1998197-39-9
1998197-39-9 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點(diǎn)602.8±55.0 °C(Predicted)
密度1.283±0.06 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
溶解度DMSO: 2mg/mL, clear
酸度系數(shù)(pKa)7.52±0.18(Predicted)
形態(tài)Solid
顏色White to off-white
應(yīng)用領(lǐng)域
用途一
ZCZ011 is a positive allosteric modulator of the cannabinoid CB1 receptor. ZCZ011 potentiated binding of [(3)H]CP55,940 to the CB1 receptor as well as enhancing AEA-stimulated [(35)S]GTPγS binding in mouse brain membranes and β-arrestin recruitment and ERK phosphorylation in hCB1 cells. In the whole animal, ZCZ011 is brain penetrant, increased the potency of these orthosteric agonists in mouse behavioral assays indicative of cannabimimetic activity, including antinociception, hypothermia, catalepsy, locomotor activity, and in the drug discrimination paradigm. ZCZ011 acts as a CB1 PAM and provide the first proof of principle that CB1 PAMs offer a promising strategy to treat neuropathic and inflammatory pain with minimal or no cannabimimetic side effects.常見問題列表
概述
ZCZ011 是一種有效且具有大腦滲透性的大麻素 1 (CB1) 受體正向變構(gòu)調(diào)節(jié)劑。ZCZ011 增強(qiáng) CP55,940 與 CB1 受體的結(jié)合，并增強(qiáng)花生四烯乙醇胺 (AEA) 刺激的 GTPγS 在小鼠腦膜上的結(jié)合。ZCZ011 還能增加 hCB1 細(xì)胞中 β- 抑制素招募和 ERK 磷酸化。ZCZ011 可用于研究神經(jīng)性疼痛和炎癥性疼痛。