102704-40-5

基本信息
中文別名
化合物 T27405 英文別名
AZ4AZ 4
AZ-4
GAT-211
GAT211 >=98% (HPLC)
3-(2-nitro-1-phenylethyl)-2-phenyl-1H-indole
1H-Indole, 3-(2-nitro-1-phenylethyl)-2-phenyl-
物理化學(xué)性質(zhì)
儲存條件-20°C儲存
溶解度DMF: 25 mg/ml; DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml; DMSO: 10 mg/ml; Ethanol: 5 mg/ml
形態(tài)結(jié)晶固體
顏色White to off-white
應(yīng)用領(lǐng)域
用途一
GAT211, aslo known as AZ-4, is a small molecule CB1 positive allosteric modulator. GAT211 suppresses allodynia and produces synergistic antiallodynic effects with fatty acid amide hydrolase and monoacylglycerol lipase inhibitors in paclitaxel-treated mice. Positive allosteric modulation of CB1-receptor signaling with GAT211shows promise as a safe and effective analgesic strategy that lacks tolerance, dependence, and abuse liability.常見問題列表
概述
GAT211 是一種大麻素 1 受體 (CB1R) 正變構(gòu)調(diào)節(jié)劑 (PAM),pKb 為 7.26。GAT211 對 cAMP 和 β-arrestin2 的 EC50 分別為 260 nM,650 nM。GAT211 可用于神經(jīng)性和/或炎癥性疼痛的研究。