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阿片类物质对反刍动物胃动力的控制:μ、κ和δ受体的功能重要性

Opioid control of the ruminant stomach motility: functional importance of mu, kappa and delta receptors.

作者信息

Ruckebusch Y, Bardon T, Pairet M

出版信息

Life Sci. 1984 Oct 22;35(17):1731-8. doi: 10.1016/0024-3205(84)90269-8.

Abstract

In sheep, the subcutaneous (SC) or intracerebroventricular (ICV) administration of the mu-type opioid agonists, fentanyl and morphine, evokes a blockade of the cyclic contractions of the reticulum. A similar inhibition of forestomach motility was recorded following the administration of the two enkephalin analogs, D-Ala2-Met5-enkephalinamide (DAMA) and D-Ala2-D-Leu5-enkephalin (DADLE) which are mixed mu - delta opioid agonists. In contrast, the reticular contractions were enhanced by the SC or ICV administration of the kappa type agonist, ethylketazocine (EKC) and U - 50 488 H. The proximal duodenum motor activity was transiently increased resulting in the occurrence of a phase III-like activity by these opioid agonists, regardless of the subtypes. The effects of the opioid agonists on reticular motility were prevented by the injection of naloxone but not by the quaternary parent compound methylnaloxone which does not cross the blood-brain barrier. The duodenal motor effects elicited by the opioid agonists were antagonized by both naloxone and methylnaloxone. The results suggest that the inhibition of the ruminant stomach motility is centrally mediated by mu - delta type opioid agonists and are consistent with opposite effects from kappa type opioid agonists. The stimulatory effect of peptide and non-peptide opioid agonists on the duodenum may result in part from direct opioid receptor-mediated actions on smooth muscle.

摘要

在绵羊中,皮下(SC)或脑室内(ICV)给予μ型阿片类激动剂芬太尼和吗啡,可引起网胃周期性收缩的阻滞。给予两种脑啡肽类似物,即混合的μ-δ阿片类激动剂D-Ala2-Met5-脑啡肽酰胺(DAMA)和D-Ala2-D-Leu5-脑啡肽(DADLE)后,也记录到了前胃运动的类似抑制。相反,皮下或脑室内给予κ型激动剂乙基酮唑辛(EKC)和U-50488H可增强网胃收缩。无论阿片类激动剂的亚型如何,这些激动剂均可使十二指肠近端运动活性短暂增加,导致出现类似Ⅲ期的活动。阿片类激动剂对网胃运动的作用可被纳洛酮注射所阻断,但不能被不能穿过血脑屏障的季铵母体化合物甲基纳洛酮所阻断。阿片类激动剂引起的十二指肠运动效应可被纳洛酮和甲基纳洛酮所拮抗。结果表明,反刍动物胃运动的抑制是由μ-δ型阿片类激动剂中枢介导的,与κ型阿片类激动剂的相反作用一致。肽类和非肽类阿片类激动剂对十二指肠的刺激作用可能部分源于阿片受体对平滑肌的直接作用。

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