Synthesis, neuropsychopharmacological effects and analgesic-antiinflammatory activities of pyrrole analogues of lefetamine

Farmaco. 1989 Sep;44(9):763-77.

Abstract

The synthesis of pyrrole analogues of the analgesic drug lefetamine is reported. These derivatives bear the 1-phenyl-2-(1H-pyrrol-1-yl)ethylamino moiety. Compounds were evaluated for analgesic activities in mice by the hot plate and Randall-Selitto tests. Antiinflammatory activity was tested by the carrageenan-induced rat paw edema method. General neuropsychopharmacological effects were also screened. The most interesting compound, N,N-dimethyl-1-phenyl-2-(1H-pyrrol-1-yl)ethylamine, showed an analgesic effect comparable to that of lefetamine, but devoid of the neurotoxicity of this drug.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
  • Anticonvulsants / chemical synthesis
  • Chemical Phenomena
  • Chemistry
  • Exploratory Behavior / drug effects
  • Female
  • Male
  • Mice
  • Motor Activity / drug effects
  • Muscle Relaxants, Central / chemical synthesis
  • Phenethylamines / chemical synthesis
  • Phenethylamines / pharmacology*
  • Psychomotor Performance / drug effects
  • Rats
  • Rats, Inbred Strains
  • Reaction Time / drug effects

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Anticonvulsants
  • Muscle Relaxants, Central
  • Phenethylamines
  • lephetamine