Effects of SK-951, a Benzofuran Derivative, as a Prokinetic Agent in Rats and Dogs.
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- Takeda Motohiro
- Pharmaceutical Laboratory, Sanwa Kagaku Kenkyusho Co., Ltd.
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- Tsukamoto Katsura
- Pharmaceutical Laboratory, Sanwa Kagaku Kenkyusho Co., Ltd.
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- Yamano Masaya
- Pharmaceutical Laboratory, Sanwa Kagaku Kenkyusho Co., Ltd.
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- Uesaka Hiroshi
- Pharmaceutical Laboratory, Sanwa Kagaku Kenkyusho Co., Ltd.
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Description
The gastrokinetic activity of SK-951 ((-)4-amino-N-[2-(1-azabicyclo[3.3.0]octan-5-yl)ethyl]-5-chloro-2, 3-dihydro-2-methylbenzo[b]furan-7-carboxamide hemifumarate), a benzofuran derivative with 5-hydroxytryptamine (5-HT)4-receptor agonist activity, was studied in rats and dogs. The effects of SK-951 were also investigated in a model of vagotomy-induced gastroparesis in comparison with cisapride. In rats, both SK-951 and cisapride enhanced gastric emptying of liquids (phenol red) at a dose of 1 - 100 mg/kg, p.o. Gastric emptying of liquid (acetaminophen) in fasted beagle dogs was enhanced significantly by SK-951 (1.0 mg/kg, i.v.), whereas the effect of cisapride (0.2 - 1.0 mg/kg, i.v.) was not statically significant. Similar results were found when radiopaque markers were given with standard meal to dogs with vagotomy-induced gastroparesis. The delayed gastric emptying of radiopaque markers by vagotomy was reversed by SK-951 (1.0 mg/kg, i.v.), whereas cisapride showed no effect at doses from 0.1 to 1.0 mg/kg, i.v. These results indicated that oral and intravenous administration of SK-951 accelerates gastric emptying of both liquids and solids in animal models. Thus, SK-951 may be a highly potent and useful prokinetic agent in comparison to cisapride.
Journal
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- The Japanese Journal of Pharmacology
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The Japanese Journal of Pharmacology 81 (3), 292-297, 1999
The Japanese Pharmacological Society
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Details 詳細情報について
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- CRID
- 1390001204285644672
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- NII Article ID
- 10008197286
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- NII Book ID
- AA00691188
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- COI
- 1:CAS:528:DyaK1MXns1Gntb4%3D
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- ISSN
- 13473506
- 00215198
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- NDL BIB ID
- 4918323
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- PubMed
- 10622218
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed