Bioactivity | Rapastinel acetate (GLYX-13 acetate) is an N-methyl-D-aspartate (NMDA) receptor modulator with long-acting antidepressant activity. Rapastinel acetate exerts its antidepressant effects by enhancing long-term potentiation (LTP) of synaptic transmission. Rapastinel acetate transiently enhances NMDAR-mediated currents in pyramidal neurons in the hippocampus and medial prefrontal cortex by binding to unique sites on the NMDAR complex. Rapastinel acetate significantly enhanced NMDAR-mediated currents at a concentration of 1 μmol/l and significantly reduced the currents at a concentration of 10 μmol/l. The mechanism of action of Rapastinel acetate is related to the reduction of affinity to intracellular calcium inactivation sites, which provides a theoretical basis for enhancing conductance mediated by NMDAR[1]. |
CAS | 491872-39-0 |
Formula | C20H35N5O8 |
Molar Mass | 473.52 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Burgdorf J, et al. The long-lasting antidepressant effects of rapastinel (GLYX-13) are associated with a metaplasticity process in the medial prefrontal cortex and hippocampus. Neuroscience. 2015 Nov 12;308:202-11. [2]. Extracellular application of the N-methyl-D-aspartate receptor allosteric modulator rapastinel acts remotely to regulate Ca2+ inactivation at an intracellular locus |