Are cannabidiol and Δ9‐tetrahydrocannabivarin negative modulators of the endocannabinoid system? A systematic review

作者: John M McPartland , Marnie Duncan , Vincenzo Di Marzo , Roger G Pertwee

DOI: 10.1111/BPH.12944

关键词:

摘要: Based upon evidence that the therapeutic properties of Cannabis preparations are not solely dependent presence Δ9-tetrahydrocannabinol (THC), pharmacological studies have been recently carried out with other plant cannabinoids (phytocannabinoids), particularly cannabidiol (CBD) and Δ9-tetrahydrocannabivarin (THCV). Results from some these fostered view CBD THCV modulate effects THC via direct blockade cannabinoid CB1 receptors, thus behaving like first-generation receptor inverse agonists, such as rimonabant. Here, we review in vitro ex vivo mechanistic THCV, synthesize data a meta-analysis. Synthesized regarding mechanisms then used to interpret results recent pre-clinical animal clinical trials. The indicates rimonabant-like their action appear very unlikely produce unwanted CNS effects. They exhibit markedly disparate profiles at receptors: is low-affinity ligand can nevertheless affect activity an indirect manner, while high-affinity potent antagonist yet only occasionally produces resulting antagonism. has also high affinity for CB2 receptors signals partial agonist, differing both These illustrate how do always predict pharmacology underlie necessity testing compounds before drawing any conclusion on functional given target.

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