The Pyrazolone Originally Reported to Be a Formyl Peptide Receptor (FPR) 2/ALX-Selective Agonist Is Instead an FPR1 and FPR2/ALX Dual Agonist

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概要

• 論文の詳細を見る

• A pyrazolone compound acting as a formyl peptide receptor (FPR) 2/ALX–selective agonist has been reported, but its pharmacological activities on human FPRs (hFPRs) and mouse FPRs (mFprs) have not been well demonstrated. In this study, we found that this compound, designated as compound A, induced concentration-dependent calcium flux not only in Chinese hamster ovary (CHO) cells expressing hFPR2/ALX but also in cells expressing hFPR1, mFpr1, or mFpr2. It also induced the receptor internalization of hFPR1 and hFPR2/ALX and, accordingly, induced calcium influx and chemotactic responses in both human and mouse neutrophils. Our study revealed that compound A is in fact an FPR1 and FPR2/ALX dual agonist.

• 社団法人 日本薬理学会の論文
• 2009-11-20

著者

• MAEDA Hiroaki

  Biological Research Laboratories, Sankyo Co., Ltd.

• SOGAWA Yoshitaka

  Biological Research Laboratories III, Daiichi Sankyo Co., Ltd.

• SHIMIZUGAWA Akiko

  Exploratory Research Laboratories I, Daiichi Sankyo Co., Ltd.

• OHYAMA Takao

  Exploratory Research Laboratories II, Daiichi Sankyo Co., Ltd.

• HIRAHARA Kazuki

  Biological Research Laboratories III, Daiichi Sankyo Co., Ltd.

• Maeda Hiroaki

  Biological Research Laboratories Sankyo Co. Ltd.

• Hirahara Kazuki

  Biological Research Laboratories Iii Daiichi Sankyo Co. Ltd.

• Shimizugawa Akiko

  Exploratory Research Laboratories I Daiichi Sankyo Co. Ltd.

• Sogawa Yoshitaka

  Cardiovascular-metabolics Research Laboratories Daiichi Sankyo Co. Ltd.

• Ohyama Takao

  Biologics Research Laboratories Daiichi Sankyo Co. Ltd.

• Maeda Hiroaki

  Frontier Research Laboratories Daiichi Sankyo Co. Ltd.

• Maeda Hiroaki

  Biological Research Laboratories III, Daiichi Sankyo Co., Ltd., Japan

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• The Pyrazolone Originally Reported to Be a Formyl Peptide Receptor (FPR) 2/ALX-Selective Agonist Is Instead an FPR1 and FPR2/ALX Dual Agonist
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