Synthetic procedure for the preparation of novel potent and selective A(3)adenosine receptor radioligands

Authors
Volpini, R Costanzi, S Lambertucci, C Vittori, S Cristalli, G
Citation
R. Volpini et al., Synthetic procedure for the preparation of novel potent and selective A(3)adenosine receptor radioligands, NUCLEOS NUC, 20(4-7), 2001, pp. 775-779
Citations number
10
Categorie Soggetti
Biochemistry & Biophysics
Journal title
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
ISSN journal
15257770 → ACNP
Volume
20
Issue
4-7
Year of publication
2001
Pages
775 - 779
Database
ISI
SICI code
1525-7770(2001)20:4-7<775:SPFTPO>2.0.ZU;2-#
Abstract
2-Phenylethynyladenosine and its N-6-methyl derivative were synthesized and evaluated in binding assays at human adenosine receptors stably transfecte d on CHO cells. Results showed that the N-6-methyl-2-phenylethynyladenosine is endowed with very high affinity and selectivity at A(3) receptor subtyp e. Hence, an alternative procedure for the synthesis of tritiated N-6-methy l-2-phenylethynyladenosine was set up to introduce tritiated methylamine in the final step.