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Rispenzepine
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。
Rispenzepine图片
CAS NO:96449-05-7
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
Rispenzepine是一种选择性毒蕈碱受体(M1和M3受体亚型)拮抗剂。
Cas No.96449-05-7
别名利喷西平
Canonical SMILESO=C1C2=CC=CN=C2N(C(C3CN(C)CCC3)=O)C4=CC=CC=C4N1
分子式C19H20N4O2
分子量336.39
溶解度Soluble in DMSO
储存条件Store at -20°C
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

Rispenzepine is a novel antimuscarinic compound with a preferential action at M1, and M3 receptor subtypes.

The presence of muscarinic autoreceptors in human and guinea pig trachea is investigated by comparing the effects of the muscarinic receptor antagonists Pirenzepine (M1), Methoctramine (M2), 4-DAMP (M3), and Rispenzepine (M1/M3) on cholinergic neural contractile responses evoked by electrical field stimulation (EFS) and [3H]ACh release. The M1, M1/M3, or M3 antagonists inhibit the EFS-evoked cholinergic contractile response in a concentration-dependent manner (4-DAMP >Rispenzepine >Pirenzepine), whereas Methoctramine facilitates this response at low concentrations (<3 μM). In ACh release studies, the M3 antagonist has no significant effect, whereas Pirenzepine, Methoctramine, and Rispenzepine significantly increase ACh release in guinea pig trachea. Rispenzepine almost completely inhibits cholinergic, contractile responses at 0.3 μM (92.7±6.2% inhibition, n=6, p<0.05; pD2 value of 7.31±0.15) [1].

[1]. Patel HJ, et al. Evidence for prejunctional muscarinic autoreceptors in human and guinea pig trachea. Am J Respir Crit Care Med. 1995 Sep;152(3):872-8.