Target Information

Target General Infomation
Target ID
T01777
Former ID
TTDR01180
Target Name
Alpha-2C adrenergic receptor
Gene Name
ADRA2C
Synonyms
Alpha-2C adrenoceptor; Alpha-2C adrenoreceptor; Subtype C4; ADRA2C
Target Type
Successful
Disease Allergic rhinitis [ICD9: 472.0, 477, 995.3; ICD10: J00, J30, J31.0, T78.4]
Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Alzheimer disease [ICD9: 331; ICD10: G30]
Asthma [ICD10: J45]
Contusion [ICD10: S36.220S]
Depression [ICD9: 311; ICD10: F30-F39]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Dementia; Obesity [ICD9:290-294, 278; ICD10: F01-F07, E66]
Diabetic nephropathy; Fibromyalgia [ICD9:250.4, 729.1; ICD10: E11.21, M79.7]
Erythema [ICD9: 695; ICD10: L51-L54]
Fibromyalgia [ICD9: 729.1; ICD10: M79.7]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Hypotension [ICD9: 458, 796.3; ICD10: I95]
Heart arrhythmia [ICD10: I47-I49]
Heart failure [ICD9: 428; ICD10: I50]
Hypertension [ICD9: 401; ICD10: I10-I16]
Male sexual disorders [ICD10: F52]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Ocular disease [ICD10: H00-H59]
Obesity [ICD9: 278; ICD10: E66]
Ocular hypertension [ICD9: 365.04; ICD10: H40.0]
Prostate disease [ICD10: N42.9]
Poison intoxication [ICD10: T36-T50]
Peptic ulcer [ICD9: 531-534; ICD10: K25-K27]
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T01777
UniProt ID
P18825
Sequence
MASPALAAALAVAAAAGPNASGAGERGSGGVANASGASWGPPRGQYSAGAVAGLAAVVGF
LIVFTVVGNVLVVIAVLTSRALRAPQNLFLVSLASADILVATLVMPFSLANELMAYWYFG
QVWCGVYLALDVLFCTSSIVHLCAISLDRYWSVTQAVEYNLKRTPRRVKATIVAVWLISA
VISFPPLVSLYRQPDGAAYPQCGLNDETWYILSSCIGSFFAPCLIMGLVYARIYRVAKLR
TRTLSEKRAPVGPDGASPTTENGLGAAAGAGENGHCAPPPADVEPDESSAAAERRRRRGA
LRRGGRRRAGAEGGAGGADGQGAGPGAAESGALTASRSPGPGGRLSRASSRSVEFFLSRR
RRARSSVCRRKVAQAREKRFTFVLAVVMGVFVLCWFPFFFSYSLYGICREACQVPGPLFK
FFFWIGYCNSSLNPVIYTVFNQDFRRSFKHILFRRRRRGFRQ
Structure
1HLL; 1HO9; 1HOD; 1HOF
Drugs and Mode of Action
Drug(s) Amezinium Drug Info Approved Hypotension [551871]
Amosulalol Drug Info Approved Hypertension [533886]
Brimonidine Drug Info Approved Ocular hypertension [468255], [522318]
Dihydroergocristine Drug Info Approved Alcohol use disorders [533548], [539825]
MOXONIDINE Drug Info Approved Alcohol use disorders [526626]
Propylhexedrine Drug Info Approved Obesity [551871]
Rilmenidine Drug Info Approved Hypertension [551871]
Tetrahydrozoline Drug Info Approved Ocular disease [529302]
Xylometazoline Drug Info Phase 4 Allergic rhinitis [468231], [522245]
IDAZOXAN HYDROCHLORIDE Drug Info Phase 3 Neurological disease [521807]
TNX-102 Drug Info Phase 3 Fibromyalgia [547624]
AGN-XX/YY Drug Info Phase 2 Diabetic nephropathy; Fibromyalgia [549889]
MEDETOMIDINE Drug Info Phase 2 Pain [529347]
ORM-12741 Drug Info Phase 2 Alzheimer disease [525230]
V-101 Drug Info Phase 2 Erythema [523141]
INDORAMIN Drug Info Withdrawn from market Hypertension [468125], [551871]
Ecabapide Drug Info Discontinued in Preregistration Peptic ulcer [544686]
Delequamine hydrochloride Drug Info Discontinued in Phase 3 Male sexual disorders [546534]
FLUPAROXAN Drug Info Discontinued in Phase 3 Depression [540696], [544705]
NOLOMIROLE HYDROCHLORIDE Drug Info Discontinued in Phase 3 Heart failure [545464]
Deriglidole Drug Info Discontinued in Phase 2 Diabetes [544511]
Fadolmidine Drug Info Discontinued in Phase 2 Pain [547121]
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]
MK-912 Drug Info Discontinued in Phase 2 Discovery agent [544718]
NMI-870 Drug Info Discontinued in Phase 2 Sexual dysfunction [547220]
SGB-1534 Drug Info Discontinued in Phase 2 Hypotension [544565]
GYKI-12743 Drug Info Discontinued in Phase 1 Hypertension [545079]
A-75169 Drug Info Terminated Glaucoma [545494]
A-80426 Drug Info Terminated Discovery agent [546043]
ARC239 Drug Info Terminated Discovery agent [540708], [544602]
F-14413 Drug Info Terminated Alzheimer disease [547865]
Midaglizole Drug Info Terminated Asthma [544537]
SK&F-104078 Drug Info Terminated Discovery agent [544626]
SNAP-5089 Drug Info Terminated Heart arrhythmia [468115], [546179]
WB-4101 Drug Info Terminated Discovery agent [468117], [545656]
Inhibitor (+/-)-nantenine Drug Info [530558]
(1,2,3,4-Tetrahydro-isoquinolin-3-yl)-methanol Drug Info [525507]
(1H-Benzoimidazol-5-yl)-(1H-imidazol-2-yl)-amine Drug Info [534315]
(1H-Imidazol-2-yl)-quinoxalin-6-yl-amine Drug Info [534315]
(2,6-Dichloro-phenyl)-(1H-imidazol-2-yl)-amine Drug Info [534315]
(2-Bromo-phenyl)-(1H-imidazol-2-yl)-amine Drug Info [534315]
(2-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine Drug Info [534087]
(3-Ethyl-indol-1-yl)-propyl-pyridin-4-yl-amine Drug Info [534087]
(3-Methyl-indol-1-yl)-propyl-pyridin-4-yl-amine Drug Info [534087]
(R)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline Drug Info [534195]
(S)-3-Methyl-1,2,3,4-tetrahydro-isoquinoline Drug Info [534195]
1,2,3,4,4a,5,10,10a-Octahydro-benzo[g]quinoline Drug Info [534719]
1,2,3,4,5,6-Hexahydro-benzo[c]azocine Drug Info [534195]
1,2,3,4-Tetrahydro-benzo[h]isoquinolin-8-ol Drug Info [534531]
1,2,3,4-Tetrahydro-isoquinolin-7-ol Drug Info [534531]
1,2,3,4-Tetrahydro-pyrazino[1,2-a]indole Drug Info [526994]
1,2,3,4-tetrahydroisoquinoline Drug Info [528403]
1-((S)-2-aminopropyl)-1H-indazol-6-ol Drug Info [527952]
2,3,4,5-Tetrahydro-1H-benzo[c]azepine Drug Info [534195]
2,3,4,5-Tetrahydro-1H-benzo[e][1,4]diazepine Drug Info [534195]
2,3,4,5-Tetrahydro-benzo[f][1,4]oxazepine Drug Info [534195]
2,3-Dihydro-1H-isoindole Drug Info [534195]
2-BFi Drug Info [525733]
3-Fluoromethyl-1,2,3,4-tetrahydro-isoquinoline Drug Info [527365]
3-Methoxymethyl-1,2,3,4-tetrahydro-isoquinoline Drug Info [525507]
3-Methyl-1,2,3,4-tetrahydro-isoquinoline Drug Info [534195]
4-(1-Naphthalen-1-yl-ethyl)-1H-imidazole Drug Info [533805]
4-(4-Methyl-indan-1-yl)-1H-imidazole Drug Info [534467]
5-Aminomethyl-naphthalen-2-ol Drug Info [534531]
6,7,8,9-Tetrahydro-5-thia-8-aza-benzocycloheptene Drug Info [534195]
7-Methoxy-2,3,4,9-tetrahydro-1H-beta-carboline Drug Info [526918]
8-Methoxy-1,2,3,4-tetrahydro-benzo[h]isoquinoline Drug Info [534531]
A-80426 Drug Info [527481]
Butyl-indol-1-yl-pyridin-4-yl-amine Drug Info [534087]
C-(6-Methoxy-naphthalen-1-yl)-methylamine Drug Info [534531]
C-Naphthalen-1-yl-methylamine Drug Info [534531]
CONESSINE Drug Info [529632]
Ethyl-indol-1-yl-pyridin-4-yl-amine Drug Info [534087]
GNF-PF-2857 Drug Info [528472]
GNF-PF-3427 Drug Info [528472]
GNF-PF-3878 Drug Info [528472]
Indol-1-yl-methyl-pyridin-4-yl-amine Drug Info [534087]
Indol-1-yl-prop-2-ynyl-pyridin-4-yl-amine Drug Info [534087]
Indol-1-yl-propyl-pyridin-4-yl-amine Drug Info [534087]
Indol-1-yl-pyridin-4-yl-amine Drug Info [534087]
INDORAMIN Drug Info [533682]
MAZAPERTINE Drug Info [533800]
MEDETOMIDINE Drug Info [533805]
METHYLNORADRENALINE Drug Info [533545]
MEZILAMINE Drug Info [533406]
MOXONIDINE Drug Info [534128]
PIPEROXAN Drug Info [533545]
R-226161 Drug Info [528772]
RX-821002 Drug Info [533375]
S-34324 Drug Info [527481]
SK&F-104078 Drug Info [533682]
SK&F-64139 Drug Info [528403]
SNAP-5089 Drug Info [525611]
SNAP-5150 Drug Info [525611]
TRACIZOLINE Drug Info [526918]
TRAMAZOLINE Drug Info [533545]
TRYPTOLINE Drug Info [526918]
WB-4101 Drug Info [533545]
Modulator (allosteric modulator) 5-(N,N-hexamethylene)-amiloride Drug Info [534623]
Antagonist 5-methylurapidil Drug Info [526042]
all-trans-4-oxo-retinoic acid Drug Info [527472]
ARC239 Drug Info [535225]
Ciproxifan Drug Info [536039]
F-14413 Drug Info [527640]
GYKI-16084 Drug Info [528199]
JP1302 Drug Info [528615]
JTH-601 Drug Info [525752]
MK-912 Drug Info [534977]
ORM-12741 Drug Info [532654]
piribedil Drug Info [526443]
spiroxatrine Drug Info [526102]
TNX-102 Drug Info [551739]
[125I]BE-2254 Drug Info [533751]
[3H]MK-912 Drug Info [533843]
[3H]rauwolscine Drug Info [526770]
[3H]RX821002 Drug Info [533799]
Agonist 6-fluoro-noradrenaline Drug Info [533826]
A61603 Drug Info [533660]
AGN-XX/YY Drug Info [550943]
amidephrine Drug Info [533826]
Chloroethylclonidine Drug Info [537921]
cirazoline Drug Info [533826]
Fadolmidine Drug Info [527103]
indanidine Drug Info [533826]
SKF 89748 Drug Info [533826]
V-101 Drug Info [532145]
xylazine Drug Info [534634]
[125I]HEAT Drug Info [533679]
Modulator A-75169 Drug Info [550028]
Amezinium Drug Info [533574], [551871]
Amosulalol Drug Info [533886], [551871]
Brimonidine Drug Info [468255]
Delequamine hydrochloride Drug Info [534174]
Deriglidole Drug Info [534576]
Dihydroergocristine Drug Info [533548], [551871]
Ecabapide Drug Info [534260]
ETHOXY-IDAZOXAN Drug Info [531785]
FLUPAROXAN Drug Info [528251]
GYKI-12743 Drug Info [528315]
IDAZOXAN HYDROCHLORIDE Drug Info [526773]
Midaglizole Drug Info [533463]
NMI-870 Drug Info [544155]
NOLOMIROLE HYDROCHLORIDE Drug Info [526875]
Propylhexedrine Drug Info [533622], [551871]
Rilmenidine Drug Info [534272], [551871]
SGB-1534 Drug Info [533371]
Tetrahydrozoline Drug Info [529302], [551871]
V-103 Drug Info [543685]
Xylometazoline Drug Info [530593], [551871]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway cGMP-PKG signaling pathway
Neuroactive ligand-receptor interaction
PANTHER Pathway Alpha adrenergic receptor signaling pathway
Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated 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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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 468231(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: 517).
Ref 468255(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: 520).
Ref 521807ClinicalTrials.gov (NCT00294944) The Effectiveness of Idazoxan in Treating TRD. U.S. National Institutes of Health.
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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.
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Ref 540696(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: 41).
Ref 540708(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: 524).
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Ref 526875Effect of nolomirole on monocrotaline-induced heart failure. Pharmacol Res. 2004 Jan;49(1):1-5.
Ref 526918Bioorg Med Chem Lett. 2004 Jan 19;14(2):527-9.Binding of an imidazopyridoindole at imidazoline I2 receptors.
Ref 526994Bioorg Med Chem Lett. 2004 Feb 23;14(4):1003-5.Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.
Ref 527103Antinociceptive properties of fadolmidine (MPV-2426), a novel alpha2-adrenoceptor agonist. CNS Drug Rev. 2004 Summer;10(2):117-26.
Ref 527365J Med Chem. 2005 Jan 13;48(1):134-40.3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.
Ref 527472Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents. J Med Chem. 2005 Mar 24;48(6):1709-12.
Ref 527481J Med Chem. 2005 Mar 24;48(6):2054-71.Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Ref 527640Activation of noradrenergic transmission by alpha2-adrenoceptor antagonists counteracts deafferentation-induced neuronal death and cell proliferation in the adult mouse olfactory bulb. Exp Neurol. 2005 Aug;194(2):444-56.
Ref 527952J Med Chem. 2006 Jan 12;49(1):318-28.1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
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Ref 528251The pharmacology of fluparoxan: a selective alpha 2-adrenoceptor antagonist. Br J Pharmacol. 1991 Apr;102(4):887-95.
Ref 528315GYKI-12743 a new postsynaptic vascular alpha-adrenoceptor antagonist. Acta Physiol Hung. 1991;77(3-4):257-67.
Ref 528403J Med Chem. 2006 Sep 7;49(18):5424-33.Comparison of the binding of 3-fluoromethyl-7-sulfonyl-1,2,3,4-tetrahydroisoquinolines with their isosteric sulfonamides to the active site of phenylethanolamineN-methyltransferase.
Ref 528472J Med Chem. 2006 Oct 19;49(21):6351-63.Structure-activity relationship of quinoline derivatives as potent and selective alpha(2C)-adrenoceptor antagonists.
Ref 528615Pharmacological characterization and CNS effects of a novel highly selective alpha2C-adrenoceptor antagonist JP-1302. Br J Pharmacol. 2007 Feb;150(4):391-402. Epub 2007 Jan 15.
Ref 528772Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. Epub 2007 Mar 21.Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
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Ref 529632J Med Chem. 2008 Sep 11;51(17):5423-30. Epub 2008 Aug 7.The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
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 530593Alpha-adrenoceptor agonistic activity of oxymetazoline and xylometazoline. Fundam Clin Pharmacol. 2010 Dec;24(6):729-39.
Ref 531785Discriminative stimulus properties of ethoxy idazoxan. J Psychopharmacol. 1995 Jan;9(3):228-33.
Ref 532145Rosacea: update on management and emerging therapies. Skin Therapy Lett. 2012 Dec;17(10):1-4.
Ref 532654A double-blind, randomized, placebo-controlled crossover trial of the alpha2C-adrenoceptor antagonist ORM-12741 for prevention of cold-induced vasospasm in patients with systemic sclerosis. Rheumatology (Oxford). 2014 May;53(5):948-52.
Ref 533371Potent alpha-adrenoceptor blocking action of SGB-1534, a new quinazoline antihypertensive agent in vitro experiments. Gen Pharmacol. 1986;17(2):143-9.
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