Chemical Name:(E)-(±)-2-Amino-4-methyl-5-phosphono-3-pentenoic acid
ethyl ester
Biological Activity:
Potent,
selective and competitive NMDA antagonist (Ki = 310 nM for
inhibition of [3H]-CPP binding in rat brain). Centrally active upon
oral administration in vivo.
Fagget al
(1990) CGP 37849 and CGP 39551: novel and potent competitive
N-methyl-D-asparate receptor antagonists with oral activity. Br.J.Pharmacol. 99
791. Loscher and Honack (1991) Anticonvulsant and behavioural effects of
two novel competitive N-methyl-D-aspartic acid receptor antagonists, CGP 37849
and CGP 39551, in the kindling model of epilepsy. Comparison with MK-801 and
carbamazepine. J.Pharmacol.Exp.Ther. 256 432. D'Hoogeet
al (1999) Effects of competitive NMDA receptor antagonists on excitatory
amino-acid-evoked currents in mouse spinal cord. Fundam.Clin.Pharmacol. 13
67.
Displays 26-fold and > 440-fold selectivity over kainate and NMDA receptors respectively. Neuro-protective; delays neuronal death in a global ischaemia model and cerebral infarction in a focal ischaemia model.