143154-08-9Relevant academic research and scientific papers
Potent Quinoxaline-Spaced Phosphono α-Amino Acids of the AP-6 Type as Competitive NMDA Antagonists: Synthesis and Biological Evaluation
Baudy, Reinhardt B.,Greenblatt, Lynne P.,Jirkovsky, Ivo L.,Conklin, Mary,Russo, Ralph J.,et al.
, p. 331 - 342 (2007/10/02)
A series of α-amino-3-(phosphonoalkyl)-2-quinoxalinepropanoic acids was synthesized and evaluated for NMDA receptor affinity using a CPP binding assay.Functional antagonism of the NMDA receptor complex was evaluated in vitro using a stimulated TCP binding assay and in vivo by empolying an NMDA-induced seizure model.Some analogues also were evaluated in the -glycine binding assay.Several compounds of the AP-6 type show potent and selective NMDA antagonistic activity both in vitro and in vivo.In particular α-amino-7-chloro-3-(phosphonomethyl)-2-quinoxalinepropanoic acid (1) d isplayed an ED50 of 1.1 mg/kg ip in the NMDA lethality model.Noteworthy is α-amino-6,7-dichloro-3-(phosphonomethyl)-2-quinoxalinepropanoic acid (3) with a unique dual activity, displaying in the NMDA receptor binding assay an IC50 of 3.4 nM and in the glycine binding assay an IC50 of 0.61 μM.
QUINOXALINE PHOSPHONO-AMINO ACIDS
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, (2008/06/13)
The compounds of the formula: STR1 in which Q is the quinoxaline nucleus; m is one of the integers 0, 1 or 2; n is one of the integers 1,2 or 3; or a pharmaceutically acceptable salt, alkyl ester or STR2 where R. sup.3 and R 4 are, independently, hydrogen, nitro, halo or methoxy, are NMDA antagonists useful in the treatment and prevention of central nervous system related pathological conditions resulting from overstimulation by excitatory amino acids.
