Role of GABAA Receptors in the Mechanism of In Vivo Psychotropic Activity of Amitriptyline in Rats

Bull Exp Biol Med. 2020 Jan;168(3):341-344. doi: 10.1007/s10517-020-04704-0. Epub 2020 Jan 15.

Abstract

Standard water-reinforced drug discrimination model was employed to train Wistar rats to discriminate the intraperitoneal injections of tricyclic antidepressant amitriptyline (5.4 mg/kg) and physiological saline. To examine the role of GABAA receptors in psychotropic action of amitriptyline, the substitution tests were performed with muscimol (0.1-1.0 mg/kg) and pregnenolone (30-50 mg/kg). Similar tests were carried out with amitriptyline interoceptive antagonists bicuculline (1 mg/kg), flumazenil (15 mg/kg), finasteride (5 mg/kg), and indomethacin (7.5 mg/kg). The study showed that interoceptive effects of amitriptyline depend on functional activity of GABAA receptors but not on the neurosteroid site of GABAA receptor complex.

Keywords: GABAA receptors; amitriptyline; drug discrimination; rats; tricyclic antidepressant.

MeSH terms

  • Amitriptyline / pharmacology*
  • Animals
  • Bicuculline / pharmacology
  • Cerebral Cortex / drug effects
  • Cerebral Cortex / metabolism
  • GABA-A Receptor Agonists / pharmacology
  • GABA-A Receptor Antagonists / pharmacology
  • Hippocampus / drug effects
  • Hippocampus / metabolism
  • Male
  • Muscimol / pharmacology
  • Nucleus Accumbens / drug effects
  • Nucleus Accumbens / metabolism
  • Pregnenolone / pharmacology
  • Psychotropic Drugs / pharmacology*
  • Rats
  • Rats, Wistar
  • Receptors, GABA-A / metabolism*

Substances

  • GABA-A Receptor Agonists
  • GABA-A Receptor Antagonists
  • Psychotropic Drugs
  • Receptors, GABA-A
  • Amitriptyline
  • Muscimol
  • Pregnenolone
  • Bicuculline