Geissoschizine methyl etHER 是从钩藤中发现的一种生物碱,是 Yokukansan 的主要活性成分,具有精神药物作用。它是一种有效的 5-羟色胺 A 受体激动剂,是 Yokukansan 改善攻击性和社交性的候选药物。
产品描述
Geissoschizine methyl ether, a major indole alkaloid found in Uncaria hook, is a major active component of Yokukansan with psychotropic effects. Geissoschizine methyl ether is a potent serotonin A receptor agonist and candidate for amelioration of aggressiveness and sociality by yokukansan
体外活性
To find the candidate ingredients, we examined competitive binding assay and [(35)S] guanosine 5'-O-(3-thiotriphosphate) (GTPγS) binding assay of seven major alkaloids in UH using Chinese hamster ovary cells expressing 5-HT(1A) receptors artificially. Only Geissoschizine methyl ether (GM) among seven alkaloids potently bound to 5-HT(1A) receptors and acted as a partial agonist. This in vitro result on GM was further demonstrated in the socially isolated mice. As did YKS and UH, GM ameliorated the isolation-induced increased aggressiveness and decreased sociality, and the effect was counteracted by coadministration of WAY-100635[1]
Cas No.
60314-89-8
分子式
C22H26N2O3
分子量
366.45
别名
缝籽嗪甲醚;缝籽木嗪甲醚
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years