Drug intelligence / Profile preview

CGP 37849

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous, Intraperitoneal
01

Overview

CGP 37849 is a synthetic, highly potent, selective, and competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor, specifically inhibiting the NMDA receptor channel function with a Ki of approximately 35 nM. Developed as a phosphono-amino acid derivative, it is orally bioavailable and has shown significant central nervous system effects in animal models, notably including anticonvulsant activity after oral and parenteral administration. CGP 37849 has been studied primarily as a tool for elucidating the physiological and pathological roles of NMDA receptors, which are critical for synaptic plasticity, learning, memory, and the mediation of glutamate excitotoxicity. It has been evaluated in models of epilepsy, ischemic brain damage, and anxiety. The drug was originally developed at CIBA-GEIGY (now part of Novartis)[1][3][4][7][8].

Other names
dl-2-amino-4-methyl-5-phosphono-3-pentenoic aciddl2-amino-4-methyl-5-phosphono-3-pentenoic aciddl 2-amino-4-methyl-5-phosphono-3-pentenoic acid(E)-2-amino-4-methyl-5-phosphonopent-3-enoic acid(E)-(±)-2-amino-4-methyl-5-phosphono-3-pentenoic acid3-pentenoic acid, 2-amino-4-methyl-5-phosphono-(3E)-
02

Targets

N-methyl-D-aspartate receptor glutamate binding site

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