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]
Heart arrhythmia [ICD10: I47-I49]
Hypertension [ICD9: 401; ICD10: I10-I16]
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]
Prostate disease [ICD10: N42.9]
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 [1], [2]
Armodafinil Drug Info Approved Pediatric cancer [3]
Bunazosin Drug Info Approved Glaucoma [3]
Doxazosin Drug Info Approved Hypertension [1], [4]
Moxisylyte Drug Info Approved Erectile dysfunction [3]
Phenylephrine hydrochloride gel Drug Info Approved Fecal incontinence [5]
Terazosin Drug Info Approved Benign prostatic hyperplasia [6], [7]
Trimazosin Drug Info Approved Congestive heart failure [3]
MEDETOMIDINE Drug Info Phase 2 Pain [8]
DL-017 Drug Info Phase 1 Hypertension [9]
INDORAMIN Drug Info Withdrawn from market Hypertension [10], [3]
Sunepitron Drug Info Discontinued in Phase 3 Discovery agent [11]
TIOSPIRONE Drug Info Discontinued in Phase 3 Discovery agent [12], [13]
Dabuzalgron Drug Info Discontinued in Phase 2 Urinary incontinence [14], [15]
Deriglidole Drug Info Discontinued in Phase 2 Diabetes [16]
FCE-22716 Drug Info Discontinued in Phase 2 Hypertension [17]
FIDUXOSIN HYDROCHLORIDE Drug Info Discontinued in Phase 2 Prostate disease [18]
GYKI-16084 Drug Info Discontinued in Phase 2 Prostate disease [19]
JTH-601 Drug Info Discontinued in Phase 2 Prostate disease [20]
MAZAPERTINE Drug Info Discontinued in Phase 2 Discovery agent [21]
NS-49 Drug Info Discontinued in Phase 2 Urinary incontinence [22], [23]
OPC-28326 Drug Info Discontinued in Phase 2 Peripheral vascular disease [24]
REC-15-2739 Drug Info Discontinued in Phase 2 Prostate disease [25]
SL-25.1039 Drug Info Discontinued in Phase 2 Urinary incontinence [26]
SL-89.0591 Drug Info Discontinued in Phase 2 Prostate disease [27]
SOU-001 Drug Info Discontinued in Phase 2 Urinary incontinence [28]
SUN-9221 Drug Info Discontinued in Phase 1 Hypertension [29]
ABANOQUIL Drug Info Terminated Discovery agent [30]
AGN-193080 Drug Info Terminated Discovery agent [31]
BMY-7378 Drug Info Terminated Discovery agent [32], [33]
CR-2991 Drug Info Terminated Hypertension [34]
NIGULDIPINE Drug Info Terminated Discovery agent [35], [36]
Siramesine Drug Info Terminated Discovery agent [37]
SK&F-104078 Drug Info Terminated Discovery agent [38]
SK&F-104856 Drug Info Terminated Discovery agent [39]
SL-91.0893 Drug Info Terminated Prostate hyperplasia [40]
SNAP-5089 Drug Info Terminated Heart arrhythmia [41], [42]
WB-4101 Drug Info Terminated Discovery agent [43], [44]
Sunepitron Drug Info Investigative Unspecified [45]
Inhibitor (+/-)-nantenine Drug Info [46]
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine Drug Info [47]
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine Drug Info [47]
1',2',3',6'-Tetrahydro-[2,4']bipyridinyl Drug Info [48]
1-(2-Chloro-phenyl)-piperazine Drug Info [49]
1-(2-Methoxy-phenyl)-piperazine Drug Info [49]
1-(3-Fluoro-pyridin-2-yl)-4-methyl-piperazine Drug Info [48]
1-(pyridin-2-yl)piperazine Drug Info [48]
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline Drug Info [50]
4-((E)-1-Naphthalen-1-yl-propenyl)-1H-imidazole Drug Info [51]
4-((Z)-1-Naphthalen-1-yl-propenyl)-1H-imidazole Drug Info [51]
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole Drug Info [52]
4-(1-Naphthalen-1-yl-propyl)-1H-imidazole Drug Info [51]
4-(1-Naphthalen-1-yl-vinyl)-1H-imidazole Drug Info [51]
4-(2,3-Dihydro-1H-phenalen-1-yl)-1H-imidazole Drug Info [51]
4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline Drug Info [50]
4-(3-Hydroxy-piperidin-3-yl)-benzene-1,2-diol Drug Info [53]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [54]
4-(4-chlorobenzyl)-2-allylphthalazin-1(2H)-one Drug Info [55]
4-(4-chlorobenzyl)-2-methylphthalazin-1(2H)-one Drug Info [55]
4-(4-chlorobenzyl)phthalazin-1(2H)-one Drug Info [55]
4-(4-Isopropyl-morpholin-2-yl)-benzene-1,2-diol Drug Info [53]
4-(4-Methyl-indan-1-yl)-1H-imidazole Drug Info [56]
4-Benzo[b]thiophen-4-yl-1H-imidazole Drug Info [57]
4-benzyl-2-methylphthalazin-1(2H)-one Drug Info [55]
4-Morpholin-2-yl-benzene-1,2-diol Drug Info [53]
5-Bromo-8-piperazin-1-yl-imidazo[1,2-a]pyrazine Drug Info [58]
6-hydroxy-3-(3',5'-dihydroxyphenyl)coumarin Drug Info [59]
8-Piperazin-1-yl-imidazo[1,2-a]pyrazine Drug Info [58]
ABANOQUIL Drug Info [60]
AGN-192172 Drug Info [61]
AGN-193080 Drug Info [61]
BMY-7378 Drug Info [62]
CORYNANTHEINE Drug Info [63]
FLUANISONE Drug Info [64]
Imidazolidin-2-ylidene-o-tolyl-amine Drug Info [61]
Imidazolidin-2-ylidene-quinoxalin-6-yl-amine Drug Info [61]
INDORAMIN Drug Info [60]
ISOCLOZAPINE Drug Info [65]
LEVONORDEFRIN Drug Info [51]
MAZAPERTINE Drug Info [66]
MEDETOMIDINE Drug Info [52]
N-(5-Bromo-quinoxalin-6-yl)-guanidine Drug Info [61]
NIGULDIPINE Drug Info [63]
OCTOCLOTHEPIN Drug Info [67]
RWJ-38063 Drug Info [68]
RWJ-68157 Drug Info [68]
RWJ-69736 Drug Info [68]
RX-821002 Drug Info [69]
Siramesine Drug Info [70]
SK&F-104078 Drug Info [63]
SK&F-104856 Drug Info [63]
SK&F-105854 Drug Info [63]
SK&F-106686 Drug Info [63]
SK&F-86466 Drug Info [63]
SNAP-5089 Drug Info [63]
SNAP-8719 Drug Info [62]
Sunepitron Drug Info [45]
TIOSPIRONE Drug Info [71]
UH-301 Drug Info [72]
WB-4101 Drug Info [60]
Agonist 4-Methoxyamphetamine Drug Info [73]
Armodafinil Drug Info [74], [75]
Dabuzalgron Drug Info [14]
SL-25.1039 Drug Info [76]
Antagonist Alfuzosin Drug Info [77]
CR-2991 Drug Info [78]
Doxazosin Drug Info [79]
FIDUXOSIN HYDROCHLORIDE Drug Info [80]
GYKI-16084 Drug Info [81]
JTH-601 Drug Info [82]
OPC-28326 Drug Info [83]
Terazosin Drug Info [84], [85]
Modulator Bunazosin Drug Info [86], [3]
Deriglidole Drug Info [87]
DL-017 Drug Info [9]
FCE-22716 Drug Info [17]
Moxisylyte Drug Info [88], [3]
NS-49 Drug Info [89]
Phenylephrine hydrochloride gel Drug Info [90]
REC-15-2739 Drug Info [91]
SL-89.0591 Drug Info [92]
SL-91.0893 Drug Info [93]
SOU-001 Drug Info [94]
SUN-9221 Drug Info [95]
Trimazosin Drug Info [96], [3]
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 1Alpha blockers for the treatment of benign prostatic hyperplasia. Rev Urol. 2007 Fall;9(4):181-90.
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: 7109).
REF 3Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
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: 7170).
REF 5Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019494)
REF 6FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074823.
REF 7(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 8Sedative 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 9Antihypertensive action and blockade of alpha1-adrenoceptors by DL-017, a quinazoline derivative. J Cardiovasc Pharmacol. 2001 Dec;38(6):893-9.
REF 10(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 11Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004255)
REF 12(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 13Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000562)
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REF 15Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013967)
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REF 20Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010685)
REF 21Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002662)
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REF 23Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005693)
REF 24Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011559)
REF 25Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003537)
REF 26Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014859)
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003628)
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REF 29Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006767)
REF 30Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000128)
REF 31Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008130)
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REF 36Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002398)
REF 37Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001859)
REF 38Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000354)
REF 39Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001560)
REF 40Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007056)
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