Journal ArticleDOI
Structure of a cannabinoid receptor and functional expression of the cloned cDNA
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TLDR
The cloning and expression of a complementary DNA that encodes a G protein-coupled receptor that is involved in cannabinoid-induced CNS effects (including alterations in mood and cognition) experienced by users of marijuana are suggested.Abstract:
Marijuana and many of its constituent cannabinoids influence the central nervous system (CNS) in a complex and dose-dependent manner. Although CNS depression and analgesia are well documented effects of the cannabinoids, the mechanisms responsible for these and other cannabinoid-induced effects are not so far known. The hydrophobic nature of these substances has suggested that cannabinoids resemble anaesthetic agents in their action, that is, they nonspecifically disrupt cellular membranes. Recent evidence, however, has supported a mechanism involving a G protein-coupled receptor found in brain and neural cell lines, and which inhibits adenylate cyclase activity in a dose-dependent, stereoselective and pertussis toxin-sensitive manner. Also, the receptor is more responsive to psychoactive cannabinoids than to non-psychoactive cannabinoids. Here we report the cloning and expression of a complementary DNA that encodes a G protein-coupled receptor with all of these properties. Its messenger RNA is found in cell lines and regions of the brain that have cannabinoid receptors. These findings suggest that this protein is involved in cannabinoid-induced CNS effects (including alterations in mood and cognition) experienced by users of marijuana.read more
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Endocannabinoid-Mediated Control of Synaptic Transmission
TL;DR: This review aims to integrate the current understanding of functions of the endocannabinoid system, especially focusing on the control of synaptic transmission in the brain, and summarizes recent electrophysiological studies carried out on synapses of various brain regions and discusses how synaptic transmission is regulated by endoc cannabinoidoid signaling.
Journal Article
The orphan receptor GPR55 is a novel cannabinoid receptor. Commentary
R. G. Pertwee,Erik Ryberg,Niklas Larsson,S. Sjögren,Stephan Hjorth,Nils-Olov Hermansson,J. Leonova,Thomas Elebring,Karolina Nilsson,Tomas Drmota,Peter J. Greasley +10 more
TL;DR: In this paper, the authors demonstrate that GPR55 is a novel cannabinoid receptor and its ligand profile with respect to CB 1 and CB 2 described here will permit delineation of its physiological function(s).
Journal ArticleDOI
Effect of Rimonabant, a Cannabinoid-1 Receptor Blocker, on Weight and Cardiometabolic Risk Factors in Overweight or Obese Patients: RIO-North America: A Randomized Controlled Trial
TL;DR: Treatment with 20 mg/d of rimonabant plus diet for 2 years promoted modest but sustained reductions in weight and waist circumference and favorable changes in cardiometabolic risk factors, however, the trial was limited by a high drop-out rate and longer-term effects of the drug require further study.
Journal ArticleDOI
Endocannabinoid signaling in the brain.
Rachel Wilson,Roger A. Nicoll +1 more
TL;DR: The primary psychoactive ingredient in cannabis, Δ9-tetrahydrocannabinol (Δ9-THC), affects the brain mainly by activating a specific receptor (CB1) and suppressing neurotransmitter release.
Journal ArticleDOI
Presynaptically Located CB1 Cannabinoid Receptors Regulate GABA Release from Axon Terminals of Specific Hippocampal Interneurons
István Katona,Beáta Sperlágh,Attila Sik,Attila Käfalvi,E. Sylvester Vizi,Ken Mackie,Tamás F. Freund +6 more
TL;DR: The results suggest that cannabinoid-mediated modulation of hippocampal interneuron networks operate largely via presynaptic receptors on CCK-immunoreactive basket cell terminals, the likely mechanism by which both endogenous and exogenous CB1 ligands interfere with hippocampal network oscillations and associated cognitive functions.
References
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Journal ArticleDOI
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G proteins and dual control of adenylate cyclase
TL;DR: It is clear that detailed understanding of the mechanism of regulation of CAMP synthesis will soon be achieved from study of the interactions of purified components that have been reconstituted in lipid bilayers of defined composition.
Journal ArticleDOI
Identification of a family of muscarinic acetylcholine receptor genes
TL;DR: Analysis of human and rat genomic clones indicates that there are at least four functional muscarinic receptor genes and that these genes lack introns in the coding sequence.