Phencyclidine and related drugs bind to the activated N-methyl-D-aspartate receptor-channel complex in rat brain membranes.
Neuroscience Letters May 6, 1987 G E Fagg
Phencyclidine (PCP) and similar drugs block NMDA-type glutamate receptors. In rat brain postsynaptic densities, binding of a PCP analogue was enhanced nearly 4-fold by the excitatory amino acids L-glutamate and NMDA, but not by other related compounds. Excitatory amino acid agonists and antagonists showed potencies in the PCP analogue binding assay that matched their affinities for NMDA-sensitive glutamate binding sites. Dissociative anesthetics and sigma-opiates inhibited PCP analogue binding but did not affect glutamate binding. The data indicate that PCP binding sites are linked to NMDA receptors, and that PCP and related drugs bind preferentially to the activated configuration of the NMDA receptor channel complex.