Identification of a Key Amino Acid of the Human 5-HT2B Serotonin Receptor Important for Sarpogrelate Binding
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 constr...
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| Main Authors: | , , , , , , |
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| Format: | Book |
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Elsevier,
2007-01-01T00:00:00Z.
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|---|---|---|---|
| 001 | doaj_ea6f7292e4fd4e53a7f7516a8e6c17ce | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Habib Abul Muntasir |e author |
| 700 | 1 | 0 | |a Murad Hossain |e author |
| 700 | 1 | 0 | |a Mohiuddin Ahmed Bhuiyan |e author |
| 700 | 1 | 0 | |a Tadazumi Komiyama |e author |
| 700 | 1 | 0 | |a Takashi Nakamura |e author |
| 700 | 1 | 0 | |a Masanobu Ozaki |e author |
| 700 | 1 | 0 | |a Takafumi Nagatomo |e author |
| 245 | 0 | 0 | |a Identification of a Key Amino Acid of the Human 5-HT2B Serotonin Receptor Important for Sarpogrelate Binding |
| 260 | |b Elsevier, |c 2007-01-01T00:00:00Z. | ||
| 500 | |a 1347-8613 | ||
| 500 | |a 10.1254/jphs.SC0060241 | ||
| 520 | |a 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 | ||
| 546 | |a EN | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Journal of Pharmacological Sciences, Vol 104, Iss 3, Pp 274-277 (2007) | |
| 787 | 0 | |n http://www.sciencedirect.com/science/article/pii/S1347861319342537 | |
| 787 | 0 | |n https://doaj.org/toc/1347-8613 | |
| 856 | 4 | 1 | |u https://doaj.org/article/ea6f7292e4fd4e53a7f7516a8e6c17ce |z Connect to this object online. |