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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The Effect of Chronic Cannabinoids on Broadband EEG Neural Oscillations in Humans
Patrick D. Skosnik,Deepak Cyril D'Souza,Adam B. Steinmetz,Chad R. Edwards,Jennifer M. Vollmer,William P. Hetrick,Brian F. O'Donnell +6 more
TL;DR: Data suggest that chronic exposure to exogenous cannabinoids can alter the ability to generate neural oscillations, particularly in the gamma range, which is consistent with preclinical animal and cellular data, which may have implications for understanding the short- and long-term psychopharmacological effects of cannabis.
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HINT1 protein cooperates with cannabinoid 1 receptor to negatively regulate glutamate NMDA receptor activity
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Combined inhibition of FAAH and COX produces enhanced anti-allodynic effects in mouse neuropathic and inflammatory pain models
Travis W. Grim,Sudeshna Ghosh,Ku-Lung Hsu,Benjamin F. Cravatt,Steven G. Kinsey,Aron H. Lichtman +5 more
TL;DR: Combined administration of subthreshold doses of these drugs produced enhanced antinociceptive effects in CCI and carrageenan pain models, the latter of which was demonstrated to require both CB1 and CB2 receptors.
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In vivo 1H magnetic resonance spectroscopy in young-adult daily marijuana users.
Ryan L. Muetzel,M. Marjanska,Paul F. Collins,Mary P. Becker,Romain Valabregue,Edward J. Auerbach,Kelvin O. Lim,Monica Luciana +7 more
TL;DR: There were no overall group effects, but two metabolites showed group by sex interactions, and higher levels of myo-inositol were observed in female users compared to female non-users and to males in both groups.
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Synthesis and structure–activity relationships (SARs) of 1,5-diarylpyrazole cannabinoid type-1 (CB1) receptor ligands for potential use in molecular imaging
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