Adenosine functionalized congeners as cardiovascular treating ag

Details Adenosine functionalized congeners as cardiovascular treating ag Adenosine functionalized congeners as cardiovascular treating ag

1992-08-06

1994-02-08

Brown, Johnnie R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

536 276, 536 2761, 536 2762, 530330, 530331, 530332, 514 17, 514 18, 514 19, A61K 3152, C07H 1700

Patent

active

052848345

ABSTRACT:
This invention comprises a series of N.sup.6 -substituted adenosine analogues bearing functionalized chains for the covalent attachment to probes or solid supports. In these compounds coronary vasodilation in the open thorax dog model, typical of A.sub.2 -adenosine receptor agonists, is shown. The potency is modulated by distal structural changes in the chain, with the highest A.sub.2 -potency observed for two methylamides, a primary amine congener, and a biotin conjugate. These compounds have antihypertensive activity and certain components are charged and are excluded from crossing the blood-brain barrier.

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