Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT(2B)/5HT(2C) Serotonin Receptor Antagonists

Adenosine derivatives developed to activate adenosine receptors (ARs) revealed µM activity at serotonin 5HT(2B) and 5HT(2C) receptors (5HTRs). We explored the SAR at 5HT(2)Rs and modeled receptor interactions in order to optimize affinity and simultaneously reduce AR affinity. Depending on N(6) subs...

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Publicado en:J Med Chem
Main Authors: Tosh, Dilip K., Ciancetta, Antonella, Warnick, Eugene, Crane, Steven, Gao, Zhan-Guo, Jacobson, Kenneth A.
Formato: Artigo
Idioma:Inglês
Publicado: 2016
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Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC5201133/
https://ncbi.nlm.nih.gov/pubmed/27933810
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.6b01183
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