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海人酸受体的选择性激动剂和拮抗剂。

Selective agonists and antagonists for kainate receptors.

作者信息

Conti Paola, De Amici Marco, De Micheli Carlo

机构信息

Istituto di Chimica Farmaceutica e Tossicologica, Viale Abruzzi 42, Milano, 20131, Italy.

出版信息

Mini Rev Med Chem. 2002 Apr;2(2):177-84. doi: 10.2174/1389557024605456.

Abstract

Kainate receptors have only recently been characterized both from the pharmacological and biological point of view. Due to the limited number of truly kainate selective ligands, most of the known agonists and antagonists are generally classified as AMPA/kainate receptors ligands. The increasing interest in the search for selective kainate ligands aims at understanding the physiological role played by these receptors and finding out potential therapeutic approaches for the treatment of a number of neurological pathologies, i.e. schizophrenia, as well as acute and chronic neurodegenerative diseases, i.e. epilepsy, cerebral ischaemia, Parkinson's and Alzheimer's diseases. This review will focus on the recently discovered ligands for kainate receptors, with a particular attention given to those molecules displaying a selectivity for the different subunits of the kainate receptors and, on the other hand, to the role played by these receptor subtypes in the pathophysiology of the central nervous system.

摘要

直到最近,才从药理学和生物学角度对海人藻酸受体进行了表征。由于真正具有海人藻酸选择性的配体数量有限,大多数已知的激动剂和拮抗剂通常被归类为AMPA/海人藻酸受体配体。对寻找选择性海人藻酸配体的兴趣日益浓厚,旨在了解这些受体所发挥的生理作用,并找出治疗多种神经病理学疾病(如精神分裂症)以及急慢性神经退行性疾病(如癫痫、脑缺血、帕金森病和阿尔茨海默病)的潜在治疗方法。本综述将聚焦于最近发现的海人藻酸受体配体,特别关注那些对海人藻酸受体不同亚基具有选择性的分子,另一方面,关注这些受体亚型在中枢神经系统病理生理学中所起的作用。

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