Buchheit K H, Bertholet A
Preclinical Research, Sandoz Ltd., Basel, Switzerland.
Eur J Pharmacol. 1988 Sep 23;154(3):335-7. doi: 10.1016/0014-2999(88)90211-7.
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.
研究了钾通道激活剂克罗卡林对肠道运动的影响。在体外,克罗卡林抑制蠕动反射,对纵行肌的作用(pIC50 = 5.8 ± 0.1)比对环行肌的作用(pIC50 = 4.8 ± 0.2)更强。在体内,腹腔注射1.2 mg/kg时小肠转运受到半数最大抑制。这些结果表明,肠道不同肌肉层对克罗卡林的敏感性不同,且小肠平滑肌对克罗卡林的敏感性低于血管平滑肌。