title: Inhibition of small intestine motility by cromakalim (BRL 34915).
abstract: The effects of the potassium channel activator, cromakalim, on intestine motility were investigated. In vitro, cromakalim inhibits the peristaltic reflex, with the action on longitudinal muscle (pIC50 = 5.8 +/- 0.1) being more potent than that on circular muscle (pIC50 = 4.8 +/- 0.2). In vivo, a half maximal inhibition of small intestinal transit occurred at 1.2 mg/kg (i.p.). These results demonstrate that different gut muscle layers show a different sensitivity to cromakalim and that small intestine smooth muscle is less sensitive to cromakalim than vascular smooth muscle.
authors.affiliation: Preclinical Research, Sandoz Ltd., Basel, Switzerland.
authors.forename: K H
authors.initials: KH
authors.lastname: Buchheit
authors.forename: A
authors.initials: A
authors.lastname: Bertholet
mesh_terms: D000818:Animals; D001578:Benzopyrans / Q000494:pharmacology*; D003000:Clonidine / Q000031:analogs & derivatives / Q000494:pharmacology; D019806:Cromakalim; D005769:Gastrointestinal Motility / Q000187:drug effects*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007421:Intestine, Small / Q000187:drug effects / Q000502:physiology; D008139:Loperamide / Q000494:pharmacology; D008297:Male; D051379:Mice; D010528:Peristalsis / Q000187:drug effects; D015221:Potassium Channels / Q000187:drug effects / Q000502:physiology; D011758:Pyrroles / Q000494:pharmacology*
chemical_list: D001578:Benzopyrans; D015221:Potassium Channels; D011758:Pyrroles; D019806:Cromakalim; C023754:tizanidine; D008139:Loperamide; D003000:Clonidine