GluN2B-NMDAR Allosteric modulator 1 is a selective GluN2B-NMDAR positive allosteric modulator. GluN2B-NMDAR Allosteric modulator 1 can increase glutamate- and aspartate-evoked GluN2B-NMDAR-gated currents with EC 50 values of 43.7 and 18 nM. GluN2B-NMDAR Allosteric modulator 1 can reverse anxiety-like behavior and social cognition deficits in mice. GluN2B-NMDAR Allosteric modulator 1 can be used for the research of neurological disease, such as anxiety [1].
In Vivo, GluN2B-NMDAR Allosteric modulator 1 (Compound 175) (1 mg/kg; i.p.; 30 min before the induction of synaptic plasticit) facilitates low-frequency stimulation-induced long-term depression via a GluN2B-containing NMDAR-dependent mechanism in anesthetized rats[1]. GluN2B-NMDAR Allosteric modulator 1 (1 mg/kg; i.p.; single dose) reverses anxiety-like behavior and social cognition deficits in 7-month-old Mecp2-OE mice and in a transgenic mouse line harboring an inducible expression of Disc1-N mice.[1].
In Vitro, GluN2B-NMDAR Allosteric modulator 1 (Compound 175) (0.001-100 μM) increases glutamate-evoked GluN1/GluN2B-NMDAR-gated currents in HEK293 cells with an EC50 of 43.7 nM (logEC50 = -7.36)[1]. GluN2B-NMDAR Allosteric modulator 1 (0.0001-1 μM) dose-dependently and selectively potentiates aspartate-evoked GluN2B-containing native NMDAR currents in primary rat hippocampal neurons with an EC50 of 18 nM[1]. GluN2B-NMDAR Allosteric modulator 1 (1 μM; 3 h) does not induce cytotoxicity in primary cortical neurons[1].
References:
[1]. Ge Y, et al. GluN2B-specific NMDAR positive allosteric modulation reverses cognitive and behavioral abnormalities in Mecp2 and Disc1 transgenic mice. Sci Adv. 2026 Jan 9;12(2):eady3891.
In Vivo, GluN2B-NMDAR Allosteric modulator 1 (Compound 175) (1 mg/kg; i.p.; 30 min before the induction of synaptic plasticit) facilitates low-frequency stimulation-induced long-term depression via a GluN2B-containing NMDAR-dependent mechanism in anesthetized rats[1]. GluN2B-NMDAR Allosteric modulator 1 (1 mg/kg; i.p.; single dose) reverses anxiety-like behavior and social cognition deficits in 7-month-old Mecp2-OE mice and in a transgenic mouse line harboring an inducible expression of Disc1-N mice.[1].
In Vitro, GluN2B-NMDAR Allosteric modulator 1 (Compound 175) (0.001-100 μM) increases glutamate-evoked GluN1/GluN2B-NMDAR-gated currents in HEK293 cells with an EC50 of 43.7 nM (logEC50 = -7.36)[1]. GluN2B-NMDAR Allosteric modulator 1 (0.0001-1 μM) dose-dependently and selectively potentiates aspartate-evoked GluN2B-containing native NMDAR currents in primary rat hippocampal neurons with an EC50 of 18 nM[1]. GluN2B-NMDAR Allosteric modulator 1 (1 μM; 3 h) does not induce cytotoxicity in primary cortical neurons[1].
References:
[1]. Ge Y, et al. GluN2B-specific NMDAR positive allosteric modulation reverses cognitive and behavioral abnormalities in Mecp2 and Disc1 transgenic mice. Sci Adv. 2026 Jan 9;12(2):eady3891.