Study of local anaesthetics. Part 98(3): Preparation and local anaesthetic activity of 4-alkylpiperazinoethyl esters of o-heptyloxyphenylcarbamic acid

Pharmazie. 1992 Feb;47(2):94-6.

Abstract

During the course of study of variations in the basic moiety of heptacainium chloride 10 derivatives of 4-alkylpiperazinoethyl esters of o-heptyloxyphenylcarbamic acid were prepared. Pharmacological investigation indicated that practically all the new compounds were several times more active than standards (cocaine and procaine). The most effective compound was 1-[2-(o-heptyloxyphenylcarbamoyloxy)ethyl]-4-butyl-piperazinium dichloride, which was 142 times more active than cocaine and 266 times more active than procaine.

Publication types

  • Comparative Study

MeSH terms

  • Anesthetics, Local / chemical synthesis*
  • Anesthetics, Local / pharmacology
  • Animals
  • Carbamates / chemical synthesis*
  • Carbamates / pharmacology
  • Carbamates / toxicity
  • Cocaine / pharmacology
  • Guinea Pigs
  • Lethal Dose 50
  • Mice
  • Piperazines / chemical synthesis*
  • Piperazines / pharmacology
  • Piperazines / toxicity
  • Piperidines / chemical synthesis*
  • Piperidines / pharmacology
  • Procaine / pharmacology

Substances

  • Anesthetics, Local
  • Carbamates
  • Piperazines
  • Piperidines
  • Procaine
  • heptacaine
  • Cocaine