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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- Formel: C19H20FN3O2S
- Molecular Weight:373.44
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
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.
Parmacokinetics
| Species | Dose | Route | Note | Cmax | Tmax | T1/2 | AUC0-t | MRT0-t | F | CL | Vss |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 12 mg/kg | p.o. | / | 3242.61 ng/mL | 0.25 h | 0.89 h | 3946.98 ng·h/mL | 1.16 h | 70.67 % | / | / |
| Mice[1] | 4 mg/kg | i.v. | / | 1567.97 ng/mL | 0.083 h | 0.72 h | 1861.57 ng·h/mL | 0.90 h | / | 35.36 mL/min/kg | 2.08 L/kg |
| Mice[1] | 8 mg/kg | i.p. | plasma | 1430.44 ng/mL | 0.333 h | 1.15 h | 1986.59 ng·h/mL | 1.11 h | / | / | / |
| Mice[1] | 8 mg/kg | i.p. | brain | 5129.81 ng/mL | 0.25 h | 0.90 h | 4926.40 ng·h/mL | 0.93 h | / | / | / |
In Vivo
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.
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Animal Model:C57BL/6J mice (subjected to 4 h daily restraint stress for 28 days)[1]
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Dosage:0.1, 0.3, 1.0 mg/kg
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Administration:i.p. or p.o.for a single dose
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Result:Increased central area entries in OFT.
Reduced immobility time in TST.
Enhanced sucrose preference in SPT (alleviating anhedonia).
Chemical Information
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Molecular Weight 373.44
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Formel C19H20FN3O2S
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SMILES
FC1=CC=C(C2(O)CCN(CC3=CC(N4C=C(SC4=N3)C)=O)CC2)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
NMDA receptor modulator 9 Related Classifications
HY-175508 Related Classifications
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