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A 77636 hydrochloride
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
A 77636 hydrochloride图片
CAS NO:145307-34-2
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
A 77636 hydrochloride 是一种有效的、具有口服活性、选择性和长效的多巴胺 D1 受体激动剂 (pKi\u003d7.40; Ki\u003d39.8 nM)，具有抗帕金森病活性。
Cas No.145307-34-2
化学名(1R,3S)-3-((1s,3R,5R,7S)-adamantan-1-yl)-1-(aminomethyl)isochroman-5,6-diol hydrochloride
Canonical SMILESOC(C1=C(C=C2)[C@H](CN)O[C@@H](C1)[C@]3(C[C@H](C4)C5)C[C@@H]4C[C@H]5C3)=C2O.Cl
分子式C20H27NO3.HCl
分子量365.9
溶解度DMF: 33 mg/ml,DMSO: 33 mg/ml,Ethanol: 33 mg/ml,Ethanol:PBS (pH 7.2) (1:6): 0.14 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

A 77636 hydrochloride is a potent and selective agonist of dopamine D1 receptor with Ki value of 39.8 nM [1].

Dopamine D1 receptor is a G-protein couple receptor for dopamine and stimulates adenylate cyclase and cyclic AMP-dependent protein kinases. Dopamine D1 receptor plays an important role in behavioral responses and neuronal growth and development.

A 77636 hydrochloride is a potent and selective dopamine D1 receptor agonist. A-77636 exhibited agonist activities with pEC50 values of 8.13 and 8.97 in the fish retina and the rat caudate-putamen, respectively [1]. In SK-N-MC neuroblastoma cell line, A-77636 significantly induced residual cAMP production [2].

In rats and mice, A-77636 induced forelimb clonus. In marmosets, A-77636 increased locomotor activity and inhibited the parkinsonian-like symptoms induced by MPTP [1]. In rat, A-77636 (4 μmol/kg) significantly increased acetylcholine release in both cortical and hippocampal. However, at a lower dose (1 μmol/kg) A-77636 only stimulated cortical acetylcholine release [3].

References:
[1].  Kebabian JW, Britton DR, DeNinno MP, et al. A-77636: a potent and selective dopamine D1 receptor agonist with antiparkinsonian activity in marmosets. Eur J Pharmacol, 1992, 229(2-3): 203-209.
[2].  Lin CW, Bianchi BR, Miller TR, et al. Persistent activation of the dopamine D1 receptor contributes to prolonged receptor desensitization: studies with A-77636. J Pharmacol Exp Ther, 1996, 276(3): 1022-1029.
[3].  Acquas E, Day JC, Fibiger HC. The potent and selective dopamine D1 receptor agonist A-77636 increases cortical and hippocampal acetylcholine release in the rat. Eur J Pharmacol, 1994, 260(1): 85-87.