Target Information

Target General Infomation
Target ID
T11448
Former ID
TTDS00032
Target Name
Alpha-2A adrenergic receptor
Gene Name
ADRA2A
Synonyms
Alpha-2A adrenoceptor; Alpha-2A adrenoreceptor; Alpha-2AAR subtype C10; ADRA2A
Target Type
Successful
Disease Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90]
Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Dementia; Obesity [ICD9:290-294, 278; ICD10: F01-F07, E66]
Heart arrhythmia [ICD10: I47-I49]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Sexual dysfunction [ICD9: 302.7; ICD10: F52]
Function
Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine >norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone= prazosin > propanolol > alprenolol = pindolol.
BioChemical Class
GPCR rhodopsin
Target Validation
T11448
UniProt ID
P08913
Sequence
MGSLQPDAGNASWNGTEAPGGGARATPYSLQVTLTLVCLAGLLMLLTVFGNVLVIIAVFT
SRALKAPQNLFLVSLASADILVATLVIPFSLANEVMGYWYFGKAWCEIYLALDVLFCTSS
IVHLCAISLDRYWSITQAIEYNLKRTPRRIKAIIITVWVISAVISFPPLISIEKKGGGGG
PQPAEPRCEINDQKWYVISSCIGSFFAPCLIMILVYVRIYQIAKRRTRVPPSRRGPDAVA
APPGGTERRPNGLGPERSAGPGGAEAEPLPTQLNGAPGEPAPAGPRDTDALDLEESSSSD
HAERPPGPRRPERGPRGKGKARASQVKPGDSLPRRGPGATGIGTPAAGPGEERVGAAKAS
RWRGRQNREKRFTFVLAVVIGVFVVCWFPFFFTYTLTAVGCSVPRTLFKFFFWFGYCNSS
LNPVIYTIFNHDFRRAFKKILCRGDRKRIV
Drugs and Mode of Action
Drug(s) Connexyn Drug Info Approved Attention deficit hyperactivity disorder [1]
MOXONIDINE Drug Info Approved Alcohol use disorders [2]
MEDETOMIDINE Drug Info Phase 2 Pain [3]
MAZAPERTINE Drug Info Discontinued in Phase 2 Discovery agent [4]
NMI-870 Drug Info Discontinued in Phase 2 Sexual dysfunction [5]
A-80426 Drug Info Terminated Discovery agent [6]
S-18616 Drug Info Terminated Pain [7]
SK&F-104078 Drug Info Terminated Discovery agent [8]
SNAP-5089 Drug Info Terminated Heart arrhythmia [9], [10]
WB-4101 Drug Info Terminated Discovery agent [11], [12]
Inhibitor (+/-)-nantenine Drug Info [13]
(1,2,3,4-Tetrahydro-isoquinolin-3-yl)-methanol Drug Info [14]
(1H-Benzoimidazol-5-yl)-(1H-imidazol-2-yl)-amine Drug Info [15]
(1H-Imidazol-2-yl)-quinoxalin-6-yl-amine Drug Info [15]
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine Drug Info [15]
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine Drug Info [15]
(2-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine Drug Info [16]
(3-Ethyl-indol-1-yl)-propyl-pyridin-4-yl-amine Drug Info [16]
(3-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine Drug Info [16]
(R)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline Drug Info [17]
(S)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline Drug Info [17]
1',2',3',6'-Tetrahydro-[2,4']bipyridinyl Drug Info [18]
1,2,3,4,4a,5,10,10a-Octahydro-benzo[g]quinoline Drug Info [19]
1,2,3,4,5,6-Hexahydro-benzo[c]azocine Drug Info [17]
1,2,3,4-Tetrahydro-benzo[h]isoquinolin-8-ol Drug Info [20]
1,2,3,4-Tetrahydro-isoquinolin-7-ol Drug Info [20]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole Drug Info [21]
1,2,3,4-tetrahydroisoquinoline Drug Info [22]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info [23]
1-(3-Fluoro-pyridin-2-yl)-4-methyl-piperazine Drug Info [18]
1-(pyridin-2-yl)piperazine Drug Info [18]
2,3,4,5-Tetrahydro-1H-benzo[c]azepine Drug Info [17]
2,3,4,5-Tetrahydro-1H-benzo[e][1,4]diazepine Drug Info [17]
2,3,4,5-Tetrahydro-benzo[f][1,4]oxazepine Drug Info [17]
2,3-Dihydro-1H-isoindole Drug Info [17]
2-BFi Drug Info [24]
3-Fluoromethyl-1,2,3,4-tetrahydro-isoquinoline Drug Info [25]
3-Methoxymethyl-1,2,3,4-tetrahydro-isoquinoline Drug Info [14]
3-Methyl-1,2,3,4-tetrahydro-isoquinoline Drug Info [17]
3-Methyl-7-nitro-1,2,3,4-tetrahydro-isoquinoline Drug Info [26]
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole Drug Info [27]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [28]
4-(4-Methyl-indan-1-yl)-1H-imidazole Drug Info [29]
4-Benzo[b]thiophen-4-yl-1H-imidazole Drug Info [30]
5-Aminomethyl-naphthalen-2-ol Drug Info [20]
6,7,8,9-Tetrahydro-5-thia-8-aza-benzocycloheptene Drug Info [17]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [31]
7-Nitro-1,2,3,4-tetrahydro-isoquinoline Drug Info [26]
8-Methoxy-1,2,3,4-tetrahydro-benzo[h]isoquinoline Drug Info [20]
A-80426 Drug Info [32]
AKUAMMIGINE Drug Info [33]
AR-129330 Drug Info [34]
Butyl-indol-1-yl-pyridin-4-yl-amine Drug Info [16]
C-(6-Methoxy-naphthalen-1-yl)-methylamine Drug Info [20]
C-Naphthalen-1-yl-methylamine Drug Info [20]
Ethyl-indol-1-yl-pyridin-4-yl-amine Drug Info [16]
GNF-PF-2857 Drug Info [35]
GNF-PF-3427 Drug Info [35]
GNF-PF-3878 Drug Info [35]
Indol-1-yl-methyl-pyridin-4-yl-amine Drug Info [16]
Indol-1-yl-prop-2-ynyl-pyridin-4-yl-amine Drug Info [16]
Indol-1-yl-propyl-pyridin-4-yl-amine Drug Info [16]
Indol-1-yl-pyridin-4-yl-amine Drug Info [16]
MAZAPERTINE Drug Info [36]
MEDETOMIDINE Drug Info [27]
METHYLNORADRENALINE Drug Info [37]
MEZILAMINE Drug Info [38]
MOXONIDINE Drug Info [39]
PIPEROXAN Drug Info [37]
R-226161 Drug Info [40]
RX-821002 Drug Info [41]
S-34324 Drug Info [32]
SK&F-104078 Drug Info [42]
SK&F-29661 Drug Info [26]
SK&F-64139 Drug Info [22]
SNAP-5089 Drug Info [43]
SNAP-5150 Drug Info [43]
TRACIZOLINE Drug Info [31]
TRAMAZOLINE Drug Info [37]
TRYPTOLINE Drug Info [31]
WB-4101 Drug Info [37]
Agonist 4-Methoxyamphetamine Drug Info [44]
Chloroethylclonidine Drug Info [45]
Connexyn Drug Info [46]
Antagonist BRL 44408 Drug Info [47], [48]
Ciproxifan Drug Info [49]
Modulator NMI-870 Drug Info [50]
S-18616 Drug Info [51]
Pathways
KEGG Pathway cGMP-PKG signaling pathway
Neuroactive ligand-receptor interaction
PANTHER Pathway Alpha adrenergic receptor signaling pathway
Reactome Adrenoceptors
Adrenaline signalling through Alpha-2 adrenergic receptor
Adrenaline,noradrenaline inhibits insulin secretion
G alpha (i) signalling events
G alpha (z) signalling events
Surfactant metabolism
WikiPathways Monoamine GPCRs
GPCRs, Class A Rhodopsin-like
Platelet Aggregation (Plug Formation)
Integration of energy metabolism
GPCR ligand binding
GPCR downstream signaling
References
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