γ-氨基丁酸门控氯离子通道的通透性通过一种“笼形”惊厥剂——叔丁基双环磷[35S]硫代酸盐的结合来描述。
The permeability of gamma-aminobutyric acid-gated chloride channels is described by the binding of a "cage" convulsant, t-butylbicyclophosphoro[35S]thionate.
作者信息
Havoundjian H, Paul S M, Skolnick P
出版信息
Proc Natl Acad Sci U S A. 1986 Dec;83(23):9241-4. doi: 10.1073/pnas.83.23.9241.
The "cage" convulsant t-butylbicyclophosphoro[35S]thionate ([35S]TBPS) binds with high affinity to sites at or near a gamma-aminobutyric acid (GABA)-gated chloride channel according to current hypothesis. We now report that the potencies of a series of anions in enhancing [35S]TBPS binding correlated highly with their relative permeabilities through GABA-gated chloride channels. Furthermore, statistically significant correlations are obtained between the apparent affinity (Kd) of [35S]TBPS estimated in the presence of these anions and their relative permeabilities through GABA-gated chloride channels. The latter relationships obtained whether the Kd of [35S]TBPS as estimated in rat cerebral cortex was correlated with the relative permeabilities of these anions in either frog dorsal root ganglion cells or primary cultures of mouse spinal cord neurons. These findings strongly suggest that [35S]TBPS binds to GABA-gated chloride channels and that the apparent affinity of this radioligand is directly related to the permeability of these channels. Thus, radioreceptor techniques using [35S]TBPS may provide a simple means of describing permeability characteristics of GABA-gated chloride channels.
根据目前的假说，“笼形”惊厥剂叔丁基双环磷[35S]硫代酸盐（[35S]TBPS）与γ-氨基丁酸（GABA）门控氯离子通道处或其附近的位点具有高亲和力结合。我们现在报告，一系列阴离子增强[35S]TBPS结合的效力与其通过GABA门控氯离子通道的相对通透性高度相关。此外，在这些阴离子存在下估计的[35S]TBPS的表观亲和力（Kd）与其通过GABA门控氯离子通道的相对通透性之间获得了具有统计学意义的相关性。无论在大鼠大脑皮层中估计的[35S]TBPS的Kd与这些阴离子在青蛙背根神经节细胞或小鼠脊髓神经元原代培养物中的相对通透性是否相关，都能得到后一种关系。这些发现强烈表明[35S]TBPS与GABA门控氯离子通道结合，并且这种放射性配体的表观亲和力与这些通道的通透性直接相关。因此，使用[35S]TBPS的放射受体技术可能提供一种描述GABA门控氯离子通道通透性特征的简单方法。
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