Puiroux J, Pedelaborde A, Loughton B G
Department of Biology, York University, North York, Ontario, Canada.
Peptides. 1993 Nov-Dec;14(6):1103-9. doi: 10.1016/0196-9781(93)90162-a.
The locust oviduct bioassay system was used to assess the ability of a variety of peptides to induce oviductal contractions. Proctolin analogues were three orders of magnitude less potent than proctolin. Proctolin supra-analogue and Arg-Tyr-Leu-Ala-Thr demonstrated high activity. Perhaps the most significant finding was the discrepancy between the high binding capacity of the proctolin analogue Arg-Tyr-Ser-Pro-Thr and its relatively low myotropic activity. This observation argues for a crucial role for the leucine residue in activating the proctolin receptor. Several other myotropic peptides were tested for their effect on oviduct contractions. FMRFamide caused contractions at doses several orders of magnitude higher than proctolin. The FLRFamide leucomyosuppression inhibited proctolin-induced contractions. In addition, myomodulin and catch relaxing peptide caused oviductal contractions at low concentrations. The enkephalins had no effect when applied alone but potentiated proctolin-induced oviduct contractions. The mechanism of the potentiation is not known. The data argue for the presence of several binding sites on the oviduct membrane.
利用蝗虫输卵管生物测定系统评估多种肽诱导输卵管收缩的能力。促肠肌肽类似物的效力比促肠肌肽低三个数量级。促肠肌肽超类似物和精氨酸 - 酪氨酸 - 亮氨酸 - 丙氨酸 - 苏氨酸表现出高活性。也许最显著的发现是促肠肌肽类似物精氨酸 - 酪氨酸 - 丝氨酸 - 脯氨酸 - 苏氨酸的高结合能力与其相对较低的促肌活性之间的差异。这一观察结果表明亮氨酸残基在激活促肠肌肽受体中起关键作用。测试了其他几种促肌肽对输卵管收缩的影响。FMRF酰胺在比促肠肌肽高几个数量级的剂量下引起收缩。FLRF酰胺的白细胞肌抑制作用抑制了促肠肌肽诱导的收缩。此外,肌调节素和捕捉松弛肽在低浓度下引起输卵管收缩。脑啡肽单独应用时无作用,但增强了促肠肌肽诱导的输卵管收缩。增强作用的机制尚不清楚。这些数据表明输卵管膜上存在多个结合位点。