L-365,260 reversed effect of sincalide against morphine on electrical and mechanical activities of rat duodenum in vitro  

L-365,260翻转辛卡利特对抗吗啡对大鼠离体十二指肠电与机械活动的影响(英文)

作　　者：杨春晓[1] 徐满英 刘风玉[2] 杨东晓[2] 王淑珍[2] 

机构地区：[1]哈尔滨医科大学附属二院神经科,哈尔滨中国150086 [2]哈尔滨医科大学附属二院生理教研室,哈尔滨中国150086

出　　处：《Acta Pharmacologica Sinica》2002年第7期8-12,共5页中国药理学报（英文版）

基　　金：Project supported by the Scientific Technological Foundation of Provincial Educational Committee of Heilongjiang in China,№ 95-8.

摘　　要：AIM: To study the antagonism of sincalide (CCK-8) to the effect of morphine and its mechanism. METH-ODS: The electrical and mechanical activities of rat duodenum in vitro were recorded simultaneously. RESULTS: Acetylcholine ( ACh, 300 nmol/L ) increased the spike potential amplitude (SPA) and the number (SPN) of rat duodenum in vitro, followed by an increase of duodenal contraction amplitudes (CA). The SPA, SPN, and CA of duodenum in vitro were not obviously affected by injection of morphine (330 nmol/ L), but it could selectively inhibit the potentiation of ACh. After administration of CCK-8 (0.7 nmol/L), the SPA, SPN, and CA of duodenal segment did not exhibit obvious changes. But CCK-8 could selectively antagonize the effects of morphine, ie, the SPA and SPN were increased again, followed by an increase of CA. CCK-B receptor antagonist L-365, 260 (30 nmol/L) reversed the antagonism of CCK-8 to the effect of morphine. CONCLUSION: CCK-8 could selectively antagonize the effect of morphine which inhibited the potentiation of ACh on duodenal activities in vitro. The antagonistic effect of CCK-8 on morphine was mainly mediated by CCK-B receptor.目的:研究辛卡利特(CCK-8)的抗吗啡作用及其作用机制。方法:采用了同步描记大鼠离体十二指肠电与机械活动的方法。结果:乙酰胆碱(ACh,300nmol/L)可使大鼠离体十二指肠峰波振幅增大、数目增多,其收缩幅度随之增大,两者呈正相关。吗啡(330nmol/L)对离体十二指肠峰波的振幅、数目和收缩幅度均无明显影响,但能选择性抑制ACh对十二指肠段电与机械活动的加强作用,呈负相关。CCK-8(0.7nmol/L)本身对十二指肠段的电与收缩活动均无明显影响,但能选择性对抗吗啡的作用,即峰波振幅、数目再次增加,收缩幅度也随之增加。在此基础上,CCK-B受体拮抗剂L-365,260(30nmol/L)能翻转CCK-8的抗吗啡作用。结论:CCK-8能对抗吗啡抑制ACh加强十二指肠活动的作用,推测该作用是通过CCK-B受体实现的。

关 键 词：SINCALIDE MORPHINE ACETYLCHOLINE uodenum ELECTROPHYSIOLOGY muscle contraction 

分 类 号：R9[医药卫生—药学]