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Synthesis of a novel water-soluble NMDA receptor antagonist

✍ Scribed by Takashi Masuko; Tadashi Kusama; Hiroki Nagaoka; Koichi Metori; Yasuo Kizawa; Muneharu Miyake

Publisher
Journal of Heterocyclic Chemistry
Year
2008
Tongue
English
Weight
382 KB
Volume
45
Category
Article
ISSN
0022-152X

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✦ Synopsis

Abstract

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A novel water‐soluble N‐methyl‐D‐aspartate (NMDA) receptor antagonist ATGDMAP 1 as synthesized and the effect of 1 on NMDA receptors was studied using voltage‐clamp recordings of recombinant NMDA receptors expressed in Xenopus oocytes. The compound 1 inhibited macroscopic currents in NR1/NR2A, NR1/NR2B, NR1/NR2C and NR1/NR2D receptor subtypes in oocytes voltage‐clamped at ‐70 mV. Mutant NR1/NR2B receptors containing NR1(T648A) or NR1(T648S) had very large holding currents when voltage‐clamped at ‐70 mV compared to that of wild‐type NMDA receptors, because these mutants generate constitutively open channels. ATGDMAP 1 and Mg^2+^, a channel blocker of the NMDA receptor, reduced the large holding currents needed for mutant NMDA receptors. These data indicate that ATGDMAP 1 directly acts on the channel pores of the NMDA receptor.

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