Work

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

Year: 1979

Type: article

Abstract: [3H]Phencyclidine binds to synaptic membranes from rat brain in a saturable, reversible, and selective fashion, with a dissociation constant Kd of 0.25 microM 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 are able to 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 pharacological activities of these analogs as measured by the rotarod assay.

Source: Proceedings of the National Academy of Sciences

DOI: 10.1073/pnas.76.9.4678

Authors: J P Vincent, B Kartalovski, P Geneste, J M Kamenka, M Lazdunski

Institution: École Nationale Supérieure de Chimie de Montpellier

Language: English

Topic: Neuroscience and Neuropharmacology Research

Subfield: Cellular and Molecular Neuroscience

Field: Neuroscience

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

Funder: Centre National de la Recherche Scientifique