SB-674042

SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity for OX1 over OX2 receptors with IC50 values of 3.76 nM and 531 nM, respectively[1][4].

[1]Langmead CJ, et al. Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br J Pharmacol. 2004 Jan;141(2):340-6.  |[2]Ellis J, et al. Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function. J Biol Chem. 2006 Dec 15;281(50):38812-24. |[3]Chang X, et al. Orexin-A Stimulates Insulin Secretion Through the Activation of the OX1 Receptor and Mammalian Target of Rapamycin in Rat Insulinoma Cells. Pancreas. 2019 Apr;48(4):568-573.  |[4]Yaeger JDW, et al. Orexin 1 Receptor Antagonism in the Basolateral Amygdala Shifts the Balance From Pro- to Antistress Signaling and Behavior. Biol Psychiatry. 2022 May 1;91(9):841-852.