Org 27569

Org 27569CAS号: 868273-06-7分子式: C24H28ClNO3分子量: 409.95描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

Org 27569是cannabinoid CB1 receptor变构调节剂,通过增强激动剂亲和力而诱导CB1受体状态改变,且降低逆向激动剂的亲和力。

纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
5-氯-3-乙基N-[2-(4-哌啶-1-基)苯基乙基]-1H-吲哚-2-甲酰胺
外观
white
可溶性/溶解性
DMSO :41 mg/mL (100 mM)
生物活性
靶点
CB1
In vitro(体外研究)
Org 27569 is an allosteric modulator of CB1 cannabinoid receptor. It significantly increases the binding of CB1 receptor agonist and causes a significant decrease in specific binding of CB1 receptor inverse agonist. Org 27569 induces CB1 high affinity agonist binding, receptor internalization, and downstream ERK phosphorylation. The allosteric ligand Org 27569 promotes agonist binding to CB1, yet blocks the agonist-induced conformational changes in TM6. Org 27569 traps the receptor in a distinct agonist-bound, but nonsignaling conformational state.
In vivo(体内研究)
ORG 27569 (3.2 and 5.6 mg/kg, i.p.) significantly attenuates cocaine associated cue-induced reinstatement, cocaine priming-induced reinstatement, methamphetamine associated cue-induced reinstatement and methamphetamine priming-induced reinstatement in rat. Org27569 (30 mg/kg, i.p.) produces CB1-independent hypophagic effects and does not affect the discriminative stimulus effects of anandamide (AEA). Org27569 (100 μg intracerebroventricularly) does not affect the pharmacologic effects of systemically administered CP55,940 compared with vehicle.

分子结构图

Org 27569