(R)-CPP

Description

(R)-CPP is an NMDA receptor antagonist (K_i = 0.14 μM). It binds to NMDA receptors containing GluN2A, GluN2B, GluN2C, and GluN2D subunits with K_i values of 0.04, 0.3, 0.6, and 2 μM, respectively. It inhibits depolarization induced by NMDA in isolated hemisected frog spinal cord (pA₂ = 6.56) and NMDA-induced sodium efflux from rat brain slices (pA₂ = 6.2). (R)-CPP inhibits the clonic phase of sound-induced seizures in DBA/2 mice (ED₅₀ = 65.8 μmol/kg) and the myoclonic phase of stroboscopic-induced seizures in P. papio photosensitive baboons (ED₅₀ = 127 μmol/kg).

Uses

(R)-CPP is a piperazine derivative demonstrating highly potent NMDA receptor antagonism.

Biological Activity

Highly potent NMDA antagonist; more active isomer. Shows some selectivity for NR2A-containing receptors (K i values are 0.041, 0.27, 0.63 and 1.99 μ M for inhibition of NR2A-, NR2B-, NR2C- and NR2D-containing recombinant NMDA receptors respectively).

storage

Room temperature (desiccate)