| Description | L-732138 is a potent and competitive antagonist of neurokinin-1 (NK-1) receptor(IC50 : 2.3 nM) |
| In vitro | L-732,138对三种人类黑色素瘤细胞系（COLO 858, MEL HO, COLO 679）进行了研究。结果显示，L-732,138能够以浓度依赖的方式抑制所研究黑色素瘤细胞的生长。此外，L-732,138还能阻断SP促分裂素的刺激。L-732,138的特异性抗肿瘤作用是通过NK-1受体实现的，其引起的黑色素瘤细胞死亡是通过凋亡机制[1]。 |
| In vivo | L-732138消除了迷走神经诱导的气管支气管组织中的血浆渗漏，并且剂量依赖性地抑制了LPS增强的迷走神经诱导的气管支气管组织中的血浆渗出[2]。 |
| Cell experiments | 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 experiments | 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] |
| Target activity | NK1:2.3 nM |
| molecular weight | 472.38 |
| Molecular formula | C22H18F6N2O3 |
| CAS | 148451-96-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 4.72 mg/mL (10 mM) |
| References | 1. Muñoz M, et al. The NK-1 Receptor Antagonist L-732,138 Induces Apoptosis and Counteracts Substance P-Related Mitogenesis in Human Melanoma Cell Lines. Cancers (Basel). 2010 Apr 20;2(2):611-23. 2. 2 .Kuo HP, et al. Lipopolysaccharide enhances neurogenic plasma exudation in guinea-pig airways. Br J Pharmacol. 1998 Oct;125(4):711-6. |