Takasaki K, Kishibayashi N, Ishii A, Karasawa A
Department of Pharmacology, Kyowa Hakko Kogyo Co., Ltd., Shizuoka, Japan.
Jpn J Pharmacol. 1994 May;65(1):67-71. doi: 10.1254/jjp.65.67.
The effects of KW-5092, [1-[2-[[[5-(piperidinomethyl)-2- furanyl]methyl]amino]ethyl]-2-imidazolidinylidene]propanedinitr ile fumarate, on the loperamide- or clonidine-induced delayed propulsion were determined in rats and compared with those of other gastroprokinetic agents. Administration of loperamide (0.3 mg/kg, s.c.) or clonidine (0.01 mg/kg, s.c.) induced delay of the evacuation time of the teflon ball, which had been inserted into the distal colon. The delayed evacuation was improved dose-dependently by KW-5092 at 3 to 10 mg/kg (p.o.) or higher. Neostigmine at 0.3 to 3 mg/kg (p.o.) and T-1815 at 1 to 100 mg/kg (p.o.) also improved the delayed ball evacuation. These results suggest that KW-5092 stimulates the delayed colonic propulsion.
在大鼠中测定了富马酸[1-[2-[[[5-(哌啶甲基)-2-呋喃基]甲基]氨基]乙基]-2-咪唑烷亚基]丙二腈（KW-5092）对洛哌丁胺或可乐定诱导的延迟推进作用，并与其他胃肠促动力剂进行了比较。皮下注射洛哌丁胺（0.3mg/kg）或可乐定（0.01mg/kg）会导致插入远端结肠的聚四氟乙烯球排空时间延迟。KW-5092以3至10mg/kg（口服）或更高剂量可剂量依赖性地改善延迟排空。口服新斯的明（0.3至3mg/kg）和T-1815（1至100mg/kg）也可改善球排空延迟。这些结果表明KW-5092可刺激延迟的结肠推进。
