Dopamine autoreceptor antagonists: effects on sleep-wake activity in the rat

Pharmacol Biochem Behav. 1987 Jan;26(1):123-9. doi: 10.1016/0091-3057(87)90544-2.


The effects of the putative dopamine (DA) autoreceptor antagonists cis-(+)-5-methoxy-1-methyl-2-(di-n-propylamino)tetralin, (+)-UH 232, and cis-(+)-5-methoxy-1-methyl-2-(n-propylamino)tetralin, (+)-AJ 76, on sleep-wake activity, EEG, and motor activity in the rat were studied. Both drugs induced a dose-dependent increase in wakefulness (W) and a reduction in non-REM sleep (NREMS). A definite tendency to a suppression of REM sleep (REMS) could also be observed. The results of spectral analysis indicated that EEG slow wave activity, a marker of sleep intensity, was particularly sensitive to the drugs. Slight differences between the two drugs were observed: (+)-AJ 76 seemed to be more efficacious than (+)-UH 232 in stimulating motor activity. (+)-UH 232 tended to suppress slow wave activity more strongly than (+)-AJ 76. It is suggested that the increase in W following administration of (+)-AJ 76 resulted predominantly from locomotor activation, while (+)-UH 232 might also act on dopaminergic mechanisms involved in the regulation of sleep.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 8-Hydroxy-2-(di-n-propylamino)tetralin* / analogs & derivatives*
  • Animals
  • Electroencephalography
  • Male
  • Motor Activity / drug effects
  • Motor Activity / physiology
  • Naphthalenes / pharmacology*
  • Rats
  • Receptors, Dopamine / drug effects*
  • Receptors, Dopamine / physiology
  • Sleep / drug effects*
  • Sleep / physiology
  • Tetrahydronaphthalenes / pharmacology*


  • Naphthalenes
  • Receptors, Dopamine
  • Tetrahydronaphthalenes
  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • 5-methoxy-1-methyl-2-(n-propylamino)tetralin
  • UH 232