PMID: 39529Mar 1, 1979

beta-Adrenergic blocking action of halonitrophenethanolamines

Archives Internationales De Pharmacodynamie Et De Thérapie
L G LettsC H Lim

Abstract

A series of phenethanolamines with N-isopropyl and N-tertbutyl substituents and ring-substituted with nitro- and halogen groups has been prepared. Using guinea-pig isolated atrial and tracheal preparations, the influence of the nitro-group on the beta 1- and beta 2-antagonist actions of the mono-halogen compounds was determined, and the antagonist and partial agonist effects of the halo-nitro-compounds on beta-adrenoceptors in these tissues measured to help elucidate structure-activity relations in this series. The halonitro compounds did not show enhanced activity compared with the mono-halogen substituted analogues. Several of the new compounds showed slight but significant beta 2-antagonist selectivity of action, and one compound was significantly beta 1-selective.

Related Concepts

Adrenergic beta-Antagonists
Cavia porcellus
Inotropism
Smooth Muscle
Myocardial Contraction
Phenethylamines
Beta-adrenergic receptor
Structure-Activity Relationship
Trachea
2-Hydroxyphenethylamine

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