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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- No. CAS: 138047-56-0
- Fòrmula: C21H25NO4
- Peso molecular:355.43
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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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No. CAS 138047-56-0
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Peso molecular 355.43
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CP-283097 Related Classifications
HY-116142 Related Classifications
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