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Title: Cannabinoid receptor localization in brain

Abstract

(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.

Authors:
; ; ; ; ; ;  [1]
  1. (National Institute of Mental Health, Bethesda, MD (USA))
Publication Date:
OSTI Identifier:
7137999
Resource Type:
Journal Article
Resource Relation:
Journal Name: Proceedings of the National Academy of Sciences of the United States of America; (USA); Journal Volume: 87:5
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; MARIHUANA; RECEPTORS; CHEMICAL COMPOSITION; AUTORADIOGRAPHY; BIOCHEMICAL REACTION KINETICS; BIOLOGICAL LOCALIZATION; BRAIN; MICE; TRITIUM COMPOUNDS; ANIMALS; BODY; CENTRAL NERVOUS SYSTEM; HERBS; HYDROGEN COMPOUNDS; KINETICS; MAGNOLIOPHYTA; MAGNOLIOPSIDA; MAMMALS; MEMBRANE PROTEINS; NERVOUS SYSTEM; ORGANIC COMPOUNDS; ORGANS; PLANTS; PROTEINS; REACTION KINETICS; RODENTS; VERTEBRATES; 550201* - Biochemistry- Tracer Techniques

Citation Formats

Herkenham, M., Lynn, A.B., Little, M.D., Johnson, M.R., Melvin, L.S., de Costa, B.R., and Rice, K.C. Cannabinoid receptor localization in brain. United States: N. p., 1990. Web. doi:10.1073/pnas.87.5.1932.
Herkenham, M., Lynn, A.B., Little, M.D., Johnson, M.R., Melvin, L.S., de Costa, B.R., & Rice, K.C. Cannabinoid receptor localization in brain. United States. doi:10.1073/pnas.87.5.1932.
Herkenham, M., Lynn, A.B., Little, M.D., Johnson, M.R., Melvin, L.S., de Costa, B.R., and Rice, K.C. Thu . "Cannabinoid receptor localization in brain". United States. doi:10.1073/pnas.87.5.1932.
@article{osti_7137999,
title = {Cannabinoid receptor localization in brain},
author = {Herkenham, M. and Lynn, A.B. and Little, M.D. and Johnson, M.R. and Melvin, L.S. and de Costa, B.R. and Rice, K.C.},
abstractNote = {(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.},
doi = {10.1073/pnas.87.5.1932},
journal = {Proceedings of the National Academy of Sciences of the United States of America; (USA)},
number = ,
volume = 87:5,
place = {United States},
year = {Thu Mar 01 00:00:00 EST 1990},
month = {Thu Mar 01 00:00:00 EST 1990}
}
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