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
More filters
Journal ArticleDOI
Crystal Structure of the Human Cannabinoid Receptor CB2.
Tian Hua,Kiran Vemuri,Mengchen Pu,Lu Qu,Lu Qu,Gye Won Han,Yiran Wu,Suwen Zhao,Wenqing Shui,Shanshan Li,Anisha Korde,Robert B. Laprairie,Edward L. Stahl,Jo-Hao Ho,Nikolai Zvonok,Han Zhou,Irina Kufareva,Beili Wu,Qiang Zhao,Michael A. Hanson,Laura M. Bohn,Alexandros Makriyannis,Raymond C. Stevens,Raymond C. Stevens,Zhi-Jie Liu,Zhi-Jie Liu +25 more
TL;DR: The structure of the CB1-AM6538 complex reveals key features of the receptor and critical interactions for antagonist binding and provides insight into the binding mode of naturally occurring CB1 ligands, such as THC, and synthetic cannabinoids.
Journal ArticleDOI
Activation of Corticotropin-Releasing Factor in the Limbic System During Cannabinoid Withdrawal
Fernando Rodríguez de Fonseca,M. Rocio A. Carrera,M. Rocio A. Carrera,Miguel Navarro,Miguel Navarro,George F. Koob,George F. Koob,Friedbert Weiss,Friedbert Weiss +8 more
TL;DR: It is suggested that long-term cannabinoid administration alters CRF function in the limbic system of the brain, in a manner similar to that observed with other drugs of abuse, and also induces neuroadaptive processes that may result in future vulnerability to drug dependence.
Journal ArticleDOI
The acute effects of cannabinoids on memory in humans: a review
TL;DR: This profile of effects suggests that cannabinoids impair all stages of memory including encoding, consolidation, and retrieval, and that cannabinoids increase intrusion errors with the inhaled and intravenous route and correspond to peak drug levels.
Journal ArticleDOI
Endocannabinoid system and stress and anxiety responses.
TL;DR: The endocannabinoid system appears to play a pivotal role in the regulation of emotional states and may constitute a novel pharmacological target for anti-anxiety therapy.
Journal ArticleDOI
Cerebrospinal Anandamide Levels are Elevated in Acute Schizophrenia and are Inversely Correlated with Psychotic Symptoms
Andrea Giuffrida,F. Markus Leweke,C.W. Gerth,D. Schreiber,D. Schreiber,Dagmar Koethe,Johannes Faulhaber,Joachim Klosterkötter,Daniele Piomelli +8 more
TL;DR: The results suggest that anandamide elevation in acute paranoid schizophrenia may reflect a compensatory adaptation to the disease state, and the endocannabinoids are a family of bioactive lipids that activate CB1 cannabinoid receptors in the brain and exert intense emotional and cognitive effects.
References
More filters
Journal Article
Protein Measurement with the Folin Phenol Reagent
TL;DR: Procedures are described for measuring protein in solution or after precipitation with acids or other agents, and for the determination of as little as 0.2 gamma of protein.
Journal ArticleDOI
Drugs abused by humans preferentially increase synaptic dopamine concentrations in the mesolimbic system of freely moving rats.
G. Di Chiara,Assunta Imperato +1 more
TL;DR: The effect of various drugs on the extracellular concentration of dopamine in two terminal dopaminergic areas, the nucleus accumbens septi (a limbic area) and the dorsal caudate nucleus (a subcortical motor area), was studied in freely moving rats by using brain dialysis as mentioned in this paper.
Journal Article
Determination and characterization of a cannabinoid receptor in rat brain.
TL;DR: The criteria for a high affinity, stereoselective, pharmacologically distinct cannabinoid receptor in brain tissue have been fulfilled.
Journal ArticleDOI
Quantitative autoradiographic localization of the D1 and D2 subtypes of dopamine receptors in rat brain
TL;DR: In this article, the distribution of D1 and D2 receptors was studied in coronal sections of rat brain, using quantitative autoradiography, and the binding of both ligands to sections from brain and from a homogenate of caudate putamen (CPu mash) reached equilibrium within 80 min at 37 degrees C.