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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Downregulation of rat brain cannabinoid binding sites after chronic Δ9-tetrahydrocannabinol treatment
TL;DR: Whether cannabinoid receptors exhibit downregulation as a consequence of the chronic exposure to delta 9-tetrahydrocannabinol (THC), which might explain certain tolerance phenomena observed in relation to motor and limbic effects of marijuana, is examined.
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Assessment of Anandamide Interaction with the Cannabinoid Brain Receptor: SR 141716A Antagonism Studies in Mice and Autoradiographic Analysis of Receptor Binding in Rat Brain
TL;DR: The results presented herein raise the possibility that anandamide may not be producing all of its effects by a direct interaction with the CB1 receptor, despite failure of SR 141716A to block its pharmacological effects in mice.
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Endogenous cannabinoid signaling
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Activation of inwardly rectifying potassium channels (GIRK1) by co-expressed rat brain cannabinoid receptors in Xenopus oocytes
TL;DR: The neuronal cannabinoid receptor clone was expressed of saturable [3H]WIN 55,212-2 binding sites and co-expression of the cannabinoid receptor with cRNA coding for the G-protein-gated inwardly rectifying K+ channel (GIRK1) resulted in oocytes exhibiting large inward K+ currents in response to the cannabinoid agonists.
Journal ArticleDOI
Quantification of cerebral cannabinoid receptors subtype 1 (CB1) in healthy subjects and schizophrenia by the novel PET radioligand [11C]OMAR.
Dean F. Wong,Hiroto Kuwabara,Andrew G. Horti,Vanessa Raymont,James Robert Brašić,Maria Guevara,Weiguo Ye,Robert F. Dannals,Hayden T. Ravert,Ayon Nandi,Arman Rahmim,Jeffrey E. Ming,Igor Grachev,Christine Roy,Nicola G. Cascella +14 more
TL;DR: In this paper, a PET tracer called [(11)C]OMAR (JHU75528) was used to image human CB1 receptors in normal aging and schizophrenia.
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