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Atiprosin Other names AY-28,228 Routes of administration Oral ATC code
(4aR ,12bS )-1-ethyl-12-methyl-4-(propan-2-yl)-1,2,3,4,4a,5,6,12b-octahydropyrazino[2',3':3,4]pyrido[1,2-a]indole
CAS Number PubChem CID ChemSpider UNII ChEMBL Formula C 20 H 29 N 3 Molar mass 311.473 g·mol−1 3D model (JSmol )
n23c1ccccc1c(c2[C@H]4N(CCN([C@@H]4CC3)C(C)C)CC)C
InChI=1S/C20H29N3/c1-5-21-12-13-22(14(2)3)18-10-11-23-17-9-7-6-8-16(17)15(4)19(23)20(18)21/h6-9,14,18,20H,5,10-13H2,1-4H3/t18-,20+/m1/s1
Y Key:WXNVFYIBELASJW-QUCCMNQESA-N
Y
N Y (what is this?)
Atiprosin (developmental code name AY-28,228 ) is an antihypertensive agent which acts as a selective α1 -adrenergic receptor antagonist .[1] [2] [3] [4] It also possesses some antihistamine activity, though it is some 15-fold weaker in this regard than as an alpha blocker .[3] It was never marketed.[1]
See also [ ]
References [ ]
^ a b David J. Triggle (1996). Dictionary of Pharmacological Agents . Boca Raton: Chapman & Hall/CRC. ISBN 0-412-46630-9 .
^ Jirkovsky I, Santroch G, Baudy R, Oshiro G (February 1987). "Octahydropyrazino[2',3':3,4]pyrido[1,2-a]indoles. A new class of potent antihypertensive agents". Journal of Medicinal Chemistry . 30 (2): 388–94. doi :10.1021/jm00385a022 . PMID 3806618 .
^ a b Grimes D, Rimele TJ, Henry DE, et al. (September 1987). "In vitro isolated tissue studies with atiprosin (AY-28,228): a new antihypertensive compound". Journal of Cardiovascular Pharmacology . 10 (3): 249–58. doi :10.1097/00005344-198709000-00001 . PMID 2444771 . S2CID 9361176 .
^ Oshiro G, Wojdan A, Klein M, Metcalf G (September 1987). "Antihypertensive and hypotensive actions of atiprosin (AY-28,228) in rats, dogs, and monkeys". Journal of Cardiovascular Pharmacology . 10 (3): 341–9. doi :10.1097/00005344-198709000-00014 . PMID 2444784 . S2CID 19086175 .
External links [ ]
Media related to Atiprosin at Wikimedia Commons
Sympatholytic (and closely related) antihypertensives (C02 )
Sympatholytics (antagonize α-adrenergic vasoconstriction )
Central
α2 -Adrenergic receptor agonists
Clonidine
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Guanfacine
Guanoxabenz
Methyldopa #
Tiamenidine ‡
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Guanadrel
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Doxazosin
Ketanserin
Indoramin
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Trimazosin
Urapidil
Non-selective α-adrenergic receptor blockers
Other antagonists
# WHO-EM
‡ Withdrawn from market
Clinical trials :
† Phase III
§ Never to phase III
α1
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Abanoquil
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Anisodine
Atiprosin
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Benoxathian
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Etoperidone
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L-765,314
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See also: Receptor/signaling modulators
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2-Pyridylethylamine
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UR-AK49
Antagonists
Others: Atypical antipsychotics (e.g., aripiprazole , asenapine , brexpiprazole , brilaroxazine , clozapine , iloperidone , olanzapine , paliperidone , quetiapine , risperidone , ziprasidone , zotepine )
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OUP-16
VUF-8430
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See also: Receptor/signaling modulators • Monoamine metabolism modulators • Monoamine reuptake inhibitors
Tricyclics
Classes Antidepressants (TCAs and TeCAs ) Antihistamines Antipsychotics Anticonvulsants Others
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