Synthesis and pharmacological evaluation of piperidinoalkanoyl-1,2,3,4-tetrahydroisoquinoline derivatives as novel specific bradycardic agents

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3049-52. doi: 10.1016/j.bmcl.2004.04.031.

Abstract

A series of piperidinoalkanoyl-1,2,3,4-tetrahydroisoquinoline derivatives were synthesized, and their bradycardic activities were investigated in the isolated right atria of guinea pigs and in conscious rats. These efforts identified the achiral compound 2f, which exhibited potent and long-lasting bradycardic activity with minimal effects on mean blood pressure in conscious rats.

MeSH terms

  • Animals
  • Bradycardia / drug therapy*
  • Cardiotonic Agents / chemical synthesis*
  • Cardiotonic Agents / pharmacology
  • Drug Evaluation, Preclinical / methods
  • Piperidones / chemical synthesis*
  • Piperidones / pharmacology
  • Rats
  • Tetrahydroisoquinolines / chemical synthesis*
  • Tetrahydroisoquinolines / pharmacology

Substances

  • Cardiotonic Agents
  • Piperidones
  • Tetrahydroisoquinolines