Synthesis and adenosine receptor affinity and potency of 8-alkynyl derivatives of adenosine

Authors
Lambertucci, C Costanzi, S Vittori, S Volpini, R Cristalli, G
Citation
C. Lambertucci et al., Synthesis and adenosine receptor affinity and potency of 8-alkynyl derivatives of adenosine, NUCLEOS NUC, 20(4-7), 2001, pp. 1153-1157
Citations number
8
Categorie Soggetti
Biochemistry & Biophysics
Journal title
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
ISSN journal
15257770 → ACNP
Volume
20
Issue
4-7
Year of publication
2001
Pages
1153 - 1157
Database
ISI
SICI code
1525-7770(2001)20:4-7<1153:SAARAA>2.0.ZU;2-G
Abstract
Adenosine derivatives bearing different (ar)alkynyl chains at the 8-positio n were synthesized and tested at human adenosine receptors. Binding studies showed that all compounds possess affinity for the A(3) subtype in the hig h nM range. Moreover, guanosine 5'-O-(3-[S-35]thio)triphosphate binding ass ay indicated that the 8-alkynyl adenosines behaved as antagonists of NECA a t A(3) receptors.