Uses
Treatment of stroke (N-methylD-aspartate NMDA receptor antagonist).
Definition
ChEBI: 3-(3-anilino-3-oxoprop-1-enyl)-4,6-dichloro-1H-indole-2-carboxylic acid is an indolyl carboxylic acid.
Biological Activity
Highly potent and selective non-competitive antagonist acting at the strychnine-insensitive glycine binding site of the NMDA receptor-channel complex (K d = 0.8 nM). Displays > 1000-fold selectivity over NMDA, AMPA and kainate binding sites. Orally bioavailable and active in vivo .
Safety Profile
A poison by
intravenous route. When heated to
decomposition it emits toxic vapors of NOx
and Cl-.