MJ15对大麻素Ⅰ型受体的阻滞及反相激动作用的研究  

Antagonistic and inverse agonistic effect of MJ15 on cannabinoid receptors Ⅰ

作　　者：曹宁[1] 杨洋[2] 周晓棉[2] 徐成[2] 王莉莉[3] 

机构地区：[1]沈阳军区总医院,沈阳110016 [2]沈阳药科大学,沈阳110016 [3]军事医学科学院毒物药物研究所,北京100850

出　　处：《中国新药杂志》2011年第5期417-421,共5页Chinese Journal of New Drugs

基　　金：重大新药创制科技重大专项(2009ZX09301-002)

摘　　要：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 antagonistic and inverse agonistic effect of MJ15 on cannabinoid receptors Ⅰ（CB1）.Methods：The samples of the ileum smooth muscle isolated from guinea pigs and vas deferens isolated from mice were put into the Magnus＇ bath,and the contractive activities were investigated.Results：The CB1 receptor agonist WIN55212-2（10-10～10-6 mol·L-1） inhibited electrically induced contraction of mouse vas deferens;the concentration-dependency was significant.The concentration-response curse was completely inhibited by SR141716A and MJ15（10-7 mol·L-1）.WIN55212-2 inhibited contraction of mouse vas deferens and guinea pig ileum smooth muscle;while SR141716A and MJ15 accelerated the contraction.Conclusion：MJ15 is an antagonist of CB1 receptor with inverse agonistic activity.

关 键 词：大麻素Ⅰ型受体 MJ15 阻滞作用 反相激动作用 

分 类 号：R966[医药卫生—药理学]