Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists

J Med Chem. 1993 Oct 15;36(21):3188-96. doi: 10.1021/jm00073a021.

Abstract

The (+)-and (-)-enantiomer of compounds 4 and 5 were synthesized and tested for central dopamine (DA) receptor stimulating activity, using biochemical and behavioral tests in rats. Based on the available data the (-)-enantiomers of 4 and 5 are characterized as centrally acting DA autoreceptor antagonists with oral activity. They display a similar pharmacological profile as the prototype DA autoreceptor antagonists (+)-1 and (+)-2 and show a certain preference for the D3 DA receptor antagonist binding site.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding Sites / drug effects
  • Biological Availability
  • Brain / drug effects
  • Brain / metabolism
  • Dopamine / biosynthesis
  • Dopamine / metabolism
  • Dopamine Antagonists*
  • Male
  • Motor Activity / drug effects
  • Piperidines / chemical synthesis*
  • Piperidines / pharmacokinetics*
  • Piperidines / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Dopamine / metabolism
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Dopamine Antagonists
  • Piperidines
  • Receptors, Dopamine
  • Dopamine