GW-468816

GW-468816 is a small molecule glycine site antagonist of the N-methyl-D-aspartate (NMDA) receptor. It was developed to aid abstinence in individuals who have recently quit smoking by delaying relapse. The drug acts by modulating glutamatergic neurotransmission through antagonism at the glycine binding site of NMDA receptors. Preclinical studies suggested efficacy in reducing nicotine-cue and nicotine-induced reinstatement of drug use after abstinence without significant motor side effects. Clinical trials investigated its potential for preventing relapse in recently abstinent smokers; however, results did not demonstrate significant benefit over placebo. The compound was initially developed by GSK[1][2][4][5][6].

Other names

2-quinolinecarboxylic acid, 7-chloro-1,2,3,4-tetrahydro-4-(2-oxo-1-phenyl-3-pyrrolidinylidene)-, (2R,4E)-