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Rivanicline hemioxalate
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。
Rivanicline hemioxalate图片
包装:500 mg
市场价:18698元

产品名称
RJR-2403 hemioxalate
(E)-Metanicotine hemioxalate
产品介绍
Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) 是一种神经元烟碱受体 (neuronal nicotinic receptor) 激动剂,对 α4β2 亚型有高度选择性(Ki= 26 nM),比对于 α7 受体的选择性高1000倍(Ki=3.6 μM)。

产品描述

Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) is a neuronal nicotinic receptor agonist, exhibiting high selectivity for the α4β2 subtype ( K i =26 nM); over 1,000 fold selectivity than α7 receptors( K i = 3.6 μM). IC50 value: 26 nM [1] Target: α4β2 nAChR in vitro: At concentrations up to 1 mM, Rivanicline does not significantly activate nAChRs in PC12 cells, muscle type nAChRs or muscarinic receptors. Dose-response curves for agonist-induced ileum contraction indicate that Rivanicline is less than one-tenth as potent as nicotine with greatly reduced efficacy. Rivanicline does not antagonize nicotine-stimulated muscle or ganglionic nAChR function (IC50 >1 mM). Chronic exposure of M10 cells to Rivanicline (10 microM) results in an up-regulation of high-affinity nAChRs phenomenologically similar to that seen with nicotine [1]. in vivo: Rivanicline significantly improved passive avoidance retention after scopolamine-induced amnesia and enhanced both working and reference memory in rats with ibotenic acid lesions of the forebrain cholinergic projection system in an 8-arm radial maze paradigm. By comparison, Rivanicline was 15 to 30-fold less potent than nicotine in decreasing body temperature, respiration, Y-maze rears and crosses and acoustic startle response [2]. Metanicotine was about 5-fold less potent than nicotine in the tail-flick test after s.c administration, but slightly more potent after central administration [3].

Cas No.

T12738

分子式

C12H16N2O4

分子量

207.23

别名

RJR-2403 hemioxalate;(E)-Metanicotine hemioxalate;Rivanicline hemioxalate

储存和溶解度

DMSO:50 mg/mL (241.28 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years