Disclosed are A₁ adenosine receptor agonists of the formula: ##STR1##

wherein:

R¹ is optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, or optionally substituted heteroaryl;

R² is hydrogen, halo, trifluoromethyl, or cyano;

R³ is hydrogen, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl,

R⁴ and R⁵ are independently hydrogen or optionally substituted acyl;

X is a covalent bond or lower alkylene optionally substituted by cycloalkyl;

X¹ is a covalent bond or alkylene;

Y is a covalent bond or lower alkylene optionally substituted by hedroxy or cycloalkyl; and

Z is —CC—, —R⁶CCR⁷—, or —CHR⁶CHR⁷—, in which R⁶ and R⁷ at each occurrence are hydrogen or lower alkyl.