Targeting Cannabinoid Receptors: Current Status and Prospects of Natural Products


Dongchen An | Steve Peigneur | Louise Antonia Hendrickx | Jan Tytgat | Louise Antonia


CB2-selective agonists”. Mixed CB1/CB2 Agonists Most known synthetic agonists of cannabinoid receptors show little selectivity between CB1 and CB2 [21], but exhibit stronger affinity for cannabinoid receptors compared to endo- and phytocannabinoids [65]. HU-210 ( a), an example of a classical synthetic cannabinoid, is a highly potent cannabinoid receptor agonist, and its potency and affinity at cannabinoid receptors exceed those of many other cannabinoids [66]. Both compounds bind with much higher affinity to CB2 than to CB1, exhibit marked potency as CB2-selective antagonists and behave as inverse agonists that can produce inverse cannabimimetic effects at CB2 by themselves [66]. These peptides can be regarded as novel cannabinoids because they exhibit activity at cannabinoid receptors and have distinct structures from phytocannabinoids and synthetic cannabinoids.

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