Affinity of Mosapride Citrate, a New Gastroprokinetic Agent,for 5-HT4 Receptors in Guinea Pig Ileum

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概要

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• We examined the binding affinity of mosapride citrate (mosapride) (4-amino-5-chloro-2-ethoxy-N-｛[4-(4-fluorobenzyl)-2-morpholinyl]methyl｝benzamide citrate), a novel gastroprokinetic agent, for the 5-hydroxytryptamine (5-HT) 4 receptors in guinea pig ileum using a selective 5-HT4-receptor radioligand, [3H]GR113808. In membrane preparations from longitudinal muscle with myenteric plexus in guinea pig ileum, specific [3H]GR113808 binding revealed a single saturable site of high affinity (Kd=0.28±0.02 nM, Bmax=45±3 fmol/mg protein). Mosapride and other 5-HT4-receptor agonists inhibited the specific binding of [3H]GR113808 in guinea pig ileum. The 5-HT4 agonists examined displayed the following inhibition potency order: BIMU-8 > cisapride > mosapride > renzapride > 5-HT > zacopride > metoclopramide. Mosapride exhibited monophasic inhibition of the specific [3H]GR113808 binding in the ileum (Ki value: 84.2 nM). The presence of mosapride (30 nM) significantly increased the Kd value to 0.44±0.05 nM in the Scatchard analysis of [3H]GR113808 binding. Bmax of [3H]GR113808, however, was not affected (48±4 fmol/mg protein) by mosapride. As for the affinity of mosapride, the addition of GppNHp (100 μM) slightly increased the Ki value to 104 nM. These results indicate that mosapride has an affinity for 5-HT4 receptors in guinea pig ileum in the radioligand binding study.

• 社団法人 日本薬理学会の論文
• 1998-05-01

著者

• YOSHIDA Naoyuki

  Discovery Pharmacology II Group, Pharmacolgy & Microbiology Research Laboratories, Dainippon Pharmac

• MINE Yukiko

  Discovery Pharmacology II, Pharmacology Research Laboratories, Dainippon Sumitomo Pharma Co., Ltd.

• Mine Yukiko

  Discovery Research Laboratories / Dainippon Pharmaceutical Co. Ltd.

• Hosoki K

  Discovery Research Laboratories / Dainippon Pharmaceutical Co. Ltd.

• Yoshida Naoyuki

  Discovery Pharmacology Ii Group Pharmacolgy & Microbiology Research Laboratories Dainippon Pharm

• Yoshida Naoyuki

  Discovery Pharmacology Ii Pharmacology Res. Laboratories Dainippon Sumitomo Pharma Co. Ltd. Jpn

• Mine Yukiko

  Discovery Pharmacology Ii Pharmacology Res. Laboratories Dainippon Sumitomo Pharma Co. Ltd. Jpn

• YOSHIZAWA Takashi

  Discovery Research Laboratories /, Dainippon Pharmaceutical Co., Ltd.

• HOSOKI Kanoo

  Discovery Research Laboratories /, Dainippon Pharmaceutical Co., Ltd.

• Yoshikawa Takashi

  Discovery Pharmacology Ii Group Pharmacolgy & Microbiology Research Laboratories Dainippon Pharm

• Yoshizawa Takashi

  Discovery Research Laboratories / Dainippon Pharmaceutical Co. Ltd.

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