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. using NKA as an agonist) and NK1 receptors in isolated guinea pig ileum (pA2 = 5. using substance P methyl 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 [beta-Ala8]-NKA (4-10) in anesthetized rats, as well as [beta-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.. Solulibility: DMSO: Soluble: =10 mg/ml: Ethanol: Slightly soluble: 0.1-1 mg/ml.