Synthesis and adenosine receptor affinity and potency of 8-alkynyl derivatives of adenosine |
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Authors: | Lambertucci C Costanzi S Vittori S Volpini R Cristalli G |
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Affiliation: | Dipartimento di Scienze Chimiche, University of Camerino, I-62032 Camerino, Italy. |
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Abstract: | Adenosine derivatives bearing different (ar)alkynyl chains at the 8-position were synthesized and tested at human adenosine receptors. Binding studies showed that all compounds possess affinity for the A3 subtype in the high nM range. Moreover, guanosine 5'-O-(3-[35S]thio)triphosphate binding assay indicated that the 8-alkynyl adenosines behaved as antagonists of NECA at A3 receptors. |
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