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目的:观察MJ15对大麻素Ⅰ型(cannabinoid receptorsⅠ,CB1)受体的阻滞及反相激动作用。方法:制备小鼠输精管和豚鼠回肠平滑肌的离体标本,观察CB1受体激动剂WIN55212-2以及阻滞剂利莫那班(SR141716A)和MJ15对其收缩特性的影响。结果:CB1受体激动剂WIN55212-2(10-10～10-6 mol.L-1)可抑制电刺激所引起小鼠输精管的收缩作用,呈现明显的剂量依赖性,而SR141716A和MJ15(10-7 mol.L-1)能阻滞WIN55212-2的抑制作用;CB1受体激动剂WIN55212-2可抑制豚鼠回肠和小鼠输精管平滑肌的收缩,而SR141716A和MJ15能促进豚鼠回肠和小鼠输精管平滑肌的收缩。结论:MJ15是CB1受体的阻滞剂,同时具有反相激动作用。
Objective: To observe the block and inverse agonism of MJ15 on cannabinoid receptors Ⅰ (CB1) receptor. Methods: The isolated vasculature of mouse vas deferens and guinea pig ileum smooth muscle was prepared. The effects of CB55 receptor antagonist WIN55212-2 and antagonist rimonabant (SR141716A) and MJ15 on contractile properties were observed. Results: The CB1 receptor agonist WIN55212-2 (10-10 ~ 10-6 mol.L-1) inhibited the vasoconstriction of mice induced by electrical stimulation in a dose-dependent manner. However, SR141716A and MJ15 (10 -7 mol.L-1) could block the inhibitory effect of WIN55212-2; CB1 receptor agonist WIN55212-2 could inhibit the contractility of guinea pig ileum and mouse vas deferens smooth muscle while SR141716A and MJ15 could promote guinea pig ileum and mouse vas deferens Smooth muscle contraction. Conclusion: MJ15 is a blocker of CB1 receptor with anti-phase agonism.