Ap. Ijzerman et al., PURINE-SUBSTITUTED ADENOSINE DERIVATIVES WITH SMALL N-6-SUBSTITUENTS AS ADENOSINE RECEPTOR AGONISTS, Nucleosides & nucleotides, 13(10), 1994, pp. 2267-2281
Adenosine, 6-hydroxylaminopurineriboside (HAPR), N6-methyladenosine an
d various derivatives of which the synthesis is described, were evalua
ted as adenosine receptor ligands in radioligand binding studies to pr
obe the relative importance for affinity of small N-6-substituents. Th
e findings were incorporated in a recently developed three-dimensional
model for the adenosine A, receptor, rationalising the more or less e
qual contribution to affinity of such different substituents as -OH an
d -CH3.