摘要
用［３Ｈ］ＭＫ８０１放射配体竟争结合法测定了（－），（＋）黄皮酰胺对大鼠前脑，海马，皮层等部位突触膜的ＮＭＤＡＲ的作用，以探讨其促智机制。同时用饱和实验分析ｐｏ给药１０ｄ后，小鼠脑内该受体密度的变化。结果表明：（－），（＋）黄皮酰胺对脑内各部位的ＮＭＤＡ受体均无特异亲和力。但（－）黄皮酰胺在体给药１０ｄ后能使小鼠脑内ＮＭＤＡ受体密度显著增高，并呈一定的量效关系。提示黄皮酰胺的药理作用有光学选择性；（－）黄皮酰胺增加脑内ＮＭＤＡ受体密度为其促智作用提供了重要理论依据。
Using radioligand binding assay, the effects of (-), (+) clausenamide on N methyl D asparate(NMDA) receptor were studied in synaptic membrane, hippocampus and cerebral cortex in rats. The Bmax and K D values of NMDA receptor in mouse brain were measured with Scatchard plot method. Results showed that there was no specific binding of (-), (+) clausenamide to NMDA receptor. However, higher Bmax values were observed in (-) clausenamide treated rats than the control group, but no effect on K D value. (+) Clausenamide treatment showed no effect on Bmax and K D values. The findings suggest that the pharmacologic actions of clausenamide depends on its chirality. Up regulation of NMDA receptor induced by (-) clausenamide is helpful to elucidate its nootropic mechanism.
出处
《药学学报》
CAS
CSCD
北大核心
1997年第4期259-263,共5页
Acta Pharmaceutica Sinica
