The role of the CB1 receptor in the regulation of sleep

Prog Neuropsychopharmacol Biol Psychiatry. 2008 Aug 1;32(6):1420-7. doi: 10.1016/j.pnpbp.2008.04.008. Epub 2008 Apr 18.


During the 1990s, transmembranal proteins in the central nervous system (CNS) that recognize the principal compound of marijuana, the delta-9-tetrahydrocannabinol (Delta9-THC) were described. The receptors were classified as central or peripheral, CB1 and CB2, respectively. To this date, it has been documented the presence in the CNS of specific lipids that bind naturally to the CB1/CB2 receptors. The family of endogenous cannabinoids or endocannabinoids comprises oleamide, arachidonoylethanolamine, 2-arachidonylglycerol, virodhamine, noladin ether and N-arachidonyldopamine. Pharmacological experiments have shown that those compounds induce cannabimimetic effects. Endocannabinoids are fatty acid derivates that have a variety of biological actions, most notably via activation of the cannabinoid receptors. The endocannabinoids have an active role modulating diverse neurobiological functions, such as learning and memory, feeding, pain perception and sleep generation. Experimental evidence shows that the administration of Delta9-THC promotes sleep. The activation of the CB1 receptor leads to an induction of sleep, this effect is blocked via the selective antagonist. Since the system of the endogenous cannabinoids is present in several species, including humans, this leads to the speculation of the neurobiological role of the endocannabinoid system on diverse functions such as sleep modulation. This review discusses the evidence of the system of the endocannabinoids as well as their physiological role in diverse behaviours, including the modulation of sleep.

Publication types

  • Review

MeSH terms

  • Animals
  • Arachidonic Acids / pharmacology
  • Arachidonic Acids / therapeutic use
  • Cannabinoid Receptor Modulators / metabolism
  • Cannabinoid Receptor Modulators / pharmacology
  • Cannabinoid Receptor Modulators / physiology
  • Humans
  • Receptor, Cannabinoid, CB1 / drug effects
  • Receptor, Cannabinoid, CB1 / physiology*
  • Receptor, Cannabinoid, CB2 / drug effects
  • Sleep / drug effects
  • Sleep / physiology*
  • Sleep Wake Disorders / drug therapy


  • Arachidonic Acids
  • Cannabinoid Receptor Modulators
  • N-(2-methyl-3-hydroxyphenyl)-5,8,11,14-eicosatetraenamide
  • Receptor, Cannabinoid, CB1
  • Receptor, Cannabinoid, CB2