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用放射配体受体结合试验法,研究了新化合物三环哌酯与人大脑皮质M受体的结合特性,并与QNB作了比较。饱和实验结果显示,[3H]三环哌酯的结合参数与[3H]QNB相近,两种配体的作用均符合单位点模型。竞争性抑制实验结果表明二者作用强度相当。[3H]三环哌酯的结合和解离速率常数均较[3H]QNB大,且其与皮质M受体的解离受季铵酚的变构调节,结果提示,两种配体与M受体有一些不同的结合特性,在M受体研究中,[3H]三环哌酯可以作为[3H]QNB的补充工具
Radioligand receptor binding assay was used to study the binding properties of tricyclic piperazine ester to M receptor in human cerebral cortex and compared with QNB. The results of saturation experiments showed that the binding parameters of [3H] tricyclohexyl ester were similar to that of [3H] QNB. Both ligands were in agreement with the single site model. Competitive inhibition test results show that both the role of intensity. The binding and dissociation rate constants of [3H] tricyclohexyl ester are larger than that of [3H] QNB, and their dissociation with cortical M receptor is regulated by the allosteric action of quaternary ammonium. The results suggest that both ligands and M receptor There are some different binding properties of the [3H] tricyclohexyl ester as an additional tool for [3H] QNB in M receptor studies