論文 - 詳細
| RRC ID | 6544 |
|---|---|
| 著者 | Muntasir HA, Hossain M, Bhuiyan MA, Komiyama T, Nakamura T, Ozaki M, Nagatomo T. |
| タイトル | Identification of a key amino acid of the human 5-HT(2B) serotonin receptor important for sarpogrelate binding. |
| ジャーナル | J Pharmacol Sci |
| Abstract |
Based on radio-ligand binding and molecular modeling studies, sarpogrelate shows a moderate selectivity for 5-HT(2B) versus 5-HT(2A) receptors. To confirm the modeling data of sarpogrelate to 5-HT(2B) receptors predicting interaction of sarpogrelate towards Asp135 in helix 3 of 5-HT(2B) receptors, we constructed and characterized the mutation of this residue by site-directed mutagenesis. The Asp135Ala mutant did not exhibit any affinity for [(3)H]rauwolscine. Therefore, it was not possible to find sarpogrelate affinity to the mutant using [(3)H]rauwolscine. The mutation also abolished agonist-stimulated inositol phosphates formation. These results provide evidence that Asp135 is important for the interaction between 5-HT(2B) receptors and sarpogrelate. |
| 巻・号 | 104(3) |
| ページ | 274-7 |
| 公開日 | 2007-7-1 |
| DOI | 10.1254/jphs.sc0060241 |
| PII | JST.JSTAGE/jphs/SC0060241 |
| PMID | 17609583 |
| MeSH | Amino Acids / metabolism* Blotting, Western Cell Line Cells, Cultured Cyproheptadine / pharmacology Humans Indoles / pharmacology Inositol Phosphates / metabolism Mutagenesis, Site-Directed Pyridines / pharmacology Radioligand Assay Receptor, Serotonin, 5-HT2B / drug effects* Receptor, Serotonin, 5-HT2B / genetics Serotonin Antagonists / metabolism* Succinates / metabolism* Yohimbine / metabolism |
| IF | 2.835 |
| 引用数 | 7 |
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オルトメトリクス指標項目
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