Prokinetic actions of luminally acting 5-HT₄ receptor agonists.

ABSTRACT:

Background

5-HT₄ receptor (5-HT₄ R) agonists exert prokinetic actions in the GI tract, but non-selective actions and potential for stimulation of non-target 5-HT₄ Rs have limited their use. Since 5-HT₄ Rs are expressed in the colonic epithelium and their stimulation accelerates colonic propulsion in vitro, we tested whether luminally acting 5-HT₄ R agonists promote intestinal motility.

Methods

Non-absorbed 5-HT₄ R agonists, based on prucalopride and naronapride, were assessed for potency at the 5-HT₄ R in vitro, and for tissue and serum distribution in vivo in mice. In vivo assessment of prokinetic potential included whole gut transit, colonic motility, fecal output, and fecal water content. Colonic

SUBMITTER: Konen JR 

PROVIDER: S-EPMC7990683 | biostudies-literature | 2021 Apr

REPOSITORIES: biostudies-literature