Ki: 4.4 μM (NK-2 receptor, rat small intestine)
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-deprived rabbit pulmonary artery). Men 10376 shows no effect on NK-3 receptor (K i , >10 μM).
Men 10376 (1 and 3 μmol/kg) antagonizes increase in bladder motility produced by the NK-2 receptor agonist in rats.