2,3-苯并二氮杂䓬与外周苯并二氮杂䓬受体的相互作用。

Interaction of 2,3-benzodiazepines with peripheral benzodiazepine receptors.

作者信息

Kenessey A, Gráf L, Páldi-Haris P, Láng T

出版信息

Pharmacol Res Commun. 1987 Jan;19(1):1-14. doi: 10.1016/0031-6989(87)90028-2.

Abstract

2,3-Benzodiazepines (BZs), such as tofizopam (TP) and GYKI-51 189 have anxiolytic potency accompanied by moderate sedative action, but no anticonvulsant and muscle relaxant activities. These compounds show relatively low affinity to the peripheral benzodiazepine (PBZ) receptors, nevertheless, they decrease the binding of (3H)Ro5-4864 to its receptors in heart, kidney and brain membranes. This diminution in the binding is due to a decrease in the affinity for the ligand (Kd) without any change in the maximal number of binding sites (Bmax). This interaction of 2,3-BZs with PBZ binding sites may explain their pharmacological profile.

摘要

2,3-苯并二氮䓬类药物（BZs），如托非索泮（TP）和GYKI-51 189具有抗焦虑效力并伴有中度镇静作用，但无抗惊厥和肌肉松弛活性。这些化合物对外周苯并二氮䓬（PBZ）受体显示出相对较低的亲和力，然而，它们会降低(3H)Ro5-4864与其在心脏、肾脏和脑膜中的受体的结合。这种结合的减少是由于对配体的亲和力（Kd）降低，而结合位点的最大数量（Bmax）没有任何变化。2,3-苯并二氮䓬类药物与PBZ结合位点的这种相互作用可能解释了它们的药理学特性。