Journal
EXPERT OPINION ON INVESTIGATIONAL DRUGS
Volume 23, Issue 2, Pages 243-254Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1517/13543784.2014.852536
Keywords
antidepressant; depression; glycine site; major depressive disorder; NMDA receptor; rapid-acting
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Funding
- Naurex, Inc.
- Naurex
- AgeneBio
- Nektar
- CoLucid
- Ralph and Marian Falk Medical Research Trust (Chicago, IL)
- NIH [MH094835]
- PK Stanton [NS044421]
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Introduction: The N-methyl-D-aspartate receptor-ionophore complex plays a key role in learning and memory and has efficacy in animals and humans with affective disorders. GLYX-13 is an N-methyl-D-aspartate receptor (NMDAR) glycine-site functional partial agonist and cognitive enhancer that also shows rapid antidepressant activity without psychotomimetic side effects. Areas covered: The authors review the mechanism of action of GLYX-13 that was investigated in preclinical studies and evaluated in clinical studies. Specifically, the authors review its pharmacology, pharmacokinetics, and drug safety that were demonstrated in clinical studies. Expert opinion: NMDAR full antagonists can produce rapid antidepressant effects in treatment-resistant subjects; however, they are often accompanied by psychotomimetic effects that make chronic use outside of a clinical trial inpatient setting problematic. GLYX-13 appears to exert its antidepressant effects in the frontal cortex via NMDAR-triggered synaptic plasticity. Understanding the mechanistic underpinning of GLYX-13's antidepressant action should provide both novel insights into the role of the glutamatergic system in depression and identify new targets for therapeutic development.
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