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^[1]. In Vitro:CP-283097 exhibits an IC₅₀ of 4 nM for inhibiting the toxicity of glutamate-induced hippocampal neurons^[1]. In Vivo:CP-283097 (s.c; and p.o., single dose) inhibits the NMDA receptors in rats with ED₅₀s of 0.3 mg/kg and 1.2 mg/kg in Haloperidol (HY-14538)-induced catalepsy model^[1].
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].