SYNTHESIS AND ADENOSINE RECEPTOR AFFINITY AND POTENCY OF 8-ALKYNYL DERIVATIVES OF ADENOSINE

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.

ACKNOWLEDGMENTS

Supported by EC Contract No BMH4-98-3474 and by a grant from the University of Camerino (Fondo di Ricerca di Ateneo).