米帕林对缓激肽和乙酰胆碱致痛作用的抑制

Inhibition of the algesic effect of bradykinin and acetylcholine by mepacrine.

Juan H

Naunyn Schmiedebergs Arch Pharmacol. 1977 Dec;301(1):23-7. doi: 10.1007/BF00501260.

Abstract

The isolated perfused rabbit ear connected to the body by its nerve only was used to investigate the influence of mepacrine on the algesic effect of bradykinin and acetylcholine. For comparison, quinidine was included in this investigation. 2. Infusion of mepacrine or quindine (2-10 microgram/ml) into the rabbit ear reduces the algesic effect of bradykinin as well as of acetylcholine in proportion to the dose. 3. Infusion of postglandin E1 (10 ng/ml) in addition to mepacrine or quinidine restores theinhibited algesic effect of bradykinin more than that of acetylcholine. 4. Mepacrine and quinidine (10 microgram/ml) reduce the brief vasoconstriction elicited by bradykinin in the rabbit ear. 5. The results suggest that mepacrine or quinidine reduce the algesic effect of bradykinin primarily by inhibiting the release of E-type prostaglandins which sensitize pain receptors and secondarily by an unspecific antagonism (local-anaesthetic action). The effect of acetylcholine, however, appears to be reduced mainly by an unspecific antagonism.

摘要

仅通过神经与身体相连的离体灌注兔耳被用于研究米帕林对缓激肽和乙酰胆碱镇痛作用的影响。为作比较，本研究中加入了奎尼丁。2. 向兔耳中输注米帕林或奎尼丁（2 - 10微克/毫升）可按剂量比例降低缓激肽和乙酰胆碱的镇痛作用。3. 除米帕林或奎尼丁外，输注前列腺素E1（10纳克/毫升）对缓激肽被抑制的镇痛作用的恢复程度大于对乙酰胆碱的恢复程度。4. 米帕林和奎尼丁（10微克/毫升）可减轻缓激肽在兔耳中引发的短暂血管收缩。5. 结果表明，米帕林或奎尼丁主要通过抑制使疼痛感受器敏感的E型前列腺素的释放，其次通过非特异性拮抗作用（局部麻醉作用）来降低缓激肽的镇痛作用。然而，乙酰胆碱的作用似乎主要通过非特异性拮抗作用而降低。