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https://hdl.handle.net/10216/95283| Author(s): | José Enrique Rodríguez-Borges Xerardo García-Mera María Carmen Balo José Brea Olga Caamaño Franco Fernández Carmen López María Isabel Loza María Isabel Nieto |
| Title: | Synthesis and pharmacological evaluation of novel 1,3,8- and 1,3,7,8-substituted xanthines as adenosine receptor antagonists |
| Issue Date: | 2010 |
| Abstract: | A number of novel xanthines bearing a variety of substituents at positions 1, 3, 7 and 8 were prepared and evaluated for their binding affinity to the human adenosine receptor A1, A2A, A2B and A3 subtypes. Several of the 1,3,8- and 1,3,7,8-substituted xanthines showed moderate-to-high affinity at human A2B and A1 receptors, with the most active compound (14q) having a pKi of 7.57 nM for hA2B receptors and a selectivity over hA2A receptors of 8.1-fold and hA1 receptors of 3.7-fold. |
| Subject: | Química orgânica, Química clínica, Engenharia química Organic chemistry, Clinical chemistry, Chemical engineering |
| Scientific areas: | Ciências da engenharia e tecnologias::Engenharia química Engineering and technology::Chemical engineering |
| URI: | https://hdl.handle.net/10216/95283 |
| Document Type: | Artigo em Revista Científica Internacional |
| Rights: | restrictedAccess |
| Appears in Collections: | FCUP - Artigo em Revista Científica Internacional |
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| File | Description | Size | Format | |
|---|---|---|---|---|
| 48313.pdf Restricted Access | 333.15 kB | Adobe PDF | Request a copy from the Author(s) |
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