L-NAME hydrochloride ,51298-62-5,IC-01245752

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 uM, 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 ¦ÌM L-arginine and 100 ¦ÌM NADPH, L-NAME HCl at 0.1¨C100 uM dose-dependently inhibited the formation of cyclic GMP in endothelial cytosol with an IC50 value of 3.1 ¦ÌM. It also inhibited [3H]-citrulline formation with an IC50 value of 0.09 ¦ÌM. L-NAME HCl at 0.1 ¨C 300 ¦ÌM induced endothelium-dependent contraction of rings of rat aorta with an EC50 value of 26 ¦ÌM in the presence of 10 nM phenylephrine. The relaxation of rings of rat aorta was inhibited by 0.1 ¨C 10 ¦ÌM L-NAME HCl at a dose-dependent manner with an IC50 value of 0.54 ¦ÌM. In Wistar rats, i.v. administration of L-NAME HCl (0.03 ¨C 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].

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].
[1]Furfine ES, Harmon MF, et al. Selective inhibition of constitutive nitric oxide synthase by L-NG-nitroarginine. Biochemistry. 1993;32(33):8512-7.

[2]Du Y, Sarthy VP, Kern TS. Interaction between NO and COX pathways in retinal cells exposed to elevated glucose and retina of diabetic rats. Am J Physiol Regul Integr Comp Physiol. 2004;287(4):R735-41.

[3]Rees DD, Palmer RM, et al. Characterization of three inhibitors of endothelial nitric oxide synthase in vitro and in vivo. Br J Pharmacol. 1990;101(3):746-52.

[4]Griffith OW, Kilbourn RG. Nitric oxide synthase inhibitors: amino acids. Methods Enzymol. 1996.

Order Information