R278995/CRA0450, a corticotropin-releasing factor (CRF(1)) receptor antagonist modulates REM sleep measures in rats: Implication for therapeutic indication

Eur J Pharmacol. 2012 Apr 5;680(1-3):63-8. doi: 10.1016/j.ejphar.2012.01.023. Epub 2012 Jan 31.

Abstract

Abnormalities in the regulation of the hypothalamic stress hormone corticotropin-releasing factor (CRF) are thought to play a critical role in mood disorders. Consequently, CRF receptor antagonists have been proposed as potential novel therapeutic agents of these conditions. Sleep disturbance is common in depressed patients and changed sleep-wake architecture is considered as potential predictor or surrogate marker of response to treatment. The aim of our study was to characterise the effects of oral administration of the corticotropin-releasing factor CRF(1) receptor antagonist R278995/CRA0450 (3 and 10mg/kg) on sleep-wake organization and electroencephalographic (EEG) components in Sprague-Dawley rats, and to determine whether the changes observed in the sleep-EEG pattern resemble those seen with antidepressants. At 3mg/kg, R278995/CRA0450 produced minor changes in sleep behaviour, while an overall reduction in power spectra was observed during deep slow wave sleep. At 10mg/kg, R278995/CRA0450 consistently reduced rapid eye movement (REM) sleep (-75.4%) and increased the REM sleep onset latency (+67%, 92.1±4.9min for vehicle vs. 153.8±24min for R278995/CRA0450), in the absence of systematic changes in spectral EEG pattern, which are characteristic anti-depressant-like effects. These findings in rats indicate that the corticotropin-releasing factor CRF(1) receptor antagonist R278995/CRA0450 is centrally active under standard conditions as it inhibits REM sleep and promotes wakefulness. The characteristic changes found in the sleep EEG model further support the hypothesis that R278995/CRA0450 could exert a non-sedative, antidepressant-like action.

MeSH terms

  • Administration, Oral
  • Animals
  • Antidepressive Agents / pharmacology
  • Benzenesulfonates / pharmacology*
  • CRF Receptor, Type 1
  • Electroencephalography / methods
  • Male
  • Quinolines / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Rats, Wistar
  • Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
  • Receptors, Corticotropin-Releasing Hormone / metabolism
  • Sleep / drug effects
  • Sleep, REM / drug effects*
  • Wakefulness / drug effects

Substances

  • 1-(8-(2,4-dichlorophenyl)-2-methylquinolin-4-yl)-1,2,3,6-tetrahydropyridine-4-carboxamide benzenesulfonate
  • Antidepressive Agents
  • Benzenesulfonates
  • Quinolines
  • Receptors, Corticotropin-Releasing Hormone
  • CRF Receptor, Type 1