Book ChapterDOI
Pharmacological actions of cannabinoids.
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TLDR
More information is beginning to emerge about the pharmacological actions of the non-psychoactive plant cannabinoid, cannabidiol, as well as acting on CB1 and CB2 receptors, and there is convincing evidence that anandamide can activate transient receptor potential vanilloid type 1 (TRPV1) receptors.Abstract:
Mammalian tissues express at least two types of cannabinoid receptor, CB1 and CB2, both G protein coupled. CB1 receptors are expressed predominantly at nerve terminals where they mediate inhibition of transmitter release. CB2 receptorsread more
Citations
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Journal ArticleDOI
The Endocannabinoid System as an Emerging Target of Pharmacotherapy
TL;DR: A comprehensive overview on the current state of knowledge of the endocannabinoid system as a target of pharmacotherapy is provided.
Journal ArticleDOI
The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: Δ9-tetrahydrocannabinol, cannabidiol and Δ9-tetrahydrocannabivarin
TL;DR: This review focuses on the manner with which three of these compounds, (−)‐trans‐Δ 9‐tetrahydrocannabinol (Δ9‐THC), (−]‐cannabidiol (CBD) and (−)-trans‐ Δ9‐TetrahYDrocannabivarin (Γ‐THCV), interact with cannabinoid CB1 and CB2 receptors.
Journal ArticleDOI
International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid Receptors and Their Ligands: Beyond CB1 and CB2
Roger G. Pertwee,Allyn C. Howlett,Mary E. Abood,Stephen P.H. Alexander,V. Di Marzo,Maurice R. Elphick,Peter J. Greasley,Harald S. Hansen,George Kunos,Ken Mackie,Raphael Mechoulam,Ruth Alexandra Ross +11 more
TL;DR: This review summarizes current data indicating the extent to which cannabinoid receptor ligands undergo orthosteric or allosteric interactions with non- CB1, non-CB2 established GPCRs, deorphanized receptors such as GPR55, ligand-gated ion channels, transient receptor potential (TRP) channels, and other ion channels or peroxisome proliferator-activated nuclear receptors.
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.
Journal ArticleDOI
Cannabinoid pharmacology: the first 66 years
TL;DR: Research into the pharmacology of individual cannabinoids that began in the 1940s is concisely reviewed and it is described how this pharmacological research led to the discovery of cannabinoid CB1 and CB2 receptors and of endogenous ligands for these receptors.
References
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Journal Article
Evaluation of cannabinoid receptor binding and in vivo activities for anandamide analogs.
Irma B. Adams,William R. Ryan,Michael C. Singer,Brian F. Thomas,D R Compton,Raj K. Razdan,Billy R. Martin +6 more
TL;DR: The levels of saturation of the anandamide structure were critical to receptor affinity and in vivo potency, with complete saturation and hydroxyl substitution with a fluorine moiety resulting in a compound with increased potency in the spontaneous activity and antinociception assays.
Journal ArticleDOI
Cannabinoid pharmacological properties common to other centrally acting drugs.
Jenny L. Wiley,Billy R. Martin +1 more
TL;DR: The tetrad tests are a useful tool in examination of structure-activity relationships of cannabinoid CB(1) receptor agonists, but the present results suggest that they must be used cautiously in the search for novel cannabinoid receptors.
Journal ArticleDOI
Acute neuronal injury, excitotoxicity, and the endocannabinoid system.
Mario van der Stelt,Wouter B. Veldhuis,Mauro Maccarrone,Peter R. Bär,Klaas Nicolay,Gerrit A. Veldink,Vincenzo Di Marzo,Johannes F.G. Vliegenthart +7 more
TL;DR: Several observations indicate that the role of the endocannabinoid system as a general endogenous protection system is questionable.
Journal ArticleDOI
Is the cannabinoid cb1 receptor a 2-arachidonoylglycerol receptor? structural requirements for triggering a ca2+ transient in ng108-15 cells
Takayuki Sugiura,Tomoko Kodaka,Sachiko Kondo,Shinji Nakane,Hironori Kondo,Keizo Waku,Yoshio Ishima,Kazuhito Watanabe,Ikuo Yamamoto +8 more
TL;DR: The results suggest that the structure of 2-arachidonoylglycerol is strictly recognized by theCB1 receptor, which raises the possibility that the CB1 receptor is originally a 2-Arachidonoyslglycersol receptor.
Journal ArticleDOI
Dimerization of G protein-coupled receptors: CB1 cannabinoid receptors as an example.
TL;DR: Data provide evidence that CB1 likely exists as a dimer in vivo and that the carboxy end of the receptor may play a role in the assembly of the oligomer.