MEN10207 (acetate)

MEN10207 is a peptide neurokinin-2 (NK2) receptor antagonist. It inhibits contractions induced by neurokinin A (NKA) in endothelium-deprived isolated rabbit pulmonary artery (pA2 = 7.89), which is endogenously enriched in NK2 receptors. It is selective for NK2 receptors in isolated rabbit pulmonary artery over NK2 receptors in isolated hamster trachea (pA2 = 5.9 using NKA as an agonist) and NK1 receptors in isolated guinea pig ileum (pA2 = 5.52 using substance P metl ester as an agonist), tissues that highly express these respective receptors, as well as NK3 receptors in isolated guinea pig cerebral cortex membranes (Ki = >10 μM). In vivo, MEN10207 (1 μmol/kg) inhibits increases in bladder motility induced by the NK2 receptor agonist [β-Ala8]-NKA (4-10) in anesthetized rats, as well as [β-Ala8]-NKA (4-10)-induced increases in bronchoconstriction in anesthetized guinea pigs. However, MEN10207 also induces bladder motility in anesthetized rats and bronchoconstriction in anesthetized guinea pigs when administered alone.