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New, potent kainate derivatives: comparison of their affinity for [3H]kainate and [3H]AMPA binding sites.

作者信息

Kwak S, Aizawa H, Ishida M, Shinozaki H

机构信息

National Institute of Neuroscience, National Center of Neurology and Psychiatry, Tokyo, Japan.

出版信息

Neurosci Lett. 1992 May 11;139(1):114-7. doi: 10.1016/0304-3940(92)90870-d.

DOI:10.1016/0304-3940(92)90870-d
PMID:1341901
Abstract

Newly synthesized kainate derivatives, 4-(2-hydroxyphenyl)-2-carboxy-3-pyrrolidineacetic acid (HFPA and 4-(2-methoxyphenyl)-2-carboxy-3-pyrrolidineacetic acid (MFPA), were potent inhibitors of [3H]kainate binding to the rat spinal cord synaptic membranes, comparable in their effectiveness to kainate and domoate, whereas acromelic acid A (ACRO-A) and B (ACRO-B) was much less effective than kainate. ACRO-A, MFPA and HFPA all inhibited [3H]AMPA binding. These novel kainate analogues provide new pharmacological tools for analyzing the mechanisms underlying activation of kainate/AMPA receptors.

摘要

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