Synthetic procedure for the preparation of novel potent and selective A3 adenosine receptor radioligands.
2-Phenylethynyladenosine and its N6-methyl derivative were synthesized and evaluated in binding assays at human adenosine receptors stably transfected on CHO cells. Results showed that the N6-methyl-2-phenylethynyladenosine is endowed with very high affinity and selectivity at A3 receptor subtype. Hence, an alternative procedure for the synthesis of tritiated N6-methyl-2-phenylethynyladenosine was set up to introduce tritiated methylamine in the final step.
Volpini
R
R
Dipartimento di Scienze Chimiche, University of Camerino, I-62032 Camerino, Italy.
Costanzi
S
S
Lambertucci
C
C
Vittori
S
S
Cristalli
G
G
D000241:Adenosine / Q000031:analogs & derivatives* / Q000737:chemistry* / Q000378:metabolism; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D007553:Isotope Labeling / Q000379:methods; D008024:Ligands; D043684:Receptor, Adenosine A3; D018047:Receptors, Purinergic P1 / Q000378:metabolism*; D013379:Substrate Specificity; D014316:Tritium
D008024:Ligands; C442710:N6-methyl-2-phenylethynyladenosine; D043684:Receptor, Adenosine A3; D018047:Receptors, Purinergic P1; D014316:Tritium; D000241:Adenosine