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MEN11467 is a selective and orally- effective peptidomimetic tachykinin NK1 receptor antagonist.

MEN11467 potently inhibits the binding of [3H] substance P (SP) to tachykinin NK1 receptors in the IM9 limphoblastoid cell line (pKi=9.4±0.1). MEN11467 is highly specific for the human tachykinin NK1 receptors, since it has negligible effects (pKi<6) on the binding of specific ligands to tachykinin NK2 or NK3 receptors and to a panel of 30 receptors ion channels unrelated to tachykinin receptors. The antagonism exerted by MEN11467 at tachykinin NK1 receptors is insurmountable in saturation binding experiments, both KD and Bmax of SP are significantly reduced by MEN11467 (0.3-10 nM). In the guinea-pig isolated ileum, MEN11467 (0.03-1 nM) produces a nonparallel rightward shift of the concentration-response curve to SP methylester with a concomitant reduction of the Emax to the agonist (pKB=10.7±0.1). Moreover the antagonist activity of MEN11467 is hardly reversible despite prolonged washout[1]. The pseudopeptide tachykinin NK1 receptor antagonist, MEN11467 is used to study tachykininergic involvement in antigen-induced mucus secretion in ferret trachea in vitro. MEN11467 (1 nM-10 μM) inhibits [Sar9]SP-induced 35SO4, output in a concentration-dependent manner with an approximate IC50 of 0.3 μM[2].

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