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GLYX 13 C화학적 특성, 용도, 생산
용도
Rapastinel 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 active) 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%).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.
Biochem/physiol Actions
GLYX-13 is a glycine-site functional partial agonist (GFPA) selective modulator of the NMDA receptor (NMDAR). It is a brain penetrable tetrapeptide which acts as a positive allosteric modulator of the NMDA receptor, acting via the glycine site. GLYX-13 has been found to be a cognitive enhancer in learning models and is currently in clinical trials as an antidepressant.
