Synthesis and cardiovascular activity of phenylalkylamine derivatives. I. Potential specific bradycardic agents

Chem Pharm Bull (Tokyo). 1992 Oct;40(10):2735-40. doi: 10.1248/cpb.40.2735.

Abstract

A series of acyclic amide derivatives of N-(omega-aminoalkyl)-N-methylhomoveratrylamine was synthesized and evaluated for their bradycardic activity in isolated guinea pig right atria. Among these compounds, (E)-N-[3-[N'-[2-(3,4-dimethoxyphenyl)ethyl]-N'-methylamino]propyl]- 4-[3,4-(methylenedioxy)phenyl]-3-butenamide (35) was the most potent in vitro and was also found to show dose-dependent bradycardia without remarkable reduction of left ventricular dp/dtmax or mean aortic pressure in anesthetized dogs.

MeSH terms

  • Animals
  • Bradycardia / chemically induced*
  • Cardiotonic Agents / chemical synthesis*
  • Cardiotonic Agents / pharmacology*
  • Dogs
  • Female
  • Guinea Pigs
  • Male
  • Verapamil / analogs & derivatives*
  • Verapamil / chemical synthesis
  • Verapamil / pharmacology*

Substances

  • Cardiotonic Agents
  • Verapamil