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脊髓中两种苯二氮䓬结合位点的特性

Properties of two benzodiazepine binding sites in spinal cord.

作者信息

Del Zompo M, Post R M, Tallman J F

出版信息

Neuropharmacology. 1983 Jan;22(1):115-8. doi: 10.1016/0028-3908(83)90269-1.

Abstract

Two types of benzodiazepine receptors were demonstrated in spinal cord. Binding to one of these sites (neuronal) was sensitive to the centrally active benzodiazepine, clonazepam, and binding was enhanced both by chloride and GABA. The second site was sensitive to 7-chloro-1,3-dihydro-1-methyl-5-(p-chlorophenyl) 2H-1,4-benzodiazepine-2-one (R05-4864) and thus is similar to the site characteristic of non-neuronal tissue. Binding to the neuronal site was inhibited by the putative glycine antagonist, strychnine, both in spinal cord and brain. This inhibition may account for the reported anti-GABAergic properties of strychnine and does not appear to be related to the glycine receptor.

摘要

在脊髓中发现了两种类型的苯二氮䓬受体。与其中一个位点(神经元位点)的结合对中枢活性苯二氮䓬氯硝西泮敏感,并且氯化物和γ-氨基丁酸(GABA)均可增强这种结合。第二个位点对7-氯-1,3-二氢-1-甲基-5-(对氯苯基)-2H-1,4-苯并二氮杂䓬-2-酮(R05-4864)敏感,因此类似于非神经元组织的位点特征。在脊髓和大脑中,假定的甘氨酸拮抗剂士的宁均可抑制与神经元位点的结合。这种抑制作用可能解释了士的宁所报道的抗GABA能特性,并且似乎与甘氨酸受体无关。

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