLPFSATMEVLGFWAFGRAFCDVWAAVDVLCC
TASILSLCTISVDRYVGVRHSLKYPAIMTERKAAAILALLWVVALVVSVGPLLGWKEPVP
PDERFCGITEEAGYAVFSSVCSFYLPMAVIVVMYCRVYVVARSTTRSLEAGVKRERGKAS
EVVLRIHCRGAATGADGAHGMRSAKGHTFRSSLSVRLLKFSREKKAAKTLAIVVGVFVLC
WFPFFFVLPLGSLFPQLKPSEGVFKVIFWLGYFNSCVNPLIYPCSSREFKRAFLRLLRCQ
CRRRRRRRPLWRVYGHHWRASTSGLRQDCAPSSGDAPPGAPLALTALPDPDPEPPGTPEM
QAPVASRRKPPSAFREWRLLGPFRRPTTQLRAKVSSLSHKIRAGGAQRAEAACAQRSEVE
AVSLGVPHEVAEGATCQAYELADYSNLRETDI
Drugs and Mode of Action
Drug(s) Alfuzosin Drug Info Approved Benign prostatic hyperplasia [536610], [542116]
Armodafinil Drug Info Approved Pediatric cancer [551871]
Bunazosin Drug Info Approved Glaucoma [551871]
Doxazosin Drug Info Approved Hypertension [536610], [542180]
Moxisylyte Drug Info Approved Erectile dysfunction [551871]
Phenylephrine hydrochloride gel Drug Info Approved Fecal incontinence [547809]
Terazosin Drug Info Approved Benign prostatic hyperplasia [538289], [542324]
Trimazosin Drug Info Approved Congestive heart failure [551871]
MEDETOMIDINE Drug Info Phase 2 Pain [529347]
DL-017 Drug Info Phase 1 Hypertension [526190]
INDORAMIN Drug Info Withdrawn from market Hypertension [468125], [551871]
Sunepitron Drug Info Discontinued in Phase 3 Discovery agent [545699]
TIOSPIRONE Drug Info Discontinued in Phase 3 Discovery agent [538617], [544679]
Dabuzalgron Drug Info Discontinued in Phase 2 Urinary incontinence [540407], [547205]
Deriglidole Drug Info Discontinued in Phase 2 Diabetes [544511]
FCE-22716 Drug Info Discontinued in Phase 2 Hypertension [533340]
FIDUXOSIN HYDROCHLORIDE Drug Info Discontinued in Phase 2 Prostate disease [547070]
GYKI-16084 Drug Info Discontinued in Phase 2 Prostate disease [546866]
JTH-601 Drug Info Discontinued in Phase 2 Prostate disease [546856]
MAZAPERTINE Drug Info Discontinued in Phase 2 Discovery agent [545274]
NS-49 Drug Info Discontinued in Phase 2 Urinary incontinence [468041], [545984]
OPC-28326 Drug Info Discontinued in Phase 2 Peripheral vascular disease [546957]
REC-15-2739 Drug Info Discontinued in Phase 2 Prostate disease [545508]
SL-25.1039 Drug Info Discontinued in Phase 2 Urinary incontinence [547287]
SL-89.0591 Drug Info Discontinued in Phase 2 Prostate disease [545536]
SOU-001 Drug Info Discontinued in Phase 2 Urinary incontinence [547251]
SUN-9221 Drug Info Discontinued in Phase 1 Hypertension [546178]
ABANOQUIL Drug Info Terminated Discovery agent [544556]
AGN-193080 Drug Info Terminated Discovery agent [546437]
BMY-7378 Drug Info Terminated Discovery agent [543289], [544847]
CR-2991 Drug Info Terminated Hypertension [547727]
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]
SL-91.0893 Drug Info Terminated Prostate hyperplasia [546240]
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]
1',2',3',6'-Tetrahydro-[2,4']bipyridinyl Drug Info [533509]
1-(2-Chloro-phenyl)-piperazine Drug Info [528039]
1-(2-Methoxy-phenyl)-piperazine Drug Info [528039]
1-(3-Fluoro-pyridin-2-yl)-4-methyl-piperazine Drug Info [533509]
1-(pyridin-2-yl)piperazine Drug Info [533509]
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-chlorobenzyl)-2-allylphthalazin-1(2H)-one Drug Info [528062]
4-(4-chlorobenzyl)-2-methylphthalazin-1(2H)-one Drug Info [528062]
4-(4-chlorobenzyl)phthalazin-1(2H)-one Drug Info [528062]
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-benzyl-2-methylphthalazin-1(2H)-one Drug Info [528062]
4-Morpholin-2-yl-benzene-1,2-diol Drug Info [526729]
5-Bromo-8-piperazin-1-yl-imidazo[1,2-a]pyrazine Drug Info [526778]
6-hydroxy-3-(3',5'-dihydroxyphenyl)coumarin Drug Info [527848]
8-Piperazin-1-yl-imidazo[1,2-a]pyrazine Drug Info [526778]
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]
INDORAMIN Drug Info [533682]
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-38063 Drug Info [525785]
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]
Agonist 4-Methoxyamphetamine Drug Info [551380]
Armodafinil Drug Info [544068], [550911]
Dabuzalgron Drug Info [540407]
SL-25.1039 Drug Info [550220]
Antagonist Alfuzosin Drug Info [535396]
CR-2991 Drug Info [550128]
Doxazosin Drug Info [536929]
FIDUXOSIN HYDROCHLORIDE Drug Info [526250]
GYKI-16084 Drug Info [528199]
JTH-601 Drug Info [525752]
OPC-28326 Drug Info [525613]
Terazosin Drug Info [535079], [535647]
Modulator Bunazosin Drug Info [527544], [551871]
Deriglidole Drug Info [534576]
DL-017 Drug Info [526190]
FCE-22716 Drug Info [533340]
Moxisylyte Drug Info [534246], [551871]
NS-49 Drug Info [525556]
Phenylephrine hydrochloride gel Drug Info [527269]
REC-15-2739 Drug Info [534138]
SL-89.0591 Drug Info [525538]
SL-91.0893 Drug Info [551953]
SOU-001 Drug Info [527154]
SUN-9221 Drug Info [525435]
Trimazosin Drug Info [533525], [551871]
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
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
Gastrin-CREB signalling pathway via PKC and MAPK
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 468041(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: 481).
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 468125(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: 501).
Ref 526190Antihypertensive action and blockade of alpha1-adrenoceptors by DL-017, a quinazoline derivative. J Cardiovasc Pharmacol. 2001 Dec;38(6):893-9.
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 533340Mechanism of the antihypertensive effect of FCE 22716, a new ergoline derivative, in the spontaneously hypertensive rat. Pharmacology. 1989;38(2):78-92.
Ref 536610Alpha blockers for the treatment of benign prostatic hyperplasia. Rev Urol. 2007 Fall;9(4):181-90.
Ref 538289FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074823.
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 540407(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: 3469).
Ref 542116(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: 7109).
Ref 542180(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: 7170).
Ref 542324(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: 7302).
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 544511Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000010)
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 545508Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003537)
Ref 545536Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003628)
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 545984Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005693)
Ref 546178Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006767)
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 546240Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007056)
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 546856Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010685)
Ref 546866Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010746)
Ref 546957Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011559)
Ref 547070Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012814)
Ref 547205Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013967)
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)
Ref 547287Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014859)
Ref 547727Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018844)
Ref 547809Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019494)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525435Synthesis and pharmacological evaluation of pyrroloazepine derivatives as potent antihypertensive agents with antiplatelet aggregation activity. Chem Pharm Bull (Tokyo). 1999 Feb;47(2):246-56.
Ref 525538Effects of alpha1-adrenoceptor antagonists on agonist and tilt-induced changes in blood pressure: relationships to uroselectivity. Eur J Pharmacol. 1999 May 28;373(1):51-62.
Ref 525556Pharmacokinetics of NS-49, a phenethylamine class alpha 1A-adrenoceptor agonist. 3rd communication: metabolism in rats, rabbits, dogs and monkeys, and effects on hepatic drug-metabolizing enzyme activities in rats after repeated administration. Arzneimittelforschung. 1999 Jul;49(7):612-7.
Ref 525613Mechanisms of action of OPC-28326, a selective hindlimb vasodilator. J Pharmacol Exp Ther. 1999 Nov;291(2):604-11.
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.
Ref 525752Effect of JTH-601, a novel alpha(1)-adrenoceptor antagonist, on prostate function in dogs. Eur J Pharmacol. 2000 Apr 7;394(1):123-30.
Ref 525785Bioorg Med Chem Lett. 2000 May 15;10(10):1093-6.Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists.
Ref 526190Antihypertensive action and blockade of alpha1-adrenoceptors by DL-017, a quinazoline derivative. J Cardiovasc Pharmacol. 2001 Dec;38(6):893-9.
Ref 526250Effect of fiduxosin, an antagonist selective for alpha(1A)- and alpha(1D)-adrenoceptors, on intraurethral and arterial pressure responses in conscious dogs. J Pharmacol Exp Ther. 2002 Feb;300(2):487-94.
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 526778J Med Chem. 1992 Oct 16;35(21):3845-57.Synthesis and hypoglycemic activity of substituted 8-(1-piperazinyl)imidazo[1,2-a]pyrazines.
Ref 527154Drug repositioning: identifying and developing new uses for existing drugs. Nat Rev Drug Discov. 2004 Aug;3(8):673-83.
Ref 527269Effects of topically instilled bunazosin, an alpha1-adrenoceptor antagonist, on constrictions induced by phenylephrine and ET-1 in rabbit retinal arteries. Invest Ophthalmol Vis Sci. 2004 Nov;45(11):4041-8.
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 527544Bunazosin, a selective alpha1-adrenoceptor antagonist, as an anti-glaucoma drug: effects on ocular circulation and retinal neuronal damage. Cardiovasc Drug Rev. 2005 Spring;23(1):43-56.
Ref 527848Bioorg Med Chem Lett. 2006 Jan 15;16(2):257-61. Epub 2005 Nov 3.Design, synthesis, and vasorelaxant and platelet antiaggregatory activities of coumarin-resveratrol hybrids.
Ref 528039J Med Chem. 1991 Jun;34(6):1850-4.Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands.
Ref 528062Bioorg Med Chem Lett. 2006 May 15;16(10):2786-90. Epub 2006 Mar 2.Vasorelaxant activity of phthalazinones and related compounds.
Ref 528199A novel approach to the treatment of benign prostatic hyperplasia. BJU Int. 2006 Jun;97(6):1252-5.
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 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 533340Mechanism of the antihypertensive effect of FCE 22716, a new ergoline derivative, in the spontaneously hypertensive rat. Pharmacology. 1989;38(2):78-92.
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 533509J Med Chem. 1984 Sep;27(9):1182-5.Adrenoceptor and tetrabenazine antagonism activities of some pyridinyltetrahydropyridines.
Ref 533525The hypotensive effect of trimazosin is not caused solely by alpha 1-adrenoceptor blockade. J Cardiovasc Pharmacol. 1984 Jan-Feb;6(1):142-50.
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 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 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 534138Functional antagonistic activity of Rec 15/2739, a novel alpha-1 antagonist selective for the lower urinary tract, on noradrenaline-induced contraction of human prostate and mesenteric artery. J Pharmacol Exp Ther. 1996 Jun;277(3):1237-46.
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 534246Pharmacokinetics of moxisylyte in healthy volunteers after intracavernous injection of increasing doses. Eur J Clin Pharmacol. 1996;49(5):411-5.
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 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 534576Mechanisms of the hypoglycemic effects of the alpha2-adrenoceptor antagonists SL84.0418 and deriglidole. Life Sci. 1998;62(9):839-52.
Ref 535079Overexpression of the alpha1B-adrenergic receptor causes apoptotic neurodegeneration: multiple system atrophy. Nat Med. 2000 Dec;6(12):1388-94.
Ref 535396Alfuzosin: a review of the therapeutic use of the prolonged-release formulation given once daily in the management of benign prostatic hyperplasia. Drugs. 2002;62(4):633-53.
Ref 535647Induction of prostate apoptosis by alpha1-adrenoceptor antagonists: mechanistic significance of the quinazoline component. Prostate Cancer Prostatic Dis. 2002;5(2):88-95.
Ref 536929The role of combination medical therapy in benign prostatic hyperplasia. Int J Impot Res. 2008 Dec;20 Suppl 3:S33-43.
Ref 540407(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: 3469).
Ref 544068Mechanisms of modafinil: A review of current research. Neuropsychiatr Dis Treat. 2007 June; 3(3): 349-364.
Ref 550128WO patent application no. 2006,1244,90, Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia.
Ref 550220Pharmaceutical co analysis sanofi aventis, 2006, Page(216).
Ref 550911US patent application no. 2014,0349,964, Methods for inducing orexin neurons and agent for treating narcolepsy or eating disorder.
Ref 551280Analogs of UK 14,304: Structural features responsible for alpha2 adrenoceptor activity, Bioorg. Med. Chem. Lett. 5(15):1745-1750 (1995).
Ref 551380Differential behavioural and neurochemical effects of para-methoxyamphetamine and 3,4-methylenedioxymethamphetamine in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2000 Aug;24(6):955-77.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 551953Tissue Selectivity of in vivo alpha1-Adrenoceptor Biding of KMD-3213 in Rats. Eur Urol 1999;36(suppl 1):113-117.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Tang and Dr. Zhang.