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Toward Biophysical Probes for the 5-HT(3) Receptor: Structure−Activity Relationship Study of Granisetron Derivatives
[Image: see text] This report describes the synthesis and biological characterization of novel granisetron derivatives that are antagonists of the human serotonin (5-HT(3)A) receptor. Some of these substituted granisetron derivatives showed low nanomolar binding affinity and allowed the identificati...
| Autores principales: | , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical Society
2010
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4166935/ https://www.ncbi.nlm.nih.gov/pubmed/20146481 http://dx.doi.org/10.1021/jm901827x |
| _version_ | 1782335349190557696 |
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| author | Vernekar, Sanjeev Kumar V. Hallaq, Hasan Y. Clarkson, Guy Thompson, Andrew J. Silvestri, Linda Lummis, Sarah C. R. Lochner, Martin |
| author_facet | Vernekar, Sanjeev Kumar V. Hallaq, Hasan Y. Clarkson, Guy Thompson, Andrew J. Silvestri, Linda Lummis, Sarah C. R. Lochner, Martin |
| author_sort | Vernekar, Sanjeev Kumar V. |
| collection | PubMed |
| description | [Image: see text] This report describes the synthesis and biological characterization of novel granisetron derivatives that are antagonists of the human serotonin (5-HT(3)A) receptor. Some of these substituted granisetron derivatives showed low nanomolar binding affinity and allowed the identification of positions on the granisetron core that might be used as attachment points for biophysical tags. A BODIPY fluorophore was appended to one such position and specifically bound to 5-HT(3)A receptors in mammalian cells. |
| format | Online Article Text |
| id | pubmed-4166935 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2010 |
| publisher | American Chemical Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-41669352014-09-19 Toward Biophysical Probes for the 5-HT(3) Receptor: Structure−Activity Relationship Study of Granisetron Derivatives Vernekar, Sanjeev Kumar V. Hallaq, Hasan Y. Clarkson, Guy Thompson, Andrew J. Silvestri, Linda Lummis, Sarah C. R. Lochner, Martin J Med Chem [Image: see text] This report describes the synthesis and biological characterization of novel granisetron derivatives that are antagonists of the human serotonin (5-HT(3)A) receptor. Some of these substituted granisetron derivatives showed low nanomolar binding affinity and allowed the identification of positions on the granisetron core that might be used as attachment points for biophysical tags. A BODIPY fluorophore was appended to one such position and specifically bound to 5-HT(3)A receptors in mammalian cells. American Chemical Society 2010-02-10 2010-03-11 /pmc/articles/PMC4166935/ /pubmed/20146481 http://dx.doi.org/10.1021/jm901827x Text en Copyright © 2010 American Chemical Society Terms of Use CC-BY (http://pubs.acs.org/page/policy/authorchoice_ccby_termsofuse.html) |
| spellingShingle | Vernekar, Sanjeev Kumar V. Hallaq, Hasan Y. Clarkson, Guy Thompson, Andrew J. Silvestri, Linda Lummis, Sarah C. R. Lochner, Martin Toward Biophysical Probes for the 5-HT(3) Receptor: Structure−Activity Relationship Study of Granisetron Derivatives |
| title | Toward Biophysical Probes for the 5-HT(3) Receptor: Structure−Activity Relationship Study of Granisetron Derivatives |
| title_full | Toward Biophysical Probes for the 5-HT(3) Receptor: Structure−Activity Relationship Study of Granisetron Derivatives |
| title_fullStr | Toward Biophysical Probes for the 5-HT(3) Receptor: Structure−Activity Relationship Study of Granisetron Derivatives |
| title_full_unstemmed | Toward Biophysical Probes for the 5-HT(3) Receptor: Structure−Activity Relationship Study of Granisetron Derivatives |
| title_short | Toward Biophysical Probes for the 5-HT(3) Receptor: Structure−Activity Relationship Study of Granisetron Derivatives |
| title_sort | toward biophysical probes for the 5-ht(3) receptor: structure−activity relationship study of granisetron derivatives |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4166935/ https://www.ncbi.nlm.nih.gov/pubmed/20146481 http://dx.doi.org/10.1021/jm901827x |
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