The Pyrazolone Originally Reported to Be a Formyl Peptide Receptor (FPR) 2/ALX–Selective Agonist Is Instead an FPR1 and FPR2/ALX Dual Agonist
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 co...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2009-01-01
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| Series: | Journal of Pharmacological Sciences |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1347861319310990 |
| _version_ | 1828394531078275072 |
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| author | Yoshitaka Sogawa Akiko Shimizugawa Takao Ohyama Hiroaki Maeda Kazuki Hirahara |
| author_facet | Yoshitaka Sogawa Akiko Shimizugawa Takao Ohyama Hiroaki Maeda Kazuki Hirahara |
| author_sort | Yoshitaka Sogawa |
| collection | DOAJ |
| description | 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. Keywords:: formyl peptide receptor, neutrophil, chemotaxis |
| first_indexed | 2024-12-10T07:55:55Z |
| format | Article |
| id | doaj.art-49539a54f92b4e53aac32c8aeda4538d |
| institution | Directory Open Access Journal |
| issn | 1347-8613 |
| language | English |
| last_indexed | 2024-12-10T07:55:55Z |
| publishDate | 2009-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Journal of Pharmacological Sciences |
| spelling | doaj.art-49539a54f92b4e53aac32c8aeda4538d2022-12-22T01:56:54ZengElsevierJournal of Pharmacological Sciences1347-86132009-01-011113317321The Pyrazolone Originally Reported to Be a Formyl Peptide Receptor (FPR) 2/ALX–Selective Agonist Is Instead an FPR1 and FPR2/ALX Dual AgonistYoshitaka Sogawa0Akiko Shimizugawa1Takao Ohyama2Hiroaki Maeda3Kazuki Hirahara4Biological Research Laboratories III, 1-16-13 Kitakasai, Edogawa-ku, Tokyo 134-8630, JapanExploratory Research Laboratories I, 1-16-13 Kitakasai, Edogawa-ku, Tokyo 134-8630, JapanExploratory Research Laboratories II, Daiichi Sankyo Co., Ltd., 1-16-13 Kitakasai, Edogawa-ku, Tokyo 134-8630, JapanBiological Research Laboratories III, 1-16-13 Kitakasai, Edogawa-ku, Tokyo 134-8630, JapanBiological Research Laboratories III, 1-16-13 Kitakasai, Edogawa-ku, Tokyo 134-8630, Japan; Corresponding author. hirahara.kazuki.s2@daiichisankyo.co.jpA 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. Keywords:: formyl peptide receptor, neutrophil, chemotaxishttp://www.sciencedirect.com/science/article/pii/S1347861319310990 |
| spellingShingle | Yoshitaka Sogawa Akiko Shimizugawa Takao Ohyama Hiroaki Maeda Kazuki Hirahara The Pyrazolone Originally Reported to Be a Formyl Peptide Receptor (FPR) 2/ALX–Selective Agonist Is Instead an FPR1 and FPR2/ALX Dual Agonist Journal of Pharmacological Sciences |
| title | The Pyrazolone Originally Reported to Be a Formyl Peptide Receptor (FPR) 2/ALX–Selective Agonist Is Instead an FPR1 and FPR2/ALX Dual Agonist |
| title_full | The Pyrazolone Originally Reported to Be a Formyl Peptide Receptor (FPR) 2/ALX–Selective Agonist Is Instead an FPR1 and FPR2/ALX Dual Agonist |
| title_fullStr | The Pyrazolone Originally Reported to Be a Formyl Peptide Receptor (FPR) 2/ALX–Selective Agonist Is Instead an FPR1 and FPR2/ALX Dual Agonist |
| title_full_unstemmed | The Pyrazolone Originally Reported to Be a Formyl Peptide Receptor (FPR) 2/ALX–Selective Agonist Is Instead an FPR1 and FPR2/ALX Dual Agonist |
| title_short | The Pyrazolone Originally Reported to Be a Formyl Peptide Receptor (FPR) 2/ALX–Selective Agonist Is Instead an FPR1 and FPR2/ALX Dual Agonist |
| title_sort | pyrazolone originally reported to be a formyl peptide receptor fpr 2 alx selective agonist is instead an fpr1 and fpr2 alx dual agonist |
| url | http://www.sciencedirect.com/science/article/pii/S1347861319310990 |
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