Ji Sang Won, Park Hyojin, Chung Jun Pyo, Lee Sang In, Lee Young Ho
Department of Internal Medicine, Yonsei University College of Medicine, Seoul, Korea.
J Pharmacol Sci. 2004 Feb;94(2):144-52. doi: 10.1254/jphs.94.144.
The mechanisms of prokinetic action of tegaserod in the gastrointestinal tract has not been studied in detail. The aim of this study was to investigate the effect of tegaserod on peristaltic reflexes and propagating peristaltic waves in guinea pig ileum. A partitioned organ bath divided into three chambers was used to investigate the effect of tegaserod on peristaltic reflexes. A sensory stimulus was applied to the intermediate chamber, and changes in the circular muscle tension were monitored in a peripheral chamber. Another peristaltic bath was used to investigate the effect of tegaserod on peristaltic waves induced by intraluminal perfusion. Guinea pig ileum exhibited contractions in the circular muscle both orally and anally in response to mucosal stroking. Tegaserod (10(-8) - 10(-6) M) did not influence the maximal amplitude and the area under the curve of contraction both orally and anally to a mucosal stimulus. Intraluminal perfusion of fluid containing tegaserod (10(-8) - 10(-6) M) significantly increased the number of peristaltic waves in a concentration-dependent manner (P<0.05). Also, tegaserod (10(-8) - 10(-6) M) significantly increased the area under the curve of peristaltic waves (P<0.05). It is concluded that tegaserod has prokinetic action on guinea pig ileum by increasing the number of the circular muscle contractions during peristalsis.
替加色罗在胃肠道中的促动力作用机制尚未得到详细研究。本研究的目的是调查替加色罗对豚鼠回肠蠕动反射和蠕动传播波的影响。使用分为三个腔室的分隔器官浴来研究替加色罗对蠕动反射的影响。向中间腔室施加感觉刺激，并在外周腔室监测环行肌张力的变化。另一个蠕动浴用于研究替加色罗对腔内灌注诱导的蠕动波的影响。豚鼠回肠在口腔和肛门处对粘膜抚摸均表现出环行肌收缩。替加色罗（10^(-8)-10^(-6) M）对粘膜刺激在口腔和肛门处的收缩最大幅度和曲线下面积均无影响。腔内灌注含替加色罗的液体（10^(-8)-10^(-6) M）以浓度依赖性方式显著增加蠕动波数量（P<0.05）。此外，替加色罗（10^(-8)-10^(-6) M）显著增加蠕动波曲线下面积（P<0.05）。得出的结论是，替加色罗通过增加蠕动期间环行肌收缩的数量对豚鼠回肠具有促动力作用。
