Substance P is an undecapeptide that binds to the neurokinin-1 (NK-1) receptor, regulating many biological functions involved in neurogenic inflammation, pain, depression, and tumor cell migration. L-732138 is an NK-1 receptor antagonist that inhibits the binding of 125I-substance P to human NK-1 receptor expressed in Chinese hamster ovary cells with an IC50 value of 2.3 ± 0.7 nM. It shows over 1000-fold lower affinity for human NK-2 and NK-3 receptors. L-732138 also competitively inhibited the binding of [125I]-L-703,606, the quinuclidine amine antagonist, to human NK-1 receptor with an IC50 value of 3 nM[1]. The IC50 growth inhibition concentrations of L-732138 on melanoma cell lines COLO 858, MEL-H0, and COLO 679 are 44.6, 76.3, and 64.2 μM, respectively[2]. In (C57BL/6xDBA/2) F1 mice, daily intravenous injection of L-732138 (20 mg/kg) for 4 days reduced bone marrow B220+ population to 8.1% compared to 21.2% in DMSO-treated group[3].
搜索
