Differential effects of the novel neurosteroid hypnotic (3β,5β,17β)-3-hydroxyandrostane-17-carbonitrile on electroencephalogram activity in male and female rats

Br J Anaesth. 2021 Sep;127(3):435-446. doi: 10.1016/j.bja.2021.03.029. Epub 2021 May 8.

Abstract

Background: We recently showed that a neurosteroid analogue, (3β,5β,17β)-3-hydroxyandrostane-17-carbonitrile (3β-OH), induced hypnosis in rats. The aim of the present study was to evaluate the hypnotic and anaesthetic potential of 3β-OH further using electroencephalography.

Methods: We used behavioural assessment and cortical electroencephalogram (EEG) spectral power analysis to examine hypnotic and anaesthetic effects of 3β-OH (30 and 60 mg kg-1) administered intraperitoneally or intravenously to young adult male and female rats.

Results: We found dose-dependent sex differences in 3β-OH-induced hypnosis and EEG changes. Both male and female rats responded similarly to i.p. 3β-OH 30 mg kg-1. However, at the higher dose (60 mg kg-1, i.p.), female rats had two-fold longer duration of spontaneous immobility than male rats (203.4 [61.6] min vs 101.3 [32.1] min), and their EEG was suppressed in the low-frequency range (2-6 Hz), in contrast to male rats. Although a sex-dependent hypnotic effect was not confirmed after 30 mg kg-1 i.v., female rats appeared more sensitive to 3β-OH with relatively small changes within delta (1-4 Hz) and alpha (8-13 Hz) bands. Finally, 3β-OH had a rapid onset of action and potent hypnotic/anaesthetic effect after 60 mg kg-1 i.v. in rats of both sexes; however, all female rats and only half of the male rats reached burst suppression, an EEG pattern usually associated with profound inhibition of thalamocortical networks.

Conclusions: Based on its behavioural effects and EEG signature, 3β-OH is a potent hypnotic in rats, with female rats being more sensitive than male rats.

Keywords: anaesthesia; electroencephalogram; hypnosis; neurosteroid; power spectral density; sex differences.

Publication types

  • Comparative Study

MeSH terms

  • Androstanols / administration & dosage
  • Androstanols / pharmacology*
  • Animals
  • Brain Waves / drug effects*
  • Cerebral Cortex / drug effects*
  • Cerebral Cortex / physiopathology
  • Dose-Response Relationship, Drug
  • Electrocorticography*
  • Female
  • Immobility Response, Tonic / drug effects*
  • Injections, Intraperitoneal
  • Injections, Intravenous
  • Male
  • Neurosteroids / administration & dosage
  • Neurosteroids / pharmacology*
  • Nitriles / administration & dosage
  • Nitriles / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Sex Factors
  • Time Factors

Substances

  • 3-hydroxyandrostane-17-carbonitrile
  • Androstanols
  • Neurosteroids
  • Nitriles