Peeters T L, Bormans V, Matthijs G, Vantrappen G
Regul Pept. 1986 Nov;15(4):333-9. doi: 10.1016/0167-0115(86)90163-1.
The biological activity of porcine and canine motilin was studied in rabbits by establishing dose-response curves of both peptides using two different methods. The dissociation constant, obtained from the displacement of iodinated porcine motilin by canine motilin was 0.6 +/- 0.3 nM, versus 1.2 +/- 0.4 nM for porcine motilin. For the 13-norleucine and 13-leucine analogues of porcine motilin a value of 0.8 +/- 0.3 nM was obtained. Both motilins were almost equipotent in stimulating the in vitro contractile response of longitudinal smooth muscle strips: half-maximal effect was achieved at a concentration of 1.0 +/- 0.1 nM for canine versus 1.3 +/- 0.2 nM for the 13-norleucine analogue of porcine motilin. We conclude that porcine and canine motilin have a comparable bioactivity in the rabbit, although canine motilin is slightly more effective. The motilin receptor is probably specific for the N-terminal portion which is identical in both molecules.
通过使用两种不同方法建立两种肽的剂量反应曲线,研究了猪胃动素和犬胃动素在兔体内的生物活性。由犬胃动素取代碘化猪胃动素得到的解离常数为0.6±0.3 nM,而猪胃动素的解离常数为1.2±0.4 nM。猪胃动素的13-去甲亮氨酸和13-亮氨酸类似物的值为0.8±0.3 nM。两种胃动素在刺激纵向平滑肌条的体外收缩反应方面几乎具有同等效力:犬胃动素在浓度为1.0±0.1 nM时达到半数最大效应,而猪胃动素的13-去甲亮氨酸类似物在浓度为1.3±0.2 nM时达到半数最大效应。我们得出结论,猪胃动素和犬胃动素在兔体内具有相当的生物活性,尽管犬胃动素的效力略高。胃动素受体可能对两个分子中相同的N末端部分具有特异性。