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International Union of Basic and Clinical Pharmacology. LXXIX. Cannabinoid Receptors and Their Ligands: Beyond CB1 and CB2
TLDR
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. Expand
Cloning of the first sn1-DAG lipases points to the spatial and temporal regulation of endocannabinoid signaling in the brain
TLDR
The cloning and enzymatic characterization of the first specific sn-1 DAG lipases are reported, providing a possible explanation for a fundamental change in endocannabinoid function during brain development. Expand
Molecular targets for cannabidiol and its synthetic analogues: effect on vanilloid VR1 receptors and on the cellular uptake and enzymatic hydrolysis of anandamide
TLDR
Results suggest that VR1 receptors, or increased levels of endogenous AEA, might mediate some of the pharmacological effects of CBD and its analogues, and (−)‐5′‐DMH‐CBD represents a valuable candidate for further investigation as inhibitor of AEA uptake and a possible new therapeutic agent. Expand
An endogenous capsaicin-like substance with high potency at recombinant and native vanilloid VR1 receptors
TLDR
The hypothesis, based on previous structure-activity relationship studies and the availability of biosynthetic precursors, that N-arachidonoyl-dopamine (NADA) is an endogenous “capsaicin-like” substance in mammalian nervous tissues is examined and found that NADA occurs in nervous tissues. Expand
Identification and Functional Characterization of Brainstem Cannabinoid CB2 Receptors
TLDR
These functional CB2 receptors in the brainstem were activated by a CB2 receptor agonist, 2-arachidonoylglycerol, and by elevated endogenous levels of endocannabinoids, which also act at CB1 receptors. Expand
CB1 Cannabinoid Receptors and On-Demand Defense Against Excitotoxicity
TLDR
The endogenous cannabinoid system provides on-demand protection against acute excitotoxicity in central nervous system neurons and could not be triggered in mutant mice. Expand
Regulation, function, and dysregulation of endocannabinoids in models of adipose and beta-pancreatic cells and in obesity and hyperglycemia.
TLDR
Peripheral endocannabinoid overactivity might explain why CB(1) blockers cause weight-loss independent reduction of lipogenesis, of hypoadiponectinemia, and of hyperinsulinemia in obese animals and humans. Expand
Non-psychotropic plant cannabinoids: new therapeutic opportunities from an ancient herb.
TLDR
Cannabidiol and Delta(9)-tetrahydrocannabivarin, a novel CB(1) antagonist which exerts potentially useful actions in the treatment of epilepsy and obesity are given special emphasis. Expand
Role in anxiety behavior of the endocannabinoid system in the prefrontal cortex.
TLDR
Findings support an anxiolytic role for physiological increases in AEA in the PFC, whereas more marked increases or decreases of this endocannabinoid might lead to an anxiogenic response due to TRPV1 stimulation or the lack of CB1 activation, respectively. Expand
Antitumor Activity of Plant Cannabinoids with Emphasis on the Effect of Cannabidiol on Human Breast Carcinoma
TLDR
Results obtained in a panel of tumor cell lines clearly indicate that, of the five natural compounds tested, cannabidiol is the most potent inhibitor of cancer cell growth, with significantly lower potency in noncancer cells. Expand
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