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[Structure of glutamate receptor ion channels and mechanisms of their blockade by organic cations].

作者信息

Magazanik L G, Tikhonov D B, Bol'shakov K B, Gmiro V E, Buldakova S L, Samoĭlova M V

机构信息

M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Acad. Sci., 194223, St. Petersburg, pr. M. Toreza, 44, Russia.

出版信息

Ross Fiziol Zh Im I M Sechenova. 2001 Aug;87(8):1026-39.

PMID:11601147
Abstract

Structural determinants of blocking the glutamate receptors of AMPA and NMDA subtypes, were studied. Close location of hydrophobic and ammonium groups is necessary for affective blocking of the NMDA receptor channels, whereas blockers of the AMPA receptor channels have a distance of about 10 angstroms between these two groups. Models of the channels meeting these topographic data have been devised using a molecular mechanics approach. The accomplished studies revealed molecular basis of channel blockade of the NMDA and AMPA receptors. This may allow designing predictable new blocking compounds with a desired selectivity.

摘要

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Studies of the roles of NMDA and AMPA glutamate receptors in the mechanism of corasole convulsions in mice.N-甲基-D-天冬氨酸(NMDA)和α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)谷氨酸受体在小鼠可拉佐惊厥机制中的作用研究。
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