Org 24598

Org 24598 is a potent and highly selective small molecule inhibitor of the glial glycine transporter GlyT1 (specifically GlyT1b, with IC50 = 6.9 nM). It displays negligible activity on GlyT2 and other monoaminergic systems, including adrenoreceptors, dopamine, 5HT receptors, and noradrenaline, dopamine, 5HT and GABA transporters. In preclinical studies, Org 24598 has demonstrated efficacy in modulating glycine neurotransmission and enhancing NMDA receptor function. It has been shown to improve cognitive flexibility and memory deficits following binge-like ethanol exposure and to reduce alcohol intake in animal models, likely through increased glycine receptor neurotransmission. Org 24598 has also inhibited the reacquisition of cocaine self-administration in preclinical addiction models, suggesting potential utility in substance use disorders and cognitive dysfunction. Its chemical structure is N-Methyl-N-[(3R)-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propyl]-glycine, and it is available as the lithium salt for research use[1][3][5][7][8][9].

Other names

R-(−)-N-Methyl-N-[3-[(4-trifluoromethyl)phenoxy]-3-phenyl-propyl]glycineOrg-24598 lithium saltOrg24598 lithium saltOrg 24598 lithium saltN-Methyl-N-[(3R)-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propyl]-glycine