Cannabinoid potentiation of glycine receptors contributes to cannabis-induced analgesia
作者： Wei Xiong , KeJun Cheng , Tanxing Cui , Grzegorz Godlewski , Kenner C Rice
DOI: 10.1038/NCHEMBIO.552
关键词:
摘要: Cannabinoids enhance the function of glycine receptors (GlyRs). However, little is known about mechanisms and behavioral implication cannabinoid-GlyR interaction. Using mutagenesis NMR analysis, we have identified a serine at 296 in GlyR protein critical for potentiation I(Gly) by Δ(9)-tetrahydrocannabinol (THC), major psychoactive component marijuana. The polarity amino acid residue hydroxyl groups THC are potentiation. Removal results compound that does not affect when applied alone but selectively antagonizes cannabinoid-induced potentiating effect on analgesic tail-flick test mice. analgesia absent mice lacking α3GlyRs those CB1 CB2 receptors. These findings reveal new mechanism underlying cannabinoid GlyRs, which could contribute to some cannabis-induced therapeutic effects.
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