Cannabinoid receptor localization in brain
TLDR
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 the in vitro assay is the same receptor that mediates behavioral and pharmacological effects of cannabinoids, including human subjective experience.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.read more
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Altered CB1 receptor and endocannabinoid levels precede motor symptom onset in a transgenic mouse model of Huntington's disease
Megan J. Dowie,Heather B. Bradshaw,Monique L. Howard,Louise F.B. Nicholson,Richard L.M. Faull,Anthony J. Hannan,Michelle Glass +6 more
TL;DR: A detailed analysis of CB1 receptor ligand binding, protein, gene expression and levels of endocannabinoids just prior to motor symptom onset (12 weeks of age) in R6/1 transgenic mice suggests that in this R 6/1 mouse colony at 12 weeks there are only very small changes in CB1 protein and receptors and thus this would be an appropriate time point to evaluate therapeutic interventions.
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Large Receptor Reserve for Cannabinoid Actions in the Central Nervous System
Andrew N. Gifford,M. Bruneus,Samuel J. Gatley,Ruoxi Lan,Alexandros Makriyannis,Nora D. Volkow +5 more
TL;DR: The experiments suggest that behavioral effects of cannabinoids, like neurochemical effects, are produced at very low receptor occupancy, suggesting the presence of a receptor reserve that is large compared with other G protein-coupled receptor systems in the central nervous system.
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Sr 144528, an antagonist for the peripheral cannabinoid receptor that behaves as an inverse agonist
Marielle Portier,Murielle Rinaldi-Carmona,Florence Pecceu,Thérèse Combes,Caroline Poinot-Chazel,Bernard Calandra,Francis Barth,Gérard Le Fur,Pierre Casellas +8 more
TL;DR: These data provide evidences for the inverse agonist property of SR 144528 and the constitutive activation of CB2 in Chinese hamster ovary-expressing cells.
Journal ArticleDOI
Suppression of conditioned nicotine and sucrose seeking by the cannabinoid-1 receptor antagonist SR141716A.
TL;DR: The present study shows that the selective cannabinoid CB1 receptor antagonist SR141716A attenuated responding for both nicotine- and sucrose-associated stimuli in a long-term extinction-reinstatement model, providing a strong rationale for the use of CB1 antagonists in the treatment of addictive behaviors.
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Weighing the Evidence: A Systematic Review on Long-Term Neurocognitive Effects of Cannabis Use in Abstinent Adolescents and Adults.
TL;DR: Findings are mixed regarding impairments in inhibition, impulsivity and decision making for CU, but there is a trend towards worse performance, and heavy use is found to be more consistently associated with effects in diverse domains than early age of onset.
References
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