[甲苯磺丁脲与大鼠内分泌胰腺的非饱和协同结合。特异性标准]

[Non-saturable cooperative binding of tolbutamide to rat endocrine pancreas. Criteria of specificity].

作者信息

Alric R, Manteghetti M, Puech R, Lignon F, Loubatières A

出版信息

C R Acad Hebd Seances Acad Sci D. 1976 Jul 19;283(3):283-6.

Abstract

The binding of 3H-tolbutamide to isolated islets, which shows a cooperative non-saturable pattern up to about 5 X 10(-5) M, was confirmed. Binding to exocrine pancreatic tissue shows much less cooperativity. Among congeners of tolbutamide, unlabelled carbutamide and chlorpropamide in isodynamic concentrations, as well as diazoxide in an exactly antagonistic amount, behave like tolbutamide 5 X 10(-5) M itselt by cancelling cooperativity when added to the labelled drug. Glipizide and glibenclamide do not.

摘要

已证实，3H-甲苯磺丁脲与分离的胰岛结合，在约5×10⁻⁵ M以下呈现协同性非饱和模式。与胰腺外分泌组织的结合显示出的协同性要少得多。在甲苯磺丁脲的同系物中，等动力学浓度的未标记氨磺丁脲和氯磺丙脲，以及等量的完全拮抗的二氮嗪，当添加到标记药物中时，通过消除协同性，其作用类似于5×10⁻⁵ M的甲苯磺丁脲本身。格列吡嗪和格列本脲则不然。