Ultra-short-acting beta-adrenergic receptor blocking agents. 1. (Aryloxy)propanolamines containing esters in the nitrogen substituent

J Med Chem. 1982 Dec;25(12):1402-7. doi: 10.1021/jm00354a002.

Abstract

In an attempt to produce short-acting beta-adrenergic receptor blocking agents, we prepared several (aryloxy)propanolamines with ester functions incorporated into the nitrogen substituent. Many of these compounds exhibited a short duration of blocking activity after their continuous intravenous infusion for 40 min. However, their durations were found to increase considerably upon longer intravenous infusion.

MeSH terms

  • Adrenergic beta-Antagonists / chemical synthesis*
  • Animals
  • Blood Pressure / drug effects
  • Chemical Phenomena
  • Chemistry
  • Dogs
  • Guinea Pigs
  • In Vitro Techniques
  • Muscle, Smooth / drug effects
  • Muscle, Smooth, Vascular / drug effects
  • Propanolamines / chemical synthesis*
  • Propanolamines / pharmacology
  • Structure-Activity Relationship
  • Time Factors

Substances

  • Adrenergic beta-Antagonists
  • Propanolamines