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L-732138

CAS No. : 148451-96-1

MCE 站：L-732138

产品活性：L-732138 是一种选择性，有效和竞争性神经激肽-1 (NK-1) 受体拮抗剂，IC₅₀ 为 2.3 nM。L-732138 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 可减轻痛觉过敏并具有抗肿瘤作用。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Neurokinin Receptor

In Vitro: L-732138 (0 -100 ?M; first doubling time; COLO 858, MEL HO and COLO 679 cells) treatment results in a concentration-dependent cytotoxicity. L-732138 inhibits cell growth with IC₅₀ of 44.6 μM for COLO 858 cells, 76.3 μM for MEL HO cells and 64.2 μM for COLO 679 cells. L-732138 blocks substance P (SP) mitogen stimulation.
L-732,138 treatment results in a large number of apoptotic cells were found in COLO 858, MEL HO and COLO 679 melanoma cell lines. In DAPI-stained cultures, at IC₅₀ concentration of 43.6% apoptotic cells for the three melanoma cell lines, whereas at IC₁₀₀ concentration of 51.4 % apoptotic cells.

In Vivo: L-732138 (10^-4-10^-2 mol/kg; intravenous injection; for 15 minutes; male Dunkin-Hartley guinea-pigs) treatment abolishes vagally-induced plasma exudation and significantly inhibits the enhancement by LPS. The LPS-enhanced vagally-induced plasma exudation is not completely inhibited by either L-732138 or SOD pretreatment alone, but is blocked by the combination of both pretreatments.

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