Russell J A, Leng G, Coombes J E, Crockett S A, Douglas A J, Murray I, Way S
Department of Physiology, Medical School, Edinburgh University, United Kingdom.
Am J Physiol. 1991 Aug;261(2 Pt 2):R358-68. doi: 10.1152/ajpregu.1991.261.2.R358.
Pethidine (also known as meperidine and as Demerol) injected subcutaneously at 10 mg/kg into parturient rats on the birth of the second pup resulted in a marked slowing of the progress of parturition, associated with reduced plasma oxytocin concentrations. Injection of the opiate antagonist naloxone counteracted the inhibition of oxytocin secretion and largely prevented the slowing of parturition. In vitro, pethidine inhibited spontaneous, oxytocin-induced and acetylcholine-induced contractions of uteri from rats immediately post partum, and these effects were not reversed by naloxone. In anesthetized lactating rats, pethidine inhibited the suckling-induced milk-ejection reflex and attenuated oxytocin-induced contractions of mammary myoepithelium. Finally, pethidine depressed plasma oxytocin concentrations in rats given 2% saline to drink for 24 h to stimulate oxytocin secretion. Thus pethidine inhibits oxytocin secretion in all three conditions; this inhibition is probably mediated by central opioid receptors. In addition, however, pethidine depresses the oxytocin responsiveness both of mammary myoepithelium and of myometrium. The latter effect at least is not opioid mediated.
在第二只幼崽出生时,给分娩的大鼠皮下注射10毫克/千克的哌替啶(也称为度冷丁和德美罗),导致分娩进程显著减慢,同时血浆催产素浓度降低。注射阿片类拮抗剂纳洛酮可抵消催产素分泌的抑制作用,并在很大程度上防止分娩减慢。在体外,哌替啶抑制产后立即取自大鼠的子宫的自发收缩、催产素诱导的收缩和乙酰胆碱诱导的收缩,而这些作用不能被纳洛酮逆转。在麻醉的泌乳大鼠中,哌替啶抑制哺乳诱导的射乳反射,并减弱催产素诱导的乳腺肌上皮收缩。最后,给饮用2%盐水24小时以刺激催产素分泌的大鼠注射哌替啶会降低其血浆催产素浓度。因此,哌替啶在所有这三种情况下均抑制催产素分泌;这种抑制作用可能是由中枢阿片受体介导的。然而,此外,哌替啶还会降低乳腺肌上皮和子宫肌层对催产素的反应性。至少后一种作用不是由阿片类介导的。