SB-674042

SB-674042 is a potent and selective small molecule antagonist of the orexin OX1 receptor (also known as hypocretin receptor 1), developed by GSK. It exhibits high affinity for the OX1 receptor with a Kd of 5.03 nM and demonstrates approximately 100-fold selectivity over the OX2 receptor (IC50 = 531 nM). As a non-peptide antagonist, it is primarily utilized as a pharmacological research tool to investigate the orexin system's role in physiological processes such as sleep-wake regulation, arousal, and reward-related behaviors. Preclinical studies have explored its potential therapeutic applications in treating depression and anxiety disorders, although it has not been approved for clinical use in humans. SB-674042 is characterized by its lack of significant activity at other major neurotransmitter receptors, including serotonergic, dopaminergic, adrenergic, and purinergic systems.

Other names

1-(5-(2-fluoro-phenyl)-2-methyl-thiazol-4-yl)-1-((S)-2-(5-phenyl-(1,3,4)oxadiazol-2-ylmethyl)-pyrrolidin-1-yl)-methanone