SB-334867 is an orexin antagonist. It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX1, with around 50x selectivity for OX1 over OX2 receptors. It has been shown to produce sedative and anorectic effects in animals, and has been useful in characterising the orexinergic regulation of brain systems involved with appetite and sleep, as well as other physiological processes. Orexin antagonists have multiple potential clinical applications including the treatment of drug addiction, insomnia, obesity and diabetes.
^Rodgers, RJ; Halford, JC; Nunes De Souza, RL; Canto De Souza, AL; Piper, DC; Arch, JR; Upton, N; Porter, RA; Johns, A (2001). "SB-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-A in rats". The European Journal of Neuroscience. 13 (7): 1444–52. doi:10.1046/j.0953-816x.2001.01518.x. PMID11298806.
^Haynes, AC; Chapman, H; Taylor, C; Moore, GB; Cawthorne, MA; Tadayyon, M; Clapham, JC; Arch, JR (2002). "Anorectic, thermogenic and anti-obesity activity of a selective orexin-1 receptor antagonist in ob/ob mice". Regulatory peptides. 104 (1–3): 153–9. doi:10.1016/S0167-0115(01)00358-5. PMID11830290.
^Eliassi, A; Nazari, M; Naghdi, N (2009). "Role of the ventromedial hypothalamic orexin-1 receptors in regulation of gastric Acid secretion in conscious rats". Journal of neuroendocrinology. 21 (3): 177–82. doi:10.1111/j.1365-2826.2009.01824.x. PMID19207823.
^Bingham, MJ; Cai, J; Deehan, MR (2006). "Eating, sleeping and rewarding: orexin receptors and their antagonists". Current Opinion in Drug Discovery & Development. 9 (5): 551–9. PMID17002215.
^Borgland, SL; Taha, SA; Sarti, F; Fields, HL; Bonci, A (2006). "Orexin a in the VTA is critical for the induction of synaptic plasticity and behavioral sensitization to cocaine". Neuron. 49 (4): 589–601. doi:10.1016/j.neuron.2006.01.016. PMID16476667.
^Narita, M; Nagumo, Y; Hashimoto, S; Narita, M; Khotib, J; Miyatake, M; Sakurai, T; Yanagisawa, M; Nakamachi, T (2006). "Direct involvement of orexinergic systems in the activation of the mesolimbic dopamine pathway and related behaviors induced by morphine". Journal of Neuroscience. 26 (2): 398–405. doi:10.1523/JNEUROSCI.2761-05.2006. PMID16407535.