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
Citations
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The psychotomimetic effects of intravenous Delta-9-tetrahydrocannabinol in healthy individuals: Implications for psychosis
Deepak Cyril D'Souza,Edward Perry,Lisa MacDougall,Yola Ammerman,Thomas B. Cooper,Thomas B. Cooper,Yu-te Wu,Gabriel Braley,Ralitza Gueorguieva,John H. Krystal +9 more
TL;DR: It is indicated that Δ-9-THC produces a broad range of transient symptoms, behaviors, and cognitive deficits in healthy individuals that resemble some aspects of endogenous psychoses and warrant further study of whether brain cannabinoid receptor function contributes to the pathophysiology of psychotic disorders.
Control of pain initiation by endogenous cannabinoids
TL;DR: In this article, anandamide attenuates the pain behavior produced by chemical damage to cutaneous tissue by interacting with CB1-like cannabinoid receptors located outside the central nervous system.
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Expression of the cannabinoid receptor CB1 in distinct neuronal subpopulations in the adult mouse forebrain
Giovanni Marsicano,Beat Lutz +1 more
TL;DR: It is suggested that a putative cross‐talk between cannabinoids and CCK might exist and will be relevant to better understanding of physiology and pharmacology of the cannabinoid system.
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Retrograde Inhibition of Presynaptic Calcium Influx by Endogenous Cannabinoids at Excitatory Synapses onto Purkinje Cells
TL;DR: It is suggested that Purkinje cells release endogenous cannabinoids in response to elevated calcium, thereby inhibiting presynaptic calcium entry and suppressing transmitter release, and suggesting a widespread role for endogenous cannabinoid in retrograde synaptic inhibition.
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The Endocannabinoid System and the Brain
TL;DR: Research on the actions of the endocannabinoid system on anxiety, depression, neurogenesis, reward, cognition, learning, and memory, and the effects are at times biphasic--lower doses causing effects opposite to those seen at high doses.
References
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Drugs abused by humans preferentially increase synaptic dopamine concentrations in the mesolimbic system of freely moving rats.
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Quantitative autoradiographic localization of the D1 and D2 subtypes of dopamine receptors in rat brain
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