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The dietary polyphenols trans-resveratrol and curcumin (Table 1) were reported to bind selectively to the human CB1 cannabinoid receptor with low nM Ki values (5.9 nM and 45 nM respectively) and to exert potent pharmacological effects in mice similar to those induced by the CB1 receptor inverse agonist rimonabant (Seely et al., 2009). Intrigued by this unexpected finding, our research groups independently measured the binding affinities of these compounds for CB1 and CB2 receptors in our laboratories. In our experiments, trans-resveratrol and curcumin only displaced [3H]CP55 940 from cannabinoid receptors at high 然 concentrations, suggesting that they lack significant affinity for these receptors. Also polydatin, a glycosilated form of resveratrol, was inactive in these binding assays. Recently, the senior author of the original report retracted the paper (Prather et al., 2009). Hence, neither trans-resveratrol nor curcumin interact functionally with the CB1 receptor, despite the fact that these compounds appear to share the ability of the CB1 receptor inverse agonist, rimonabant, to induce weight loss in mice.
The dietary polyphenols trans-resveratrol and curcumin (Table 1) were reported to bind selectively to the human CB1 cannabinoid receptor with low nM Ki values (5.9 nM and 45 nM respectively)
Does the low binding affinity of curcumin (45nM) to CB1 receptors may act as a selective partial agonist
Quote from: tkadm30 on 29/12/2016 11:35:45Does the low binding affinity of curcumin (45nM) to CB1 receptors may act as a selective partial agonistAs demonstrated in the study, curcumin lacks the affinity to displace the full CB1/CB2 agonist CP 55,940 - unless they reach high concentrations [as in 然]. These levels aren't even achievable in vivo, so any appreciable affects by curcumin at these receptors would be highly improbable.
Started by Duncan CooksonBoard Chemistry