2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. GluN2B-NMDAR Allosteric modulator 1

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 EC50 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.

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GluN2B-NMDAR Allosteric modulator 1

GluN2B-NMDAR Allosteric modulator 1 Chemical Structure

CAS No. : 2419700-58-4

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Description

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 EC50 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].

IC50 & Target[1]

GluN2B

 

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GluN2B-NMDAR Allosteric modulator 1 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mecp2-OE mice (7 months old); a transgenic mouse line harboring an inducible expression of Disc1-N mice (C57BL/6; 3-4 months old) [1]
Dosage: 1 mg/kg
Administration: I.p.; single dose (30 minutes before each behavioral test)
Result: Restored center time in the open-field test to WT levels (reversing anxiety-like behavior) and significantly improved social preference index in Mecp2-OE mice.
Increased time spent in the center of the open-field test (reversing anxiety-like behavior), increased spontaneous alternation in the Y-maze test (improving spatial working memory) and increased social preference index in the three-chamber test (reversing sociability deficit) in Disc1-N mice.
Molecular Weight

295.38

Formula

C17H21N5
CAS No.
SMILES

CC(N1C=CN=C1CNCC2=CC=C(N3C=CN=C3)C=C2)C
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Purity & Documentation
References
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GluN2B-NMDAR Allosteric modulator 1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GluN2B-NMDAR Allosteric modulator 12419700-58-4iGluRIonotropic glutamate receptorsGluN2BNMDARsGluN2Dlong-term depressionInhibitorinhibitorinhibit

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