NG-nitro-L-arginine methyl ester (L-NAME) have been widely used to inhibit constitutive NO synthase (NOS) in different biological systems. L-NAME commonly used for the induction of NO-deficient hypertension[1].
Freshly dissolved L-NAME was a 50 fold less potent inhibitor of purified brain NOS (mean IC50 = 70 μM) than L-NOARG (IC50 = 1.4 μM), but the apparent inhibitory potency of L-NAME approached that of L-NOARG upon prolonged incubation at neutral or alkaline pH. HPLC analyses revealed that NOS inhibition by L-NAME closely correlated with hydrolysis of the drug to L-NOARG[1].
IL-NAME and the related compound L-NA (100 μM) constricted pressurized vessels (Sprague–Dawley rats) with myogenic tone. Removal of the endothelium did not cause constriction or alter myogenic tone, however the constrictor effect of L-NAME persisted. The constrictor effect of L-NAME was abolished by L-arginine (1 mM)[2].
References:
[1]: Pfeiffer S, Leopold E, et al. Inhibition of nitric oxide synthesis by NG-nitro-L-arginine methyl ester (L-NAME): requirement for bioactivation to the free acid, NG-nitro-L-arginine. Br J Pharmacol. 1996 Jul;118(6):1433-40.
[2].Murphy TV, Kotecha N, et al. Endothelium-independent constriction of isolated, pressurized arterioles by Nomega-nitro-L-arginine methyl ester (L-NAME). Br J Pharmacol. 2007 Jul;151(5):602-9. doi: 10.1038/sj.bjp.0707262. Epub 2007 Apr 30.
NG-硝基-L-精氨酸甲酯 (L-NAME) 已广泛用于抑制不同生物系统中的组成型一氧化氮合酶 (NOS)。 L-NAME 通常用于诱导 NO 缺乏型高血压[1]。
与 L-NOARG（IC50 = 1.4）相比，新鲜溶解的 L-NAME 对纯化脑 NOS 的抑制作用（平均 IC50 = 70 μM）低 50 倍μM)，但在中性或碱性 pH 条件下长时间孵育后，L-NAME 的表观抑制效力接近 L-NOARG。 HPLC 分析表明，L-NAME 对 NOS 的抑制作用与药物水解为 L-NOARG 密切相关[1]。
IL-NAME 和相关化合物 L-NA (100 μM) 收缩具有生肌张力的加压血管（Sprague-Dawley 大鼠）。去除内皮不会引起收缩或改变肌原性张力，但 L-NAME 的收缩效应仍然存在。 L-NAME 的收缩作用被 L-精氨酸 (1 mM)[2] 消除。