γ-氨基丁酸（GABA）和碘化甲基荷包牡丹碱预处理后GABA受体结合的动力学差异。

Kinetic differences in GABA receptor binding following GABA and bicuculline methiodide pretreatment.

作者信息

Maksay G, Ticku M K

出版信息

Neurosci Lett. 1984 Oct 12;51(2):219-24. doi: 10.1016/0304-3940(84)90554-8.

Abstract

The kinetics of [3H]GABA binding were studied in cortical membranes following GABA and bicuculline methiodide (BCM) pretreatment at 37 degrees C. The slower parts of the biphasic ON and OFF rates can be attributed to the high affinity sites. BCM pretreatment decreased the ON and OFF rates of [3H]GABA binding, including the rapid initial ON- and OFF-phases. Decreased association rates of GABA were independent of GABA and concentration and suggested a rate determining dissociation of bound BCM (t1/2 = 35 min).

摘要

在37摄氏度下，对经γ-氨基丁酸（GABA）和甲磺酸荷包牡丹碱（BCM）预处理后的皮质膜中[3H]GABA结合动力学进行了研究。双相开启和关闭速率的较慢部分可归因于高亲和力位点。BCM预处理降低了[3H]GABA结合的开启和关闭速率，包括快速的初始开启和关闭阶段。GABA结合速率的降低与GABA及其浓度无关，提示结合的BCM解离速率决定了整体速率（半衰期=35分钟）。