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Org-24461 is a small molecule inhibitor of glycine transporter type-1 (GlyT1), initially developed by Egis Gyógyszergyár for nervous system diseases, particularly targeting conditions such as schizophrenia. It inhibits glycine uptake at synaptic and non-synaptic sites, thereby modulating glutamatergic neurotransmission. Org-24461 has shown activity in preclinical models relevant to neuropsychiatric disorders but has not advanced to clinical approval due to toxic side effects and lack of advance beyond phase 0 or preclinical development. Its primary mechanism of action is selective GlyT1 inhibition, with no evidence for anxiolytic effects or behavioral side effects seen with antipsychotics[1][2][3][5].
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