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Oleamide-mediated sleep induction does not depend on perturbation of membrane homeoviscosity
Authors:Gobbi M  Mennini T  Valle F D  Cervo L  Salmona M  Diomede L
Affiliation:Department of Molecular Biochemistry, Istituto di Ricerche Farmacologiche 'Mario Negri', Via Eritrea 62, 20157, Milan, Italy. gobbi@irfm.mnegri.it
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.
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