Localization of the 5-HT4 receptor in the human and the guinea pig colon

Effects of Mosapride Citrate, a 5-HT4 Receptor Agonist, on Colonic Motility in Conscious Guinea Pigs

“…Although the distribution of 5-HT4 receptors has been recently established in the colon of guinea pigs (16,17), there are no reports showing that 5-HT4-receptor agonists bind to colonic 5-HT4 receptor sites. Thus, in order to confirm the in vivo effects of mosapride and cisapride, we performed in vitro receptor autoradiography using Recently, selective 5-HT 4 -receptor agonists such as prucalopride and tegaserod, have been demonstrated to facilitate colonic transit and increase stool frequency, and they have been proven valuable for the treatment of slow transit constipation (26).…”

“…Thus, in order to confirm the in vivo effects of mosapride and cisapride, we performed in vitro receptor autoradiography using Recently, selective 5-HT 4 -receptor agonists such as prucalopride and tegaserod, have been demonstrated to facilitate colonic transit and increase stool frequency, and they have been proven valuable for the treatment of slow transit constipation (26). From these findings and the fact that the distribution of 5-HT4 receptors in the colon of guinea pigs is similar to that in the colon of humans (16,17), it is suggested that mosapride enhances colonic motility through 5-HT4-receptor activation in guinea pigs and that this enhancement of colonic motility as well as gastric motility may lead to improvement of constipation in patients with dysfunction of the lower GI motility.…”

“…Recent studies, using in vitro receptor autoradiograms of the stomach and colon have shown that the distribution of 5-HT4 receptors in guinea pigs is similar to that in humans (16,17). In addition, Sakurai-Yamashita et al (16) reported that 5-HT 4 receptors are present in the myenteric plexus and the muscle of both human and guinea pig colon.…”

“…In addition, Sakurai-Yamashita et al (16) reported that 5-HT 4 receptors are present in the myenteric plexus and the muscle of both human and guinea pig colon. These results suggest that the effects of 5-HT4 receptor agonists on colonic motility in the guinea pig are similar to those in humans.…”

Effect of Mosapride Citrate Hydrate on the Colon Cleansing Action of Polyethylene Glycol Electrolyte Lavage Solution (PEG-ELS) in Guinea Pigs

“…It has been reported that mosapride increases gastric emptying in rats and human (16,17) and enhances motility in the upper GI tract of conscious dogs (12,18). Recent studies have indicated that 5-HT 4 receptors are present in the myenteric plexus and the muscle of the stomach and colon of both humans and guinea pigs (19,20). Additionally, using receptor autoradiograms, it was shown that mosapride has high affinity for 5-HT 4 receptors in the colons of guinea pigs (21).…”