Interaction of gacyclidine enantiomers with 'non-NMDA' binding sites in the rat central nervous system.

Abstract Gacyclidine, a channel blocker of N -methyl- d -aspartate receptors (NMDAR), exhibits potent neuroprotective properties and a low self-neurotoxicity. Preventing its interaction with NMDARs we demonstrate, through the use of its enantiomers, that gacyclidine also interacts with other (‘non-NMDA’) binding sites. The autoradiographic study showed that these sites displayed a uniform specific binding in the forebrain and a more discrete distribution in the molecular layer of the cerebellum. The ‘non-NMDA’ binding sites could exert a modulatory control on glutamatergic neurotransmission.