新規ジヒドロベンゾキサジンカルボキサミド誘導体,Y-25130のセロトニン3受容体への親和性

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概要

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• The binding of Y-25130 on serotonin 3 (5-HT<SUB>3</SUB>) receptors was evaluated by examining its effect on <SUP>3</SUP>H-BRL 43694 (<SUP>3</SUP>H-granisetron) binding to rat cerebral cortex membranes in comparison with those of granisetron, ondansetron and metoclopramide. Y-25130, granisetron, ondansetron, metoclopramide, 5-HT and 2-methyl-5-HT displaced the specific binding of <SUP>3</SUP>H-granisetron to the synaptosomal membranes in a concentration-dependent manner. The rank order of potency for inhibition of <SUP>3</SUP>H-granisetron binding by the test compounds was Y-25130≅granisetron > ondansetron> 2-methyl- 5-HT≅5-HT≅metoclopramide. To determine the manner of interaction between Y-25130 and 5-HT<SUB>3</SUB> receptors, Scatchard analysis of <SUP>3</SUP>H-granisetron specific binding to the membranes of the cerebral cortex in the absence or presence of various concentrations of Y-25130 was performed. It was indicated that Y-25130 exerted a typical competitive-type inhibition of <SUP>3</SUP>H-granisetron binding. The present study indicates that Y-25130 binds competitively to 5-HT<SUB>3</SUB> receptors with high affinity.

• 社団法人 日本薬理学会の論文

著者

• 竹原 修造

  吉富製薬・中央研

• 酒盛 政光

  Research Laboratories Yoshitomi Pharmaceutical Industries Ltd.

• 酒盛 政光

  吉富製薬 (株) 中央研究所

• 竹原 修造

  吉富製薬 (株) 中央研究所

• 瀬戸口 通英

  吉富製薬 (株) 中央研究所

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• 新規ジヒドロベンゾキサジンカルボキサミド誘導体,Y-25130のセロトニン3受容体への親和性
• 新規ジヒドロベンゾキサジンカルボキサミド誘導体,Y-25130のセロトニン3受容体への親和性

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