Identification of SK-951, a Novel Benzofuran Derivative, as an Agonist to 5-HT_4 Receptors
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概要
- 論文の詳細を見る
The pharmacological profile 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) was identified in relation to serotonin 5-HT3 and 5-HT4 receptors by the receptor binding assay and functional studies. The receptor binding assay showed that SK-951 bound to the 5-HT3 receptor with a high affinity, to the 5-HT4 receptor with relatively higher affinity and to the muscarinic M2 receptor with a low affinity, but not to dopamine D1 and D2 and serotonin 5-HT1 and 5-HT2 and muscarinic M1 and M3 receptors. SK-951 caused relaxations of tunica muscularis mucosae preparations from rat esophagus which were precontracted with carbachol, and the effects were antagonized by GR113808, a selective 5-HT4 antagonist. In the longitudinal muscle with myenteric plexus (LMMP) preparations from guinea pig ileum, SK-951 enhanced the electrically-stimulated contraction of preparations in which the 5-HT1, 5-HT2 and 5-HT3 receptors were blocked, and it enhanced the electrically-stimulated release of [3H]acetylcholine (ACh). These effects of SK-951 were antagonized by GR113808. SK-951 inhibited the 5-HT3 receptor-mediated contractions. These results indicate that SK-951 possesses properties of an agonist for the 5-HT4 receptor and an antagonist for the 5HT3 receptor. Thus, SK-951 is a new and potent 5-HT4-receptor agonist and causes contractions of guinea pig ileum mediated by enhancement of ACh release via the 5-HT4 receptor.
- 社団法人 日本薬理学会の論文
- 1999-02-01
著者
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TANIYAMA Kohtaro
Departments of Pharmacology
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Taniyama K
Nagasaki Univ. Graduate School Of Biomedical Sci. Nagasaki Jpn
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Taniyama Kohtaro
Division Of Pharmacology Department Of Translational Medical Sciences Nagasaki University Graduate S
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Taniyama Kohtaro
Department Of Pharmacology Nagasaki University Graduate School Of Biomedical Sciences
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Taniyama K
Division Of Pharmacology Department Of Translational Medical Sciences Nagasaki University Graduate S
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Takemura Keiko
Department Of Pharmacology Nagasaki University School Of Medicine
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Takeda M
Pharmaceutical Laboratory Sanwa Kagaku Kenkyusho Co. Ltd
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Takeda Motohiro
Pharmaceutical Laboratory Sanwa Kagaku Kenkyusho Co. Ltd.
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SUZUKI Tsunemasa
Pharmaceutical Laboratory, Sanwa Kagaku Kenkyusho Co., Ltd.,
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Suzuki T
Pharmaceutical Laboratory Sanwa Kagaku Kenkyusho Co. Ltd
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Suzuki Tsunemasa
Pharmaceutical Laboratory Sanwa Kagaku Kenkyusho Co. Ltd.
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TSUKAMOTO Katsura
Pharmaceutical Laboratory, Sanwa Kagaku Kenkyusho Co., Ltd.,
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MIZUTANI Yuka
Pharmaceutical Laboratory, Sanwa Kagaku Kenkyusho Co., Ltd.
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Mizutani Yuka
Pharmaceutical Laboratory Sanwa Kagaku Kenkyusho Co. Ltd.
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Tsukamoto Katsura
Pharmaceutical Laboratory Sanwa Kagaku Kenkyusho Co. Ltd
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Takeda Motohiko
Pharmaceutical Laboratory, Sanwa Kagaku Kenkyusho Co., Ltd.
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Taniyama Kohtaro
Department of Pharmacology 2, Nagasaki University School of Medicine
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