Men 10376  (Synonyms: Neurokinin-2 receptor antagonist)

Men 10376 is a selective tachykinin NK-2 receptor antagonist, with a K_i of 4.4 μM for rat small intestine NK-2 receptor.

Ki: 4.4 μM (NK-2 receptor, rat small intestine)^[1]

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)^[1]. Men 10376 shows pA₂s 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)^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Men 10376 (1 and 3 μmol/kg) antagonizes increase in bladder motility produced by the NK-2 receptor agonist in rats^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1081.22

C₅₇H₆₈N₁₂O₁₀

135306-85-3

Asp-Tyr-{d-Trp}-Val-{d-Trp}-{d-Trp}-Lys-NH2

DY-{d-Trp}-V-{d-Trp}{d-Trp}-K-NH2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Quartara L, et al. N-terminal truncated analogs of men 10376 as tachykinin NK-2 receptor antagonists. Life Sci. 1992;51(25):1929-36.  [Content Brief]

  [2]. Maggi CA, et al. In vivo evidence for tachykininergic transmission using a new NK-2 receptor-selective antagonist, MEN 10,376. J Pharmacol Exp Ther. 1991 Jun;257(3):1172-8.  [Content Brief]