NAB-14

NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC₅₀ of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier^[1]. IC50 & Target: GluN2C/GluN2Dr^[1] In Vitro: NAB-14 (compound 14) shows inhibition with IC₅₀s of 15 µM and 5.1 µM for GluN1/2AC1/2CC2 and GluN1/2AC1/2CC2 receptors, respectively^[1].
NAB-14 (20 µM; 24 h) inhibits native GluN2D-containing receptors in brain slices with no effect on native GluN2A- or GluN2B-containing NMDARs in cultures cortical neurons^[1].
NAB-14 (10 µM) reduces the peak amplitude of evoked EPSCs to 55 ± 3.0%, and significantly reduced the τW of EPSC deactivation^[1].
NAB-14 (10 µM) decreases the peak amplitude and charge transfer of interneuron EPSCs to 59 ± 9.9% and 63 ± 9.7%, respectively. And NAB-14 decreases τW for interneuron EPSCs from 150 ± 12 ms to 101 ± 14 ms^[1]. In Vivo: NAB-14 (20 mg/kg; p.o.) shows high systemic exposure with peak brain free of 3.2 and 3.8 nM for mouse and rat, respectively^[1].