Cannabichromene是大麻素CB2受体激动剂。,British Journal of Pharmacology

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Cannabichromene是大麻素CB2受体激动剂。
British Journal of Pharmacology ( IF 6.8 ) Pub Date : 2019-11-21 , DOI: 10.1111/bph.14815
Michael Udoh ₁ , Marina Santiago ₁ , Steven Devenish ₂ , Iain S McGregor ₂ , Mark Connor ₁

Affiliation

背景与目的大麻素（CBC）是大麻属植物中含量最丰富的植物大麻素之一。它具有适度的抗伤害感受和抗炎作用，并在体内增强了Δ9-四氢大麻酚的某些作用。CBC如何发挥这些作用的定义不清，关于其对大麻素受体功效的信息很少。我们试图确定CBC对大麻素CB1和CB2受体的功能活性。实验方法使用稳定表达血凝素标签的人CB1和CB2受体的AtT20细胞。进行细胞膜电位和细胞表面受体损失的测定。关键结果CBC激活CB2受体，但不激活CB1受体，从而产生AtT20细胞超极化。这种激活被CB2受体拮抗剂AM630抑制，并且对百日咳毒素敏感。CBC的施用通过随后共同施用有效的CB1和CB2受体激动剂CP55,940降低了CB2受体的活化，但没有降低CB1受体的活化。连续CBC的应用导致细胞表面CB2受体的丢失和CB2受体诱导的超极化的脱敏。结论和意义CBC是一种选择性CB2受体激动剂，在超极化AtT20细胞中显示出比四氢大麻酚更高的功效。CBC还可以募集CB2受体调节机制。CBC可能通过CB2受体介导的炎症调节来提高某些大麻制剂的潜在治疗效果。连续CBC的应用导致细胞表面CB2受体的丢失和CB2受体诱导的超极化的脱敏。结论和意义CBC是一种选择性CB2受体激动剂，在超极化AtT20细胞中显示出比四氢大麻酚更高的功效。CBC还可以募集CB2受体调节机制。CBC可能通过CB2受体介导的炎症调节来提高某些大麻制剂的潜在治疗效果。连续CBC的应用导致细胞表面CB2受体的丢失和CB2受体诱导的超极化的脱敏。结论和意义CBC是一种选择性CB2受体激动剂，在超极化AtT20细胞中显示出比四氢大麻酚更高的功效。CBC还可以募集CB2受体调节机制。CBC可能通过CB2受体介导的炎症调节来提高某些大麻制剂的潜在治疗效果。

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Cannabichromene is a cannabinoid CB2 receptor agonist.

BACKGROUND AND PURPOSE Cannabichromene (CBC) is one of the most abundant phytocannabinoids in Cannabis spp. It has modest antinociceptive and anti-inflammatory effects and potentiates some effects of Δ9 -tetrahydrocannabinol in vivo. How CBC exerts these effects is poorly defined and there is little information about its efficacy at cannabinoid receptors. We sought to determine the functional activity of CBC at cannabinoid CB1 and CB2 receptors. EXPERIMENTAL APPROACH AtT20 cells stably expressing haemagglutinin-tagged human CB1 and CB2 receptors were used. Assays of cellular membrane potential and loss of cell surface receptors were performed. KEY RESULTS CBC activated CB2 but not CB1 receptors to produce hyperpolarization of AtT20 cells. This activation was inhibited by a CB2 receptor antagonist AM630, and sensitive to Pertussis toxin. Application of CBC reduced activation of CB2 , but not CB1 , receptors by subsequent co-application of CP55,940, an efficacious CB1 and CB2 receptor agonist. Continuous CBC application induced loss of cell surface CB2 receptors and desensitization of the CB2 receptor-induced hyperpolarization. CONCLUSIONS AND IMPLICATIONS CBC is a selective CB2 receptor agonist displaying higher efficacy than tetrahydrocannabinol in hyperpolarizing AtT20 cells. CBC can also recruit CB2 receptor regulatory mechanisms. CBC may contribute to the potential therapeutic effectiveness of some cannabis preparations, potentially through CB2 receptor-mediated modulation of inflammation.

更新日期：2019-11-01

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