%0 Journal Article %1 Volpini2009 %A Volpini, R. %A Buccioni, M. %A Ben, D. Dal %A Lambertucci, C. %A Lammi, C. %A Marucci, G. %A Ramadori, A. T. %A Klotz, K. N. %A Cristalli, G. %D 2009 %J J Med Chem %K & A3/*agonists Adenosine Adenosine/analogs Animals CHO Cricetinae Cricetulus Dose-Response Drug Fluorometry Humans Relationship, Specificity Substrate derivatives/*chemical synthesis/*pharmacology Receptor Cell %N 23 %P 7897-900 %T Synthesis and biological evaluation of 2-alkynyl-N6-methyl-5'-N-methylcarboxamidoadenosine derivatives as potent and highly selective agonists for the human adenosine A3 receptor %U http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=19839592 %V 52 %X A new series of 2-aralkynyl-N(6)-methyl-MECAs 10-13 were synthesized and evaluated in radioligand binding studies and in a new Eu-GTP functional assay that provides a powerful alternative to radioisotope use. The new compounds possess high affinity and selectivity for the AA(3)R with N(6)-methyl-2-phenylethynylMECA (10) showing a subnanomolar affinity and about 100000-fold selectivity vs AA(1)R and AA(2A)R. Furthermore, the new nucleosides showed to be full agonists, the N(6)-methyl-2-(2-pyridinyl)ethynylMECA (13) being the most potent in the series.

@article{Volpini2009, abstract = {A new series of 2-aralkynyl-N(6)-methyl-MECAs 10-13 were synthesized and evaluated in radioligand binding studies and in a new Eu-GTP functional assay that provides a powerful alternative to radioisotope use. The new compounds possess high affinity and selectivity for the AA(3)R with N(6)-methyl-2-phenylethynylMECA (10) showing a subnanomolar affinity and about 100000-fold selectivity vs AA(1)R and AA(2A)R. Furthermore, the new nucleosides showed to be full agonists, the N(6)-methyl-2-(2-pyridinyl)ethynylMECA (13) being the most potent in the series.}, added-at = {2010-12-14T18:12:02.000+0100}, author = {Volpini, R. and Buccioni, M. and Ben, D. Dal and Lambertucci, C. and Lammi, C. and Marucci, G. and Ramadori, A. T. and Klotz, K. N. and Cristalli, G.}, biburl = {https://www.bibsonomy.org/bibtex/23d72b50c06ed8d090f69fbeb216d1747/pharmawuerz}, endnotereftype = {Journal Article}, interhash = {6caf151f2cc9f942f0b197d00e734761}, intrahash = {3d72b50c06ed8d090f69fbeb216d1747}, issn = {1520-4804 (Electronic) 1520-4804 (Linking)}, journal = {J Med Chem}, keywords = {& A3/*agonists Adenosine Adenosine/analogs Animals CHO Cricetinae Cricetulus Dose-Response Drug Fluorometry Humans Relationship, Specificity Substrate derivatives/*chemical synthesis/*pharmacology Receptor Cell}, month = {Dec 10}, note = {Volpini, Rosaria Buccioni, Michela Dal Ben, Diego Lambertucci, Catia Lammi, Carmen Marucci, Gabriella Ramadori, Anna T Klotz, Karl-Norbert Cristalli, Gloria Research Support, Non-U.S. Gov't United States Journal of medicinal chemistry J Med Chem. 2009 Dec 10;52(23):7897-900.}, number = 23, pages = {7897-900}, shorttitle = {Synthesis and biological evaluation of 2-alkynyl-N6-methyl-5'-N-methylcarboxamidoadenosine derivatives as potent and highly selective agonists for the human adenosine A3 receptor}, timestamp = {2010-12-14T18:20:41.000+0100}, title = {Synthesis and biological evaluation of 2-alkynyl-N6-methyl-5'-N-methylcarboxamidoadenosine derivatives as potent and highly selective agonists for the human adenosine A3 receptor}, url = {http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=19839592}, volume = 52, year = 2009 }