Effect of KW-5092 ([1-[2-[[[5-(piperidinomethyl)-2-furanyl]methyl]amino]ethyl]-2- imidazolidinylidene]propanedinitrile fumarate) on intestinal motility and release of endogenous acetylcholine (ACh) were measured simultaneously in the small intestine of anesthetized dog using the in vivo microdialysis method. Intraarterial and intravenous administrations of KW-5092 accelerated the intestinal motility and increased dialysate ACh concentrations. These KW-5092-induced responses paralleled the increase in blood concentration of KW-5092. Thus, the acceleration of intestinal motility by KW-5092 was found in vivo to be associated with an increase in ACh release from the intestinal cholinergic neurons.

01 Jun 1999·European Journal of PharmacologyQ3 · MEDICINE

KW-5092, a novel gastrokinetic agent, facilitates luminal serotonin release from the guinea-pig colon

Q3 · MEDICINE

Article

Author: Kojima, S

The present study was designed to determine the influence of KW-5092 ((1-[2-[[[5-(piperidinomethyl)-2-furanyl]methyl]amino]ethyl]-2- imidazolidinylidene) propanedinitrile fumarate), a novel gastroprokinetic agent on intraluminal serotonin (5-hydroxytryptamine, 5-HT) release which reflects the release of 5-HT from enterochromaffin cells, using the luminally perfused isolated guinea-pig proximal colon in vitro. 5-HT was determined by high-performance liquid chromatography with electrochemical detection. KW-5092 (1-10 microM) concentration-dependently caused an increase in the luminal 5-HT outflow. In the presence of atropine (0.2 microM) or tetrodotoxin (0.3 microM), the stimulatory action of KW-5092 (10 microM) was inhibited by 94% and 74%, respectively. These results suggest that KW-5092 stimulates intraluminal 5-HT release from luminally perfused proximal colon of the guinea-pig via the stimulation of cholinergic neurons. Because 5-HT is recognized as an important messenger substance in the control of intestinal motility, this stimulatory effect could be considered as an indirect action of KW-5092 that may contribute to its prokinetic effects.

01 Sep 1998·Journal of Pharmacy and PharmacologyQ3 · MEDICINE

Effects of KW-5092 on Antroduodenal Coordination and Gastric Emptying in Guinea-pigs

Q3 · MEDICINE

Article

Author: Kishibayashi, N ; Karasawa, A

AbstractKW-5092 (2-[1-[2-[[5-(piperidinomethyl)-2-furanyl]methylamino]ethyl]imidazonylidin-2-ylidenene]malononitrile fumarate) is a novel gastroprokinetic agent with both acetylcholine release facilitatory and acetylcholinesterase inhibitory activity. We have investigated the effects of KW-5092 on antroduodenal coordination and gastric emptying in guinea-pigs.In the guinea-pig isolated gastroduodenal preparation, KW-5092 at 3 times 10−7 to 3 times 10−6 M significantly increased antroduodenal coordination. The effect of KW-5092 was almost completely inhibited by atropine or tetrodotoxin. Cisapride, a gastroprokinetic agent with acetylcholine release facilitatory activity, also increased coordination whereas neither acetylcholine nor the acetylcholinesterase inhibitor neostigmine affected it. In-vivo, KW-5092 and cisapride enhanced gastric emptying whereas neostigmine delayed it.These results suggest that acetylcholine release facilitation, but not acetylcholinesterase inhibition, is involved in the enhancement by KW-5092 of antroduodenal coordination and gastric emptying.

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Indication	Highest Phase	Country/Location	Organization	Date
Gastroesophageal Reflux	Phase 2	JP	Kyowa Kirin Co., Ltd.	-
Gastroesophageal Reflux	Phase 2	JP	Kyowa Hakko Bio Co., Ltd.	-

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