An endogenous ligand of the brain sigma/PCP receptor antagonizes NMDA-induced neurotransmitter release.

Abstract:

:The present study provides evidence for the presence of an endogenous ligand for the phencyclidine (PCP) receptor of mammalian brain. Partially purified bovine hippocampal extracts potently and dose dependently inhibit binding to PCP receptors of [3H]N-(1-[2-thienyl]-cyclohexyl)piperidine (TCP), a highly potent and specific ligand of PCP receptors. In addition to demonstrating PCP-like binding properties, the partially purified extract mimics biological actions of PCP upon neurotransmitter release. HPLC fractions active in the [3]TCP binding assay, by contrast to fractions inactive in the binding assay, potently elicited stimulation of spontaneous acetylcholine and dopamine efflux and inhibited NMDA-stimulated release of acetylcholine and dopamine. The transmitter release assay provides validation of a PCP-like physiological activity exerted by bovine hippocampal extracts partially purified by HPLC.

journal_name

Brain Res

journal_title

Brain research

authors

Zukin SR,Zukin RS,Vale W,Rivier J,Nichtenhauser R,Snell LD,Johnson KM

doi

10.1016/0006-8993(87)91499-5

subject

Has Abstract

pub_date

1987-07-21 00:00:00

pages

84-9

issue

1

eissn

0006-8993

issn

1872-6240

pii

0006-8993(87)91499-5

journal_volume

416

pub_type

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