1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. iGluR
  3. NMDA receptor modulator 9

NMDA receptor modulator 9 is an orally active NMDA receptor positive allosteric modulator (PAM). NMDA receptor modulator 9 enhances GluN2A receptor activity. NMDA receptor modulator 9 demonstrates significant antidepressant-like effects in chronic restraint stress (CRS)-induced depression mice. NMDA receptor modulator 9 can be used for the study of depression.

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NMDA receptor modulator 9

NMDA receptor modulator 9 Chemical Structure

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Description

NMDA receptor modulator 9 is an orally active NMDA receptor positive allosteric modulator (PAM). NMDA receptor modulator 9 enhances GluN2A receptor activity. NMDA receptor modulator 9 demonstrates significant antidepressant-like effects in chronic restraint stress (CRS)-induced depression mice. NMDA receptor modulator 9 can be used for the study of depression[1].

In Vitro

NMDA receptor modulator 9 (Compound Y36) (30 μM) significantly enhances GluN2A receptor-mediated currents only when coadministered with both glutamate and Glycine (HY-Y0966) in Xenopus oocytes expressing GluN1/GluN2A[1].
NMDA receptor modulator 9 shows higher efficacy (Emax = 397.7%) than GNE-3419 (Emax = 196.4%), reducing the EC50 values and increasing the Emax values for glutamate/Glycine at GluN2A receptor[1].
NMDA receptor modulator 9 (200 μM) exhibits no significant cytotoxicity in HEK293, PC12, and SH-SY5Y cell lines[1].
NMDA receptor modulator 9 exhibits weak affinity for the hERG channel with an IC50 of 67.85 μM, indicating low risk of cardiac toxicity[1].

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

In Vivo

NMDA receptor modulator 9 (Compound Y36) (0.1-1.0 mg/kg, i.p. or p.o., single dose) alleviates depression-related behaviors in chronic restraint stress (CRS) mice[1].
NMDA receptor modulator 9 (Compound Y36) (200-350 mg/kg, p.o., single dose) exhibits slow mortality with an LD50 of 270.82 mg/kg in male C57BL/6J mice[1].
NMDA receptor modulator 9 (0.3-1.0 mg/kg, i.p., every 2 days for 30 days) causes no abnormal behavior, stable body weight, no significant changes in organ/body weight ratios, and no obvious nephrotoxicity, hepatotoxicity or myocardial injury in ICR mice[1].

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

Animal Model: C57BL/6J mice (subjected to 4 h daily restraint stress for 28 days)[1]
Dosage: 0.1, 0.3, 1.0 mg/kg
Administration: i.p. or p.o.for a single dose
Result: Increased central area entries in OFT.
Reduced immobility time in TST.
Enhanced sucrose preference in SPT (alleviating anhedonia).
Molecular Weight

373.44

Formula

C19H20FN3O2S

SMILES

FC1=CC=C(C2(O)CCN(CC3=CC(N4C=C(SC4=N3)C)=O)CC2)C=C1

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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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.

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Product Name:
NMDA receptor modulator 9
Cat. No.:
HY-175508
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