L-659874 

L-659874 is a selective NK2 receptor antagonist with an IC₅₀ value of 0.49 μM in hamsters. L-659874 inhibits NK2 receptor-mediated hydrolysis of inositol phospholipids. L-659874 could be used for research on the correlation between pain signal transduction and smooth muscle responses.^[1].

L-659874 (preincubated for 15 min prior to stimulation with Eledoisin (HY-P0006); co-incubated with Eledoisin for a total duration of 45 min at 0.01-100 μM) potently inhibits NK₂ receptor-mediated Eledoisin-induced phosphatidylinositol hydrolysis in hamster bladder slices, with an IC₅₀ of 0.49 μM^[1].
L-659874 blocks the binding of iodine-125-labeled BH-Eledoisin to hamster bladder cell membranes, with an IC₅₀ of 0.04 μM^[1].

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

822.00

C₄₀H₅₅N₉O₈S

125989-15-3

Ac-Leu-Met-Gln-Trp-Phe-Gly-NH2

Ac-LMQWFG-NH2

C([C@@H](C(N[C@@H](CC1=CC=CC=C1)C(NCC(N)=O)=O)=O)NC([C@@H](NC([C@@H](NC([C@H](CC(C)C)NC(C)=O)=O)CCSC)=O)CCC(N)=O)=O)C=2C=3C(NC2)=CC=CC3

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• [1]. Suman-Chauhan N, et al. Pharmacological characterization of tachykinin-stimulated inositol phospholipid hydrolysis in peripheral tissues. Br J Pharmacol. 1990;101(4):1001-1005.  [Content Brief]