Oleamide-mediated sleep induction does not depend on perturbation of membrane homeoviscosity

FEBS Lett. 1999 Dec 17;463(3):281-4. doi: 10.1016/s0014-5793(99)01630-0.

Abstract

To verify whether the sleep-inducing properties of oleamide were related to its ability to perturb membrane homeoviscosity, affecting 5-HT(2A) receptors, we compared the effects of oleamide and oleic acid, the latter lacking both the sleep-inducing effect and the action on 5-HT(2A) receptors. In binding studies the two compounds did not directly interact with rat brain cortex 5-HT(2A) receptors, nor did they increase the affinity of a 5-HT(2A) agonist, either in vitro or ex vivo. They had similar fluidizing effects, in vitro at high concentrations (>/=10 microM), and ex vivo after a dose of 100 mg/kg, and they reduced locomotor activity with similar potency. There thus appears to be no causal relationship between the fluidizing effects of oleamide and its sleep-inducing properties.

MeSH terms

  • Animals
  • Brain / drug effects
  • Brain / metabolism
  • Fluorescence Polarization
  • Hypnotics and Sedatives / pharmacology*
  • Male
  • Membrane Fluidity / drug effects
  • Oleic Acid / pharmacology
  • Oleic Acids / pharmacology*
  • Rats
  • Receptor, Serotonin, 5-HT2A
  • Receptors, Serotonin / drug effects*
  • Serotonin Antagonists / pharmacology
  • Serotonin Receptor Agonists / pharmacology
  • Sleep / drug effects*
  • Synaptosomes / drug effects
  • Synaptosomes / metabolism

Substances

  • Hypnotics and Sedatives
  • Oleic Acids
  • Receptor, Serotonin, 5-HT2A
  • Receptors, Serotonin
  • Serotonin Antagonists
  • Serotonin Receptor Agonists
  • Oleic Acid
  • oleylamide