Orexin-1 and orexin-2 receptor antagonists reduce ethanol self-administration in high-drinking rodent models

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Orexin-1 and orexin-2 receptor antagonists reduce ethanol self-administration in high-drinking rodent models

To examine the role of orexin-1 and orexin-2 receptor activity on ethanol self-administration, compounds that differentially target orexin (OX) receptor subtypes were assessed in various self-administration paradigms using high-drinking rodent models. Effects of the OX1 antagonist SB334867, the OX2 antagonist LSN2424100, and the mixed OX1/2 antagonist almorexant (ACT-078573) on home cage ethano...

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Orexins are hypothalamic neuropeptides which bind to two G-protein-coupled receptors, orexin-1 (OX(1)R) and orexin-2 (OX(2)R) receptor. While a role for OX(1)R has been established in both ethanol reinforcement and ethanol-seeking behaviour, the role of OX(2)R in these behaviours is relatively less-studied. The aim of this study was to determine the role of central OX(2)R in ethanol-taking and ...

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Orexin directly excites orexin neurons through orexin 2 receptor.

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The Dual Orexin/Hypocretin Receptor Antagonist, Almorexant, in the Ventral Tegmental Area Attenuates Ethanol Self-Administration

Recent studies have implicated the hypocretin/orexinergic system in reward-seeking behavior. Almorexant, a dual orexin/hypocretin R(1) and R(2) receptor antagonist, has proven effective in preclinical studies in promoting sleep in animal models and was in Phase III clinical trials for sleep disorders. The present study combines behavioral assays with in vitro biochemical and electrophysiologica...

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ژورنال

عنوان ژورنال: Frontiers in Neuroscience

سال: 2014

ISSN: 1662-453X

DOI: 10.3389/fnins.2014.00033