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Description: SB-649868 (GSK-649868) is a novel, potent, selective and orally bioactive orexin (OX) 1 and OX2 receptor antagonist with pKi of 9.4 and 9.5 for OX1 and OX2 receptor, respectively. It can be potentially used for the treatment of insomnia and sleep disorder. The hypothalamic peptides orexin-A and orexin-B are potent agonists of two G-protein coupled receptors, namely the OX(1) and the OX(2) receptor. These receptors are widely distributed, though differentially, in the rat brain. In particular, the OX(1) receptor is highly expressed throughout the hypothalamus, whilst the OX(2) receptor is mainly located in the ventral posterior nucleus.
References: Eur J Pharmacol. 2012 Oct 5; 692(1-3):1-9; Bioorg Med Chem Lett. 2011 Sep 15; 21(18):5562-7.
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All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.
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