Interaction of phencyclidine ("angel dust") with a specific receptor in rat brain membranes.

Publisher Website
Google Scholar
Abstract
[3H]Phencyclidine a major drug of abuse which causes prolonged psychosis, binds to synaptic membranes from rat brain in a saturable, reversible and selective fashion, with a Kd of 0.25 .mu.M and a maximal binding capacity of 2.4 pmol/mg of membrane protein, i.e., 250 pmol/g of brain. The binding activity is concentrated in synaptosomal fractions, is higher in cerebral cortex and corpus striatum than in other parts of the rat brain and is not detectable in the spinal cord. Only molecules of the phencyclidine series and ketamine bind to the phencyclidine receptor. [3H]Phencyclidine bound to its receptor is not displaced by the classical neurotransmitters or neuromodulators. There is a good correlation between the apparent affinities of a series of phencyclidine analogs for the phencyclidine receptor and the pharmacological activities of the analogs as measured by the rotarod assay.