| Autor: |
Habib Abul Muntasir, Murad Hossain, Mohiuddin Ahmed Bhuiyan, Tadazumi Komiyama, Takashi Nakamura, Masanobu Ozaki, Takafumi Nagatomo |
| Jazyk: |
angličtina |
| Rok vydání: |
2007 |
| Předmět: |
|
| Zdroj: |
Journal of Pharmacological Sciences, Vol 104, Iss 3, Pp 274-277 (2007) |
| Druh dokumentu: |
article |
| ISSN: |
1347-8613 |
| DOI: |
10.1254/jphs.SC0060241 |
| Popis: |
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. Keywords:: 5-HT2B receptor, sarpogrelate, site-directed mutagenesis |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
|
