NAB-14

• CAT Number: I032983
• CAS Number: 1237541-73-9
• Molecular Formula: C20H21N3O3
• Molecular Weight: 351.40
• Purity: ≥95%
• Synonyms: [4-(1H-indol-7-ylcarbamoyl)phenyl] N,N-diethylcarbamate
• InChI: InChI=1S/C20H21N3O3/c1-3-23(4-2)20(25)26-16-10-8-15(9-11-16)19(24)22-17-7-5-6-14-12-13-21-18(14)17/h5-13,21H,3-4H2,1-2H3,(H,22,24)
• InChIKey: WCGIKJOMEYPSIP-UHFFFAOYSA-N
• SMILES: CCN(CC)C(=O)OC1=CC=C(C=C1)C(=O)NC2=CC=CC3=C2NC=C3

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].
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].
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].

Reference

[1]. Swanger SA, et al. A Novel Negative Allosteric Modulator Selective for GluN2C/2D-Containing NMDA Receptors Inhibits Synaptic Transmission in Hippocampal Interneurons. ACS Chem Neurosci. 2018 Feb 21;9(2):306-319.
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