Phencyclidine-like effects of tetrahydroisoquinolines and related compounds

J Med Chem. 1989 Jun;32(6):1242-8. doi: 10.1021/jm00126a016.

Abstract

A series of 1,2,3,4-tetrahydroisoquinolines, tetrahydrothieno[2,3-c]pyridines, and related compounds were evaluated for their ability to inhibit binding of [3H]-1-[1-(2-thienyl)piperidine and [3H]-N-allylnormetazocine to phencyclidine (PCP) and sigma receptors, respectively. A representative series of compounds was evaluated in behavioral assays to determine the ability of the compounds to induce PCP-like stereotyped behavior and ataxia. All of the compounds caused stereotyped behavior and ataxia, indicating their agonist actions at the PCP site.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Ataxia / chemically induced
  • Behavior, Animal / drug effects*
  • Chemical Phenomena
  • Chemistry
  • Isoquinolines / chemical synthesis
  • Isoquinolines / metabolism
  • Isoquinolines / pharmacology*
  • Male
  • Molecular Structure
  • Phenazocine / analogs & derivatives
  • Phenazocine / metabolism
  • Phencyclidine / analogs & derivatives
  • Phencyclidine / metabolism
  • Phencyclidine / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Receptors, Neurotransmitter / metabolism
  • Receptors, Phencyclidine
  • Stereotyped Behavior / drug effects
  • Structure-Activity Relationship
  • Tetrahydroisoquinolines*

Substances

  • Isoquinolines
  • Receptors, Neurotransmitter
  • Receptors, Phencyclidine
  • Tetrahydroisoquinolines
  • 1,2,3,4-tetrahydroisoquinoline
  • SK&F 10047
  • tenocyclidine
  • Phenazocine
  • Phencyclidine