S 38093

Description: S 38093 is a novel brain-penetrant antagonist (inverse agonist) of the H3 (histamine H3) receptor with Ki of 8.8, 1.44 and 1.2 uM for rat, mouse and human H3 receptors, respectively. It may provide an innovative strategy to improve age-associated cognitive deficits. In cellular models, S 38093 is able to antagonize mice H3 receptors (KB=0.65 uM) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (KB=0.11 uM). In cells expressing a high H3 density, S 38093 behaves as a moderate inverse agonist at rat and human H3 receptors (EC50=9 and 1.7 uM, respectively). S 38093, as a novel H3 inverse agonist, is a good candidate for further in vivo evaluations, in particular in animal models of cognition.

References: Eur J Pharmacol. 2017 May 15; 803:11-23; Sci Rep. 2017 Feb 20; 7:42946.

Related CAS#: 1222097-72-4 (HCl)