Cannabinoid receptor localization in brain

Journal Article · Wed Feb 28 23:00:00 EST 1990 · Proceedings of the National Academy of Sciences of the United States of America; (USA)

DOI:https://doi.org/10.1073/pnas.87.5.1932· OSTI ID:7137999

Herkenham, M; Lynn, A B; Little, M D; Johnson, M R; Melvin, L S; de Costa, B R; Rice, K C ^[1]

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1. National Institute of Mental Health, Bethesda, MD (USA)

(3H)CP 55,940, a radiolabeled synthetic cannabinoid, which is 10-100 times more potent in vivo than delta 9-tetrahydrocannabinol, was used to characterize and localize a specific cannabinoid receptor in brain sections. The potencies of a series of natural and synthetic cannabinoids as competitors of (3H)CP 55,940 binding correlated closely with their relative potencies in several biological assays, suggesting that the receptor characterized in our in vitro assay is the same receptor that mediates behavioral and pharmacological effects of cannabinoids, including human subjective experience. Autoradiography of cannabinoid receptors in brain sections from several mammalian species, including human, reveals a unique and conserved distribution; binding is most dense in outflow nuclei of the basal ganglia--the substantia nigra pars reticulata and globus pallidus--and in the hippocampus and cerebellum. Generally high densities in forebrain and cerebellum implicate roles for cannabinoids in cognition and movement. Sparse densities in lower brainstem areas controlling cardiovascular and respiratory functions may explain why high doses of delta 9-tetrahydrocannabinol are not lethal.

• OSTI ID: 7137999
• Journal Information: Proceedings of the National Academy of Sciences of the United States of America; (USA), Journal Name: Proceedings of the National Academy of Sciences of the United States of America; (USA) Vol. 87:5; ISSN PNASA; ISSN 0027-8424
• Country of Publication: United States
• Language: English

Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ANIMALS
AUTORADIOGRAPHY
BIOCHEMICAL REACTION KINETICS
BIOLOGICAL LOCALIZATION
BODY
BRAIN
CENTRAL NERVOUS SYSTEM
CHEMICAL COMPOSITION
HERBS
HYDROGEN COMPOUNDS
KINETICS
MAGNOLIOPHYTA
MAGNOLIOPSIDA
MAMMALS
MARIHUANA
MEMBRANE PROTEINS
MICE
NERVOUS SYSTEM
ORGANIC COMPOUNDS
ORGANS
PLANTS
PROTEINS
REACTION KINETICS
RECEPTORS
RODENTS
TRITIUM COMPOUNDS
VERTEBRATES