L-732138 是选择性有效和竞争性神经激肽-1受体拮抗剂，IC50为 2.3 nM，可减轻痛觉过敏并具有抗肿瘤作用。它在克隆的人NK-1受体中的效力比在克隆大鼠NK-1受体中高 200 倍，比人类 NK-2 和 NK-3 受体高 1000 倍以上。

L-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM)

L-732,138 against three human melanoma cell lines (COLO 858, MEL HO, COLO 679).?L-732,138 elicits cell growth inhibition in a concentration dependent manner in the melanoma cells studied.?Moreover, L-732,138 blocks SP mitogen stimulation.?The specific antitumor action of L-732,138 occurred through the NK-1 receptor and melanoma cell death was by apoptosis[1].

L-732138?Abolished the vagally-induced plasma leakage in tracheobronchial tissues, and dose-dependently inhibited the LPS enhanced vagally-induced plasma exudation in traceobronchial tissues[2].

Cell Line:COLO 858, MEL HO and COLO 679 cells. Concentration:0 μM, 20 μM, 40 μM, 60 μM, 80 μM, 100 μM. Incubation Time:First doubling time[1].

Animal Model:Male Dunkin-Hartley guinea-pigs (350-500 g) injected with lipopolysaccharide (LPS)[3].Dosage:10-4 mol/kg ,10-3 mol/kg and 10-2 mol/kg. Administration:Intravenous injection; for 15 minutes[2]

148451-96-1

C22H18F6N2O3

472.387

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years