For research use only. Not for therapeutic Use.
NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes[1].
NP10679 (1-1000 nM) shows pH-dependently effects to GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively[2].
NP10679 shows functional inhibition to 5-HT2A, α adrenergic receptor-1A (α1A), H1-histamine receptor (H1) and hERG channel with IC50 values of 1.71, 0.154, 0.073 and 0.617 μM, respectively[2].
NP10679 shows Ki values of 2.29, 0.638, 1.92, 0.603, 1.92, 0.495, 3.09, 0.040 and 0.135 for 5-HT1D, 5-HT2A, 5-HT2B, α1A, α1B, α1D, α2C, H1 and serotonin transporter SERT[2].
NP10679 (2, 5 and 10 mg/kg; i.p., prior to transient ischemia) reduces infarct volumes of transient ischemia mice[2].
| Synonyms | 6-[(2R)-2-hydroxy-3-[4-[4-(trifluoromethyl)phenyl]piperazin-1-yl]propoxy]-3,4-dihydro-1H-quinolin-2-one |
| Molecular Formula | C23H26F3N3O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H26F3N3O3/c24-23(25,26)17-2-4-18(5-3-17)29-11-9-28(10-12-29)14-19(30)15-32-20-6-7-21-16(13-20)1-8-22(31)27-21/h2-7,13,19,30H,1,8-12,14-15H2,(H,27,31)/t19-/m1/s1 |
| InChIKey | QJKYLYXHWSCZQT-LJQANCHMSA-N |
| SMILES | C1CC(=O)NC2=C1C=C(C=C2)OCC(CN3CCN(CC3)C4=CC=C(C=C4)C(F)(F)F)O |
| Reference | [1]. Zaczek R, et al. Phase 1 Clinical Results for NP10679, a pH-sensitive GluN2B-selective N-methyl-d-aspartate Receptor Inhibitor. Clin Pharmacol Drug Dev. 2023 Jan 15. [2]. Myers SJ, et al. A Glutamate N-Methyl-d-Aspartate (NMDA) Receptor Subunit 2B-Selective Inhibitor of NMDA Receptor Function with Enhanced Potency at Acidic pH and Oral Bioavailability for Clinical Use. J Pharmacol Exp Ther. 2021 Oct;379(1):41-52. |
