8-SUBSTITUTED XANTHINES AS SELECTIVE ADENOSINE RECEPTOR AGENTS

摘要

Xanthine derivatives having general structure (I) including the (R) and (S) enantiomers and racemic mixtures thereof, and thepharmaceutically acceptable salts thereof, wherein R1 and R2 are each independently (C1-C4)lower alkyl or (C2-C4)lower alkenyl Z is (II)or (III) or (IV) wherein R3 is hydrogen, (C1-C3)lower alkyl, nitro, amino. hydroxy, fluoro, bromo or chloro, R4 is (C1-C4)lower alkyl and nis 1 or 2 which act selectively at adenosine receptors and which are in general as adenosine antagonists are disclosed. From in vitro studiesit is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitrocorrelates with adenosine receptor activity in vivo. Pharmaceutical preparations of the subject compounds can be prepared on the basis ofthe selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others,such as decreasing blood pressure without decreasing heart rate.