A New 5-HT_3 Receptor Ligand. II. Structure-Activity Analysis of 5-HT_3 Receptor Agonist Action in the Gut

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概要

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• Several modified 2-piperazinyl benzoxazole derivatives, which exhibit an agonistic effect on gastrointestinal motility, were synthesized and their effects on the contraction of guinea-pig ileum were examined. The quaternary piperazinyl benzoxazole structure has a restricted conformation and stereostructure compared to those of the other 5-HT_3 receptor agonists, serotonin and meta-chlorophenylbiguanide. The mutual positions of the aromatic ring, nitrogen atom and terminal amine are considered to form the pharmacophore of the 5-HT_3 receptor agonist in the gut. In the serotonin-evoked reflex bradycardia [Bezold-Jarisch (B-J) reflex] inhibition test using rats the B-J reflex-inducing ratio was different for each synthesized compound. These results suggest that, in these 5-HT_3 receptor agonists, the substituents of the benzoxazole ring influence the B-J reflex-inducing activity in rats.

• 公益社団法人日本薬学会の論文
• 1998-03-15

著者

• Kobayashi K

  Pharmaceutical Research Center Meiji Seika Kaisha

• Yamada M

  Pharmaceutical Research Center Meiji Seika Kaisha

• Watanabe T

  Chiba Univ. Chiba Jpn

• YAMADA Megumi

  Pharmaceutical Research Center, Meiji Seika Kaisha

• SATO Yasuo

  Pharmaceutical Research Center, Meiji Seika Kaisha

• KOBAYASHI Kazuko

  Pharmaceutical Research Center, Meiji Seika Kaisha

• KONNO Fukio

  Pharmaceutical Research Center, Meiji Seika Kaisha

• SONEDA Tomoko

  Pharmaceutical Research Center, Meiji Seika Kaisha

• WATANABE Takashi

  Pharmaceutical Research Center, Meiji Seika Kaisha

• Yamada Megumi

  Pharmaceutical Research Center Meiji Seika Kaisha

• Konno F

  Pharmaceutical Research Center Meiji Seika Kaisha

• Konno Fukio

  Pharmaceutical Research Center Meiji Seika Kaisha

• Soneda T

  Pharmaceutical Research Center Meiji Seika Kaisha

• Soneda Tomoko

  Pharmaceutical Research Center Meiji Seika Kaisha

• Kobayashi Kazuko

  Pharmaceutical Research Center Meiji Seika Kaisha

• Sato Yasuo

  Pharmaceutical Research Center Meiji Seika Kaisha

• Watanabe Takashi

  Pharmaceutical Research Center Meiji Seika Kaisha

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