CP-283097
CP-283097 is an orally active and conformationally restricted and NR2B subtype-selective NMDA antagonist. CP-283097 efficiently competitively inhibits the binding of [³H]CP-101,606 to the rat meninges, with an IC50 value of 18 nM. CP-283097 exhibits nearly complete inhibition of the current mediated by the NR2B receptor (IC50 = 206 nM), while the inhibitory effect on the NR2A or NR2C receptors is very weak. CP-283097 demonstrates excellent central nervous system permeability and in vivo efficacy in animal models. CP-283097 can be used for neurological diseases related to excessive activation of NMDA receptors.
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- CAS No.: 138047-56-0
- Formule: C21H25NO4
- Masse moléculaire:355.43
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
CP-283097 exhibits an IC50 of 4 nM for inhibiting the toxicity of glutamate-induced hippocampal neurons[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CP-283097 (1-15 mg/kg, i.v., single dose) inhibits the expression of c-Fos induced by NMDA with and ED50 of 4 mg/kg in mice[1].
CP-283097 (0.2-2 mg/kg, i.v., single dose) exhibits efficacy in inhibiting electrically induced cortical spreading depression (CSD) in the rat[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cortical spreading depression model established in rats[1]
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Dosage:0.2, 0.6 and 2 mg/kg bolus + 0.2, 0.6 and 2 mg/kg infusion
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Administration:Intravenous injection (i.v.), single dose
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Result:Dose-dependently inhibited CSD propagation.
Chemical Information
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CAS No. 138047-56-0
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Masse moléculaire 355.43
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Formule C21H25NO4
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SMILES
O[C@@H]1[C@H](N2CCC(O)(CC2)CC3=CC=CC=C3)COC4=CC(O)=CC=C41
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CP-283097 Related Classifications
HY-116142 Related Classifications
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