VU0240391

VU0240391 is a small molecule inhibitor of the glycine transporter 1 (GlyT1), developed through a scaffold-hopping approach to merge features from Merck and Pfizer's piperidine-derived GlyT1 inhibitors and generate a novel [3.1.0]-based N-methylimidazole sulfonamide scaffold. VU0240391 demonstrates high potency and selectivity for GlyT1, exhibits robust pharmacokinetic properties (including significant CNS penetration), and shows *in vitro* and *in vivo* efficacy comparable to advanced GlyT1 inhibitors. It has been primarily studied as a research tool and potential therapeutic for neuropsychiatric conditions such as schizophrenia, for which GlyT1 inhibition may modulate glutamatergic neurotransmission and address cognitive and negative symptoms[1][4].

Other names

12d