某些N-（2-甲基或1,2-二甲基吲哚-3-基甲酰基）氨基酸衍生物对苯二氮䓬受体结合的特异性抑制作用。
Specific inhibition of benzodiazepine receptor binding by some N-(2-methyl or 1,2-dimethylindol-3-ylglyoxylyl)amino acid derivatives.
作者信息
Primofiore G, Marini A M, Da Settimo F, Salvadori C, Martini C, Lucacchini A, Giannaccini G
机构信息
Istituto di Chimica Farmaceutica dell'Università di Pisa, Italy.
出版信息
Farmaco. 1990 Mar;45(3):341-51.
Several N-(2-methyl or 1,2-dimethylindol-3-ylglyoxylyl)amino acid derivatives were synthesized and tested for their affinity for the benzodiazepine receptor in bovine cortical membranes. The 2-methyl derivatives showed a lower affinity than the unmethylated analogues, and the 1,2-dimethyl derivatives practically lacked any affinity for the benzodiazepine receptor. The importance of the indole N-H group is therefore evidenced for an optimal interaction of these ligands with receptor site.
合成了几种N-(2-甲基或1,2-二甲基吲哚-3-基乙二酰基)氨基酸衍生物，并测试了它们对牛脑皮层膜中苯二氮䓬受体的亲和力。2-甲基衍生物的亲和力低于未甲基化的类似物，而1,2-二甲基衍生物实际上对苯二氮䓬受体没有任何亲和力。因此，吲哚N-H基团对于这些配体与受体位点的最佳相互作用很重要。
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