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地西泮结合抑制剂(DBI):γ-氨基丁酸A(GABAA)受体功能内源性调节剂家族的前体。历史、观点及临床意义

DBI (diazepam binding inhibitor): the precursor of a family of endogenous modulators of GABAA receptor function. History, perspectives, and clinical implications.

作者信息

Barbaccia M L, Berkovich A, Guarneri P, Slobodyansky E

机构信息

Dept. of Experimental Medicine, Rome II University Medical School, Italy.

出版信息

Neurochem Res. 1990 Feb;15(2):161-8. doi: 10.1007/BF00972206.

Abstract

Biochemical, electrophysiological, and lately, molecular biological techniques have shown that GABAA receptors are heterogeneous supramolecular complexes and can be divided into at least three major subgroups: GABAA1, GABAA2, and GABAA3. They differ mainly in the structural and functional properties of the allosteric modulatory center associated with each one of them. This paper will review the present state of research based on the evidence that DBI (diazepam binding inhibitor) and its natural processing products can selectively modulate GABAergic transmission at different GABAA receptor subtypes. Furthermore, the possibility that the DBI family of peptides represents a novel and meaningful neurochemical correlate for neuropsychiatric pathology, sustained by an alteration of GABAergic transmission, will be discussed.

摘要

生化、电生理以及最近的分子生物学技术表明,GABAA受体是异质性超分子复合物,可至少分为三个主要亚组:GABAA1、GABAA2和GABAA3。它们的主要区别在于与各自相关的变构调节中心的结构和功能特性。本文将基于DBI(地西泮结合抑制剂)及其天然加工产物可在不同GABAA受体亚型上选择性调节GABA能传递这一证据,综述当前的研究现状。此外,还将讨论肽类DBI家族代表一种与神经精神病理学相关的新型且有意义的神经化学关联物的可能性,这种关联由GABA能传递的改变所支持。

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