GLUTATHIONE RECEPTOR PROBES FOR CNS STUDIES

现在有初步证据表明，谷胱甘肽(GSH)作为一种 哺乳动物中枢神经系统中的神经递质。装订 用放射性标记的谷胱甘肽测定了受体位置的常数。 突触膜和培养的星形胶质细胞上。有证据表明 GSH受体在其他各种中枢神经系统结构中也有分布。我们建议 合成研究这些受体部位的GSH荧光探针 并与放射性标记的GSH竞争测定其结合常数。 将使用具有合适结合常数的荧光标记探针 研究中枢神经系统和其他外周的结合部位分布 并检测培养细胞中第二信使(IP3)的激活 星形胶质细胞。不同GSM官能团上的荧光标记将 也有助于阐明GSM受体位点的性质。

Preliminary evidence now exists that glutathione (GSH) acts as a neurotransmitter in the mammalian central nervous systems. Binding constants for receptor sites have been measured using radiolabeled GSH on synaptic membranes and on cultured astrocyte cells. There is evidence for GSH receptor sites in various other CNS structures as well. We propose to synthesize fluorescent GSH probes for the study of these receptor sites and measure their binding constants in competition with radiolabeled GSH. Fluorescence labeled probes with suitable binding constants will be used to study the distribution of binding sites in the CNS and other peripheral tissues and to examine second messenger (IP3) activation in cultured astrocytes. Fluorescent labeling on different GSM functional groups will also help elucidate the nature of the GSM receptor site.