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硫酸孕烯醇酮:N-甲基-D-天冬氨酸受体的正变构调节剂。

Pregnenolone sulfate: a positive allosteric modulator at the N-methyl-D-aspartate receptor.

作者信息

Wu F S, Gibbs T T, Farb D H

机构信息

Department of Pharmacology and Experimental Therapeutics, Boston University School of Medicine, Massachusetts 02118.

出版信息

Mol Pharmacol. 1991 Sep;40(3):333-6.

PMID:1654510
Abstract

The N-methyl-D-aspartate (NMDA) receptor is believed to play a major role in learning and in excitotoxic neuronal damage associated with stroke and epilepsy. Pregnenolone sulfate, a neurosteroid, specifically enhances NMDA-gated currents in spinal cord neurons, while inhibiting receptors for the inhibitory amino acids glycine and gamma-aminobutyric acid, as well as non-NMDA glutamate receptors. This observation is consistent with the hypothesis that neurosteroids such as pregnenolone sulfate are involved in regulating the balance between excitation and inhibition in the central nervous system.

摘要

N-甲基-D-天冬氨酸(NMDA)受体被认为在学习以及与中风和癫痫相关的兴奋性毒性神经元损伤中起主要作用。硫酸孕烯醇酮是一种神经甾体,它能特异性增强脊髓神经元中NMDA门控电流,同时抑制抑制性氨基酸甘氨酸和γ-氨基丁酸的受体以及非NMDA谷氨酸受体。这一观察结果与如下假设一致,即硫酸孕烯醇酮等神经甾体参与调节中枢神经系统中兴奋与抑制之间的平衡。

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