Enhancement by KW-5092, a Novel Gastroprokinetic Agent, of the Gastrointestinal Motor Activity in Dogs.
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概要
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KW-5092({1-[2-[[[5-(piperidinomethyl)-2-furanyl]methyl]amino]ethyl]-2-imidazolidinylidene} propanedinitrile fumarate) is a novel gastroprokinetic agent with acetylcholinesterase (AChE) inhibitory activity and acetylcholine (ACh) release facilitatory activity. The present study examined the effects of KW-5092 on gastrointestinal (GI) motor activity in dogs. In anesthetized dogs, KW-5092 at 0.03 to 1 mg/kg, i.v. dose-dependently enhanced the gastric antral and the colonic motor activity. Neostigmine, an AChE inhibitor, enhanced the motor activity at 0.03 and 0.1 mg/kg, i.v. Ranitidine, a histamine H<SUB>2</SUB>-receptor antagonist with AChE inhibitory activity and ACh release facilitatory activity, enhanced the motor activity but decreased blood pressure at 1 to 10 mg/kg, i.v. In conscious dogs, KW-5092 at 0.03 to 1 mg/kg, i.v. or 1 to 10 mg/kg, p.o. dose-dependently enhanced the gastric antral, duodenal, ileal and the colonic motor activities. Neostigmine at 0.1 mg/kg, i.v. or 3 mg/kg, p.o. enhanced the duodenal, ileal and colonic motor activities, but induced excitement, slavering, vomiting and diarrhea. Ranitidine at 3 mg/kg, i.v. enhanced the gastric antral and colonic motor activities, but induced collapse or akinesia. The present results suggest that KW-5092 enhances the GI motor activity in a wide range from the gastric antrum to the colon and does not induce behavioral and cardiovascular side effects. KW-5092 may be a useful drug for the treatment of GI motility dysfunctions.
- 公益社団法人 日本薬理学会の論文
著者
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Kitazawa Takio
Department Of Biosciences School Of Veterinary Medicine Rakuno Gakuen University
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Tomaru Atsushi
Department Of Pharmacology Pharmaceutical Research Laboratories Kyowa Hakko Kogyo Co. Ltd.
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Karasawa Akira
Deparment Of Pharmacology Pharmaceutical Research Laboratories Kyowa Hakko Kogyo Co. Ltd.
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Kishibayashi Nobuyuki
Deparment Of Pharmacology Pharmaceutical Research Laboratories Kyowa Hakko Kogyo Co. Ltd.
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Ishii Akio
Department Of Mechanical Science And Bioengineering Graduate School Of Engineering Science Osaka University
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Kitazawa Takio
Department of Pharmacology, Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd.
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SHUTO Katsuichi
Department of Cardiovascular Pharmacology, Pharmaceuticals Research Laboratories, Kyowa Hakko Kogyo Co., Ltd.
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Ichikawa Shunji
Department of Pharmacology, Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd.
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