Pseudoallosteric modulation by (+)-MK801 of NMDA (N-methyl-D-aspartate)-coupled phencyclidine binding sites
- National Institutes of Health, Bethesda, MD (USA)
Two high affinity phencyclidine (PCP) binding sites, labeled by ({sup 3}H)1-(1-(2-thienyl)cyclohexyl)piperidine (({sup 3}H)TCP), have been identified in guinea pig brain, with one site coupled to the N-methyl-D-aspartate (NMDA) receptor (site 1) and the other site associated with the dopamine reuptake carrier complex (site 2). In this study, PCP enhanced the dissociation of ({sup 3}H)TCP from PCP site 1 and site 2, while (+){minus}MK801 only enhanced dissociation of ({sup 3}H)TCP from PCP site 1. Although additional studies will be required to determine the exact mechanism(s) of these effects, these data demonstrate that the interactions of PCP with both site 1 and site 2 are more complex than previously appreciated.
- OSTI ID:
- 6039091
- Journal Information:
- Life Sciences; (USA), Journal Name: Life Sciences; (USA) Vol. 47:16; ISSN 0024-3205; ISSN LIFSA
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
AMINES
ANIMALS
AZINES
BIOCHEMICAL REACTION KINETICS
BODY
BRAIN
CENTRAL NERVOUS SYSTEM
GUINEA PIGS
HETEROCYCLIC COMPOUNDS
HYDROGEN COMPOUNDS
ISOTOPE APPLICATIONS
KINETICS
LABELLING
MAMMALS
MEMBRANE PROTEINS
NERVOUS SYSTEM
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PIPERIDINES
PROTEINS
PYRIDINES
REACTION KINETICS
RECEPTORS
RODENTS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES