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Men 10376 TFA is a selective tachykinin NK-2 receptor antagonist, with a K i of 4.4 μM for rat small intestine NK-2 receptor.
Appearance:Solid
IC50& Target:Ki: 4.4 μM (NK-2 receptor, rat small intestine)
In Vitro:Men 10376 is a selective tachykinin NK-2 receptor, with a K i of 4.4 μM, and shows low selectivity for NK-1 and NK-3 receptors (K i , >10 μM). Men 10376 shows pA 2 s of 5.66 and 8.08 for NK-1 (guinea-pig ileum) and NK-2 receptors (endothelium-deprive
In Vivo:Men 10376 (1 and 3 μmol/kg) antagonizes increase in bladder motility produced by the NK-2 receptor agonist in rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Biological Activity:Men 10376 TFA is a selective tachykinin NK-2 receptor antagonist, with a K i of 4.4 μM for rat small intestine NK-2 receptor.