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]
Heart arrhythmia [ICD10: I47-I49]
Heart failure [ICD9: 428; ICD10: I50]
Hypertension [ICD9: 401; ICD10: I10-I16]
Hypotension [ICD9: 458, 796.3; ICD10: I95]
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]
Obesity [ICD9: 278; ICD10: E66]
Ocular hypertension [ICD9: 365.04; ICD10: H40.0]
Ocular disease [ICD10: H00-H59]
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]
Prostate disease [ICD10: N42.9]
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
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
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 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.
Ref 522245ClinicalTrials.gov (NCT00630474) Nasal Decongestion and Obstructive Sleep Apnea. U.S. National Institutes of Health.
Ref 522318ClinicalTrials.gov (NCT00675207) Comparison of Brimonidine Purite, Dorzolamide, and Brinzolamide as Adjunctive Therapy to Prostaglandin Analogs. U.S. National Institutes of Health.
Ref 523141ClinicalTrials.gov (NCT01186068) Dose Response Study of Patients With Erythematous Rosacea. U.S. National Institutes of Health.
Ref 525230ClinicalTrials.gov (NCT02471196) Efficacy of ORM-12741 on Agitation/Aggression Symptoms in Alzheimer's Disease.
Ref 526626The role of I(1)-imidazoline and alpha(2)-adrenergic receptors in the modulation of glucose metabolism in the spontaneously hypertensive obese rat model of metabolic syndrome X. J Pharmacol Exp Ther.2003 Aug;306(2):646-57. Epub 2003 May 19.
Ref 529302Prolonged cardiovascular effects after unintentional ingestion of tetrahydrozoline. Clin Toxicol (Phila). 2008 Feb;46(2):171-2.
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 533548Effect of dihydroergocristine on blood pressure and activity at peripheral alpha-adrenoceptors in pithed rats. Eur J Pharmacol. 1984 Jan 13;97(1-2):21-7.
Ref 533886Effects of amosulalol, a combined alpha 1- and beta-adrenoceptor-blocking agent, on ischemic myocardial energy metabolism in dogs. J Pharm Sci. 1993 Mar;82(3):291-5.
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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).
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)
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Ref 547220Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014166)
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Ref 525507J Med Chem. 1999 Jun 3;42(11):1982-90.3,7-Disubstituted-1,2,3,4-tetrahydroisoquinolines display remarkable potency and selectivity as inhibitors of phenylethanolamine N-methyltransferase versus the alpha2-adrenoceptor.
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Ref 525733Bioorg Med Chem Lett. 2000 Mar 20;10(6):605-7.Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand.
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Ref 526102Affinity of serotonin receptor antagonists and agonists to recombinant and native alpha1-adrenoceptor subtypes. Jpn J Pharmacol. 2001 Jun;86(2):189-95.
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Ref 526770Pharmacological characteristics of alpha 2-adrenergic receptors: comparison of pharmacologically defined subtypes with subtypes identified by molecular cloning. Mol Pharmacol. 1992 Jul;42(1):1-5.
Ref 526773Different sites of action for alpha 2-adrenoceptor antagonists in the modulation of noradrenaline release and contraction response in the vas deferens of the rat. J Pharm Pharmacol. 1992 Mar;44(3):231-4.
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.
Ref 528199A novel approach to the treatment of benign prostatic hyperplasia. BJU Int. 2006 Jun;97(6):1252-5.
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.
Ref 533375J Med Chem. 1986 Oct;29(10):2000-3.Alpha-adrenoreceptor reagents. 4. Resolution of some potent selective prejunctional alpha 2-adrenoreceptor antagonists.
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