AM1241

一种CB2受体激动剂；对CB2受体的选择性强于CB1受体（Kis = 7.1 和 580 nM）；被认为是一种蛋白质激动剂，因为它在不同的实验中具有中性拮抗剂和部分激动剂的活性；在体外的作用因物种而异，在人类CB2受体上作为激动剂作用（EC50 = 190 nM），但在大鼠和小鼠的CB2受体上则表现为逆激动剂作用（EC50分别为216和463 nM）；对大鼠后肢热刺激引起的镇痛有显著作用；具有神经保护作用，能够在体外防止Gp120诱导的凋亡，并提高神经前体细胞的生存率和分化；当以每日10 mg/kg剂量给与GFAP/Gp120转基因小鼠时，能增加海马区的神经发生；在ALS小鼠模型中，能够延缓运动功能障碍的发生。A CB2 receptor agonist; selective for CB2 over CB1 (Kis = 7.1 and 580 nM); considered a protean agonist because it has neutral antagonist and partial agonist activity, depending on the assay utilized; acts in a species-dependent manner in vitro, acting as an agonist at human CB2 receptors (EC50 = 190 nM) but an inverse agonist at rat and mouse CB2 receptors (EC50s = 216 and 463 nM, respectively); produces antinociception to thermal stimuli in rat hindpaw; neuroprotective, preventing Gp120-induced apoptosis in vitro and increasing survival and differentiation of neural progenitor cells; increases hippocampal neurogenesis in GFAP/Gp120 transgenic mice when administered at a dose of 10 mg/kg daily for ten days; delays motor impairment in a murine model of ALS.