A new series of 2-aralkynyl-N6-methyl-MECAs 10-13 were synthesized and evaluated in radioligand binding studies and in a newEu-GTP functional assay that provides a powerful alternative to radioisotope use. The new compounds possess high affinity and selectivity for the AA3R with N6-methyl-2-phenylethynylMECA (10) showing a subnanomolar affinity and about 100000-fold selectivity vs AA1R and AA2AR. Furthermore, the new ucleosides showed to be full agonists, the N6-methyl-2-(2-pyridinyl)- ethynylMECA (13) being the most potent in the series.
Synthesis and biological evaluation of 2-alkynyl-N6-methyl-5'-N-methylcarboxamidoadenosine derivatives as potent and highly selective agonists for the human adenosine A(3) receptor
VOLPINI, Rosaria;BUCCIONI, Michela;DAL BEN, DIEGO;LAMBERTUCCI, Catia;MARUCCI, Gabriella;CRISTALLI, Gloria
2009-01-01
Abstract
A new series of 2-aralkynyl-N6-methyl-MECAs 10-13 were synthesized and evaluated in radioligand binding studies and in a newEu-GTP functional assay that provides a powerful alternative to radioisotope use. The new compounds possess high affinity and selectivity for the AA3R with N6-methyl-2-phenylethynylMECA (10) showing a subnanomolar affinity and about 100000-fold selectivity vs AA1R and AA2AR. Furthermore, the new ucleosides showed to be full agonists, the N6-methyl-2-(2-pyridinyl)- ethynylMECA (13) being the most potent in the series.File in questo prodotto:
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