beta-Adrenergic blocking agents. alpha- and gamma-methyl(aryloxy)propanolamines

J Med Chem. 1981 Oct;24(10):1211-4. doi: 10.1021/jm00142a017.

Abstract

A series of gamma-methyl- (5) and alpha-methyl(aryloxy)propanolamines (6) were synthesized and evaluated for beta-adrenergic blocking action. The binding constant (KD) was determined for compounds 5a-j on cultured C6-2B astrocytoma cells. Compounds 5a-j and 6a-e were evaluated for beta 1-antagonist action on guinea pig atria and beta 2-antagonist action on guinea pig tracheal strips. Several gamma-methyl(aryloxy)propanolamines showed affinity for beta receptors and a possible preference for beta 2 receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic beta-Antagonists / chemical synthesis
  • Adrenergic beta-Antagonists / metabolism
  • Adrenergic beta-Antagonists / pharmacology*
  • Animals
  • Guinea Pigs
  • Heart / drug effects
  • In Vitro Techniques
  • Propanolamines / chemical synthesis
  • Propanolamines / pharmacology*
  • Receptors, Adrenergic, beta / metabolism
  • Structure-Activity Relationship
  • Trachea / drug effects

Substances

  • Adrenergic beta-Antagonists
  • Propanolamines
  • Receptors, Adrenergic, beta