Identification of a Key Amino Acid of the Human 5-HT2B Serotonin Receptor Important for Sarpogrelate Binding
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概要
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Based on radio-ligand binding and molecular modeling studies, sarpogrelate shows a moderate selectivity for 5-HT2B versus 5-HT2A receptors. To confirm the modeling data of sarpogrelate to 5-HT2B receptors predicting interaction of sarpogrelate towards Asp135 in helix 3 of 5-HT2B receptors, we constructed and characterized the mutation of this residue by site-directed mutagenesis. The Asp135Ala mutant did not exhibit any affinity for [3H]rauwolscine. Therefore, it was not possible to find sarpogrelate affinity to the mutant using [3H]rauwolscine. The mutation also abolished agonist-stimulated inositol phosphates formation. These results provide evidence that Asp135 is important for the interaction between 5-HT2B receptors and sarpogrelate.
- 社団法人 日本薬理学会の論文
著者
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Nakamura Takashi
Department of Cardiology, Saiseikai Shigaken Hospital
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Ozaki Masanobu
Department of Toxicology, Niigata University of Pharmacy and Applied Life Science
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BHUIYAN Mohiuddin
Department of Pharmacology, Niigata University of Pharmacy and Applied Life Sciences
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HOSSAIN Murad
Department of Pharmacology, Niigata University of Pharmacy and Applied Life Sciences
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NAGATOMO Takafumi
Department of Pharmacology, Niigata University of Pharmacy and Applied Life Sciences
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KOMIYAMA Tadazumi
Department of Biochemistry, Niigata College of Pharmacy
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Ozaki Masanobu
Department Of Cardiology Fukuoka University School Of Medicine
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MUNTASIR Habib
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Niigata University of Pharmacy and A
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Muntasir Habib
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
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Nagatomo Takafumi
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
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Komiyama Tadazumi
Department Of Biochemistry Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
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Bhuiyan Mohiuddin
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
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Hossain Murad
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
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Nakamura Takashi
Department Of Cardiology Saiseikai Shiga Hospital
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Muntasir Habib
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Niigata University of Pharmacy and Applied Life Sciences, Japan
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