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A Cannabinoid-1 Receptor Antagonist MJ08 with Different Effects in Stomach and Small Intestine
Yang Yu1, Wei Chen2, Dan Meng1
1Life Science and Biology Pharmacy College, Shenyang Pharmaceutical University, Shenyang, Liaoning, China.
Abstract:
To investigate the inverse agonistic effect of a novel type 1 cannabinoid (CB In vivo, carbon propulsion within the stomach of mice was undertaken to investigate the effects of MJ08. In vitro, the effects of MJ08 were investigated on the contraction of smooth muscle on the isolated gastric fundus, gastric body, duodenum, jejunum, and ileum.Western blotting results showed that MJ08 (0.62 mg/kg body weight) reversed WIN55,212-2 (1.0 mg/kg)-induced reduction of carbon transit. MJ08 (1.25, 2.5 mg/kg) stimulated carbon transit dose dependently, demonstrating an inverse agonistic effect. In vitro experiments showed that the expression of MJ08 increased the contraction of small intestine, and that its inverse agonistic effect was significantly stronger than that of SR141716A, but no effect was noted on the gastric body. Western blotting showed that the MJ08 increased the expression of CBMJ08 is not only an antagonist but also an inverse agonist of the CB
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