Journal ArticleDOI
Enzymatic synthesis and degradation of anandamide, a cannabinoid receptor agonist.
Dale G. Deutsch,Suzette A. Chin +1 more
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TLDR
The stability of anandamide in serum and its rapid breakdown in cells and tissues are consistent with the observation that it is active when administered systemically, and its duration of action will be regulated by its rate of degradation in cells.About:
This article is published in Biochemical Pharmacology.The article was published on 1993-09-01. It has received 718 citations till now. The article focuses on the topics: Cannabinoid & Anandamide.read more
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Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors.
Raphael Mechoulam,Shimon Ben-Shabat,Lumir Hanus,Moshe Ligumsky,Norbert E. Kaminski,Anthony R. Schatz,Asher Gopher,Shlomo Almog,Billy R. Martin,David R. Compton,Roger G. Pertwee,Graeme Griffin,Michael Bayewitch,Jacob Barg,Zvi Vogel +14 more
TL;DR: Upon intravenous administration to mice, 2-Ara-Gl caused the typical tetrad of effects produced by THC: antinociception, immobility, reduction of spontaneous activity, and lowering of the rectal temperature.
Journal ArticleDOI
Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides
Benjamin F. Cravatt,Dan K. Giang,Stephen P. Mayfield,Dale L. Boger,Richard A. Lerner,Norton B. Gilula +5 more
TL;DR: It is shown that oleamide hydrolase may serve as the general inactivating enzyme for a growing family of bioactive signalling molecules, the fatty-acid amides6–8, and the structure and sleep-inducing properties of cis-9-octadecenamide, a lipid isolated from the cerebrospinal fluid of sleep-deprived cats are reported.
Journal ArticleDOI
Formation and inactivation of endogenous cannabinoid anandamide in central neurons.
V. Di Marzo,Angelo Fontana,Hugues Cadas,S. Schinelli,Guido Cimino,J.-C. Schwartz,Daniele Piomelli +6 more
TL;DR: It is reported that anandamide is produced in and released from cultured brain neurons in a calcium ion-dependent manner when the neurons are stimulated with membrane-depolarizing agents, indicating that multiple biochemical pathways may participate in an andamide formation in brain tissue.
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Role of Endogenous Cannabinoids in Synaptic Signaling
TL;DR: The synthetic pathways of endocannabinoids are discussed, along with the putative mechanisms of their release, uptake, and degradation, and the fine-grain anatomical distribution of the neuronal cannabinoid receptor CB1 is described in most brain areas, emphasizing its general presynaptic localization and role in controlling neurotransmitter release.
Journal ArticleDOI
Pharmacology of cannabinoid cb1 and cb2 receptors
TL;DR: This review focuses on the classification, binding properties, effector systems and distribution of cannabinoid receptors, and describes the various cannabinoid receptor agonists and antagonists now available and considers the main in vivo and in vitro bioassay methods that are generally used.
References
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Journal ArticleDOI
Isolation and structure of a brain constituent that binds to the cannabinoid receptor
William A. Devane,Lumir Hanus,Aviva Breuer,Roger G. Pertwee,Lesley A. Stevenson,Graeme Griffin,Dan Gibson,Asher Mandelbaum,A. Etinger,Raphael Mechoulam +9 more
TL;DR: In this article, an arachidonylethanthanolamide (anandamide) was identified in a screen for endogenous ligands for the cannabinoid receptor and its structure was determined by mass spectrometry and nuclear magnetic resonance spectroscopy and confirmed by synthesis.
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Structure of a cannabinoid receptor and functional expression of the cloned cDNA
TL;DR: 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.
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Distribution of neuronal cannabinoid receptor in the adult rat brain: a comparative receptor binding radioautography and in situ hybridization histochemistry.
TL;DR: This study provides, for the first time, indirect assessment of the neurons containing cannabinoid receptor in the entire adult rat brain and will serve as a basis for future direct morphological confirmation using receptor immunohistochemistry and for functional studies.
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Pharmacological activity of the cannabinoid receptor agonist, anandamide, a brain constituent
Ester Fride,Raphael Mechoulam +1 more
TL;DR: Anandamide administered i.p. in mice, caused lowering of activity in an immobility and in an open field test, and produced hypothermia and analgesia, which parallel those caused by psychotropic cannabinoids.
Journal ArticleDOI
Behavioral, biochemical, and molecular modeling evaluations of cannabinoid analogs.
Billy R. Martin,D R Compton,Brian F. Thomas,W. R. Prescott,P. J. Little,Raj K. Razdan,M R Johnson,L S Melvin,Raphael Mechoulam,S. J. Ward +9 more
TL;DR: The structural diversity and wide-ranging potencies of the analogs described herein provide the opportunity to develop a pharmacophore for the cannabinoids using molecular modeling techniques.