2-substituted adenosines with a-2 receptor affinity

Details 2-substituted adenosines with a-2 receptor affinity 2-substituted adenosines with a-2 receptor affinity

C - Chemistry, Metallurgy

07

H

C07H 19/167 (2006.01) A61K 31/70 (2006.01) C07H 19/16 (2006.01)

Patent

CA 2145682

Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine agonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectively and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo. Pharmaceutical preparations of the subject compounds can be prepared on the basis of the 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.

Divulgation d'analogues de l'adénosine qui ont une affinité pour les récepteurs de l'adénosine et qui agissent généralement comme des agonistes de l'adénosine. Des études in vitro ont révélé qu'il est possible de distinguer des effets physiologiques spécifiques par suite de cette affinité avec les récepteurs de l'adénosine et que l'affinité in vitro concorde avec l'affinité in vivo. Des préparations pharmaceutiques des composés en question peuvent être constituées en fonction de l'activité de liaison sélective des composés ci-dévoilés et amélioreront certains effets physiologiques tout en réduisant d'autres effets, comme abaisser la pression artérielle sans réduire le rythme cardiaque.

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