L-NAME HCl is a non-selective NOS inhibitor with Ki values of 15 nM, 39 nM and 4.4 μM for nNOS (bovine), eNOS (human), and iNOS (murine), respectively.
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Nitric oxide synthase (NOS) is an enzyme responsible for the production of nitric oxide (NO) from L-arginine. L-NAME HCl is an inhibitor for bovine brain NOS and mouse macrophage NOS with Ki values of 15 nM and 4.4 μM, respectively[1]. In rMC-1 cells, the accumulation of NO induced by glucose (25 mM) was inhibited by 1 mM L-NAME HCl. The treatment of L-NAME HCl at 1 mM also led to significantly decreased cell death in glucose-stimulated rMC-1 cells. Elevated production of PGE2 in BREC cells was significantly suppressed by 1 mM L-NAME HCl[2]. With the presence of 30 μM L-arginine and 100 μM NADPH, L-NAME HCl at 0.1 – 100 μM dose-dependently inhibited the formation of cyclic GMP in endothelial cytosol with an IC50 value of 3.1 μM. It also inhibited [3H]-citrulline formation with an IC50 value of 0.09 μM. L-NAME HCl at 0.1 – 300 μM induced endothelium-dependent contraction of rings of rat aorta with an EC50 value of 26 μM in the presence of 10 nM phenylephrine. The relaxation of rings of rat aorta was inhibited by 0.1 – 10 μM L-NAME HCl at a dose-dependent manner with an IC50 value of 0.54 μM. In Wistar rats, i.v. administration of L-NAME HCl (0.03 – 300 mg/kg) dose-dependently increased the mean arterial blood pressure with an EC50 value of 2.4 mg/kg, and the highest blood pressure induced by L-NAME HCl was 44.1 mmHg. The same treatment of L-NAME HCl also resulted in bradycardia at a concentration-dependent manner[3].
作用机制
L-NAME HCl is a soluble methyl ester that inhibits NOS. Intracellular esterases convert a variable and unknown fraction of L-NAME to L-NNA, which tightly but reversibly binds to NOS, competing with L-arginine[4].
L-NAME HCl 细胞研究
细胞系
浓度
检测类型
检测时间
活动说明
数据源
mouse BV2 cells
Function assay
24 h
Inhibition of Nitric oxide synthase activity in mouse BV2 cells assessed as LPS-induced NO production after 24 hrs by Griess reaction, IC50=18.9 μM
21377368
mouse RAW264.7 cells
Function assay
17-20 h
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma/LPS-stimulated nitric oxide production after 17 to 20 hrs by Griess assay, IC50=27.13 μM
Inhibition of Nitric oxide synthase activity in mouse BV2 cells assessed as LPS-induced NO production after 24 hrs by Griess reaction, IC50=18.9 μM
21377368
mouse RAW264.7 cells
Function assay
17-20 h
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma/LPS-stimulated nitric oxide production after 17 to 20 hrs by Griess assay, IC50=27.13 μM
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