Rislenemdaz, also known as CERC-301, inhibits calcium influx agonist-stimulated NMDA-GluN1a/GluN2B L(tk-) cells with an IC50 of 3.6 nM. Rislenemdaz is at least 1000-fold more selective for the GluN2B receptor compared to all targets tested, including hERG potassium channels. At 10 uM, Rislenemdaz is also minimally active against sigma-type receptors[1].
Rislenemdaz 动物研究
Animal study
At doses of 1, 3, 10 and 30 mg/kg, Rislenemdaz significantly reduced immobility frequency and significantly increased swimming behaviour. At the time of sampling, plasma levels of Rislenemdaz were approximately 15, 120, 390, 1,420, 4,700, and 14,110 nM, which corresponded to approximately 5, 29, 56, 83, 94, and 98% of the RO in rats, respectively. The LD50s for the increase in swimming frequency and the decrease in immobility were approximately 0.3 and 0.7 mg/kg, which corresponded to approximately 30% and 50% of the RO. Rislenemdaz (1, 3, 10 and 30 mg/kg) significantly increased the total swimming distance compared to the control group in a 60-min test[1].
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