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Description: GNE 5729 is a novel, potent, brain permeable positive allosteric modulator (PAM) and GluN2A subunit-selective of NMDAR with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 uM for GluN2C and GluN2D, respectively. The N-methyl-d-aspartate receptor (NMDAR) is an ionotropic glutamate receptor, gated by the endogenous coagonists glutamate and glycine, permeable to Ca2+ and Na+. NMDAR dysfunction is associated with numerous neurological and psychiatric disorders, including schizophrenia, depression, and Alzheimer's disease. GNE-0723 is a and brain-penetrant positive allosteric modulatorof NMDARs.
References: ACS Med Chem Lett. 2016 Oct 31; 8(1):84-89.
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