1998197-39-9
1998197-39-9 结构式
物理化学性质
沸点602.8±55.0 °C(Predicted)
密度1.283±0.06 g/cm3(Predicted)
储存条件2-8°C
溶解度DMSO: 2mg/mL, clear
酸度系数(pKa)7.52±0.18(Predicted)
形态Solid
颜色White to off-white
应用领域
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.常见问题列表
概述
ZCZ011 是一种有效且具有大脑渗透性的大麻素 1 (CB1) 受体正向变构调节剂。ZCZ011 增强 CP55,940 与 CB1 受体的结合，并增强花生四烯乙醇胺 (AEA) 刺激的 GTPγS 在小鼠脑膜上的结合。ZCZ011 还能增加 hCB1 细胞中 β- 抑制素招募和 ERK 磷酸化。ZCZ011 可用于研究神经性疼痛和炎症性疼痛。