Target Information

Target General Infomation
Target ID
T92609
Former ID
TTDC00292
Target Name
Alpha-1A adrenergic receptor
Gene Name
ADRA1A
Synonyms
Alpha 1A-adrenoceptor; Alpha 1A-adrenoreceptor; Alpha adrenergic receptor 1c; Alpha-1C adrenergic receptor; ADRA1A
Target Type
Successful
Disease Benign prostatic hyperplasia [ICD9: 600; ICD10: N40]
Cognitive disorders [ICD9: 290-294, 294.0, 780.09, 780.9, 780.93; ICD10: F01-F07, F04, F05, R41.3]
Female sexual dysfunction [ICD9: 302.7; ICD10: F52]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Hypertension [ICD9: 401; ICD10: I10-I16]
Heart arrhythmia [ICD10: I47-I49]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Prostate hyperplasia [ICD10: N40]
Prostate cancer; Benign prostatic hyperplasia [ICD9: 140-229, 185, 600; ICD10: C61, N40]
Prostate disease [ICD10: N42.9]
Post-traumatic stress disorder [ICD9: 309.81; ICD10: F43.1]
Stress urinary incontinence [ICD10: N39.3]
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, and its effect is mediated by G(q) and G(11) proteins.
BioChemical Class
GPCR rhodopsin
Target Validation
T92609
UniProt ID
P35348
Sequence
MVFLSGNASDSSNCTQPPAPVNISKAILLGVILGGLILFGVLGNILVILSVACHRHLHSV
THYYIVNLAVADLLLTSTVLPFSAIFEVLGYWAFGRVFCNIWAAVDVLCCTASIMGLCII
SIDRYIGVSYPLRYPTIVTQRRGLMALLCVWALSLVISIGPLFGWRQPAPEDETICQINE
EPGYVLFSALGSFYLPLAIILVMYCRVYVVAKRESRGLKSGLKTDKSDSEQVTLRIHRKN
APAGGSGMASAKTKTHFSVRLLKFSREKKAAKTLGIVVGCFVLCWLPFFLVMPIGSFFPD
FKPSETVFKIVFWLGYLNSCINPIIYPCSSQEFKKAFQNVLRIQCLCRKQSSKHALGYTL
HPPSQAVEGQHKDMVRIPVGSRETFYRISKTDGVCEWKFFSSMPRGSARITVSKDQSSCT
TARVRSKSFLQVCCCVGPSTPSLDKNHQVPTIKVHTISLSENGEEV
Drugs and Mode of Action
Drug(s) NAFTOPIDIL Drug Info Approved Hypertension [551871]
SILODOSIN Drug Info Approved Benign prostatic hyperplasia [468101], [529941], [530665]
Tamsulosin Drug Info Approved Benign prostatic hyperplasia [468085], [536610]
Xatral Drug Info Approved Benign prostatic hyperplasia [551871]
Besipirdine Drug Info Phase 3 Cognitive disorders [550094]
Dutasteride + tamsulosin Drug Info Phase 3 Prostate cancer; Benign prostatic hyperplasia [521609]
MEDETOMIDINE Drug Info Phase 2 Pain [529347]
CM-2236 Drug Info Preclinical Post-traumatic stress disorder [548834]
Sunepitron Drug Info Discontinued in Phase 3 Discovery agent [545699]
TIOSPIRONE Drug Info Discontinued in Phase 3 Discovery agent [538617], [544679]
L-771688 Drug Info Discontinued in Phase 2 Prostate disease [547208]
MAZAPERTINE Drug Info Discontinued in Phase 2 Discovery agent [545274]
RBx-2258 Drug Info Discontinued in Phase 2 Prostate hyperplasia [547000]
SOU-001 Drug Info Discontinued in Phase 2 Urinary incontinence [547251]
Taprizosin Drug Info Discontinued in Phase 2 Prostate hyperplasia [547527]
UPIDOSIN Drug Info Discontinued in Phase 2 Discovery agent [468110], [545508]
RS-100975 Drug Info Discontinued in Phase 1 Prostate disease [468114], [547119]
SDZ-NVI-085 Drug Info Discontinued in Phase 1 Major depressive disorder [544963]
A-131701 Drug Info Terminated Discovery agent [546501]
A-204176 Drug Info Terminated Stress urinary incontinence [547179]
ABANOQUIL Drug Info Terminated Discovery agent [544556]
AGN-193080 Drug Info Terminated Discovery agent [546437]
BMY-7378 Drug Info Terminated Discovery agent [543289], [544847]
KRG-3332 Drug Info Terminated Glaucoma [547722]
L-757464 Drug Info Terminated Prostate hyperplasia [546739]
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]
SNAP-6201 Drug Info Terminated Discovery agent [546603]
WB-4101 Drug Info Terminated Discovery agent [468117], [545656]
Sunepitron Drug Info Investigative Unspecified [528210]
Inhibitor (+/-)-nantenine Drug Info [530558]
(-)-SNAP-5399 Drug Info [527393]
(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-(4-tert-Butyl-phenyl)-4,5-dihydro-1H-imidazole Drug Info [527180]
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]
8-Piperazin-1-yl-imidazo[1,2-a]pyrazine Drug Info [526778]
A-119637 Drug Info [527393]
A-123189 Drug Info [527393]
A-131701 Drug Info [527393]
A-315456 Drug Info [527393]
ABANOQUIL Drug Info [533682]
AGN-192172 Drug Info [551280]
AGN-193080 Drug Info [551280]
BMY-7378 Drug Info [527512]
CORYNANTHEINE Drug Info [527393]
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]
L-765314 Drug Info [527393]
L-771688 Drug Info [527393]
LEVONORDEFRIN Drug Info [534160]
MAZAPERTINE Drug Info [533800]
MEDETOMIDINE Drug Info [533805]
N-(5-Bromo-quinoxalin-6-yl)-guanidine Drug Info [551280]
NAFTOPIDIL Drug Info [527393]
NIGULDIPINE Drug Info [533638]
OCTOCLOTHEPIN Drug Info [531171]
R-226161 Drug Info [528772]
Ro-11-04253 Drug Info [527393]
RS-100329 Drug Info [527393]
RS-513815 Drug Info [527393]
RWJ-38063 Drug Info [527393]
RWJ-68141 Drug Info [527393]
RWJ-68157 Drug Info [527393]
RWJ-69736 Drug Info [527393]
RX-821002 Drug Info [533375]
SILODOSIN Drug Info [527393]
Siramesine Drug Info [533739]
SK&F-104078 Drug Info [533638]
SK&F-104856 Drug Info [533638]
SK&F-105854 Drug Info [527393]
SK&F-106686 Drug Info [533638]
SK&F-86466 Drug Info [533638]
SNAP-5036 Drug Info [527393]
SNAP-5089 Drug Info [533638]
SNAP-6201 Drug Info [527393]
SNAP-7915 Drug Info [527393]
SNAP-8719 Drug Info [527512]
SNAP-94847 Drug Info [528972]
SPIPERONE Drug Info [527393]
Sunepitron Drug Info [528210]
TIOSPIRONE Drug Info [534093]
UH-301 Drug Info [534363]
UPIDOSIN Drug Info [527393]
WB-4101 Drug Info [533682]
Agonist 4-Methoxyamphetamine Drug Info [551380]
A-204176 Drug Info [526245]
CM-2236 Drug Info [550867]
Antagonist Besipirdine Drug Info [534361]
Dutasteride + tamsulosin Drug Info [550963]
GG-818 Drug Info [534666]
KRG-3332 Drug Info [534750]
L-757464 Drug Info [546740]
RBx-2258 Drug Info [544170]
REC2615 Drug Info [536493]
RS-100975 Drug Info [525514]
SDZ-NVI-085 Drug Info [534234]
Taprizosin Drug Info [528839]
Xatral Drug Info [549823]
Modulator SOU-001 Drug Info [527154]
Tamsulosin Drug Info [556264]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Calcium signaling pathway
cGMP-PKG signaling pathway
Neuroactive ligand-receptor interaction
AMPK signaling pathway
Adrenergic signaling in cardiomyocytes
Vascular smooth muscle contraction
Salivary secretion
PANTHER Pathway Alpha adrenergic receptor 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
Endothelin Pathways
GPCR ligand binding
GPCR downstream signaling
AMPK Signaling
References
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Ref 468101(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: 493).
Ref 468110(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: 496).
Ref 468114(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: 497).
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).
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