Rapastinel, formerly known as GLYX-13 and BV-102, is a novel antidepressant drug approved as an adjunctive therapy for the treatment of treatment-resistant major depressive disorder. It is a centrally active, intravenously administered (non-orally bioavailable) amidated tetrapeptide (Thr-Pro-Pro-Thr-NH2) that acts as a selective, weak partial agonist (mixed antagonist/agonist) of an allosteric site at the glycine site of the NMDA receptor complex (Emax ≈ 25%).[1][2] The drug is a rapid-acting and long-lasting antidepressant as well as robust cognitive enhancer by virtue of its ability to both inhibit and enhance NMDA receptor-mediated signal transduction. References: Moskal JR, Burgdorf JS, Stanton PK, Kroes RA, Disterhoft JF, Burch RM, Amin Khan M. The Development of Rapastinel (Formerly GLYX-13); a rapid acting and long lasting antidepressant. Curr Neuropharmacol. 2016 Mar 21. [Epub ahead of print] PubMed PMID: 26997507.

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CAS：117928-94-6