Description |
L-NAME hydrochloride inhibits NOS with an IC50 of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC50 value of 1.4 μM.
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Target |
IC50: 70 μM (NOS)[1]
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In Vitro |
L-arginine analogues are widely used inhibitors of nitric oxide synthase (NOS) activity, with Nw-nitro-L-arginine methyl ester (L-NAME) being at the head[2]. Freshly dissolved L-NAME is 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 reveal that NOS inhibition by L-NAME closely correlated with hydrolysis of the drug to L-NOARG[1].
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In Vivo |
L-NAME infusion significantly decreases NKT-leukocyte level, tumor-necrosis factor (TNF)-alpha production by T-splenocytes and macrophages, and interferon-gamma production by T-leukocytes, monocytes, and T-splenocytes, as well as increased interleukin-6 production by T-leukocytes and monocytes and nitrate/nitrite production by T-leukocytes[3]. There is increasing evidence that nitric oxide may be involved in learning and memory. l-NAME produces a task-dependent impairment of fear extinction, and implies that nitric oxide signaling is involved in memory process of certain fear extinction tasks[4]. Chronic L-NAME administration induces cardiac hypertrophy in rodent models. Six weeks L-NAME administration induces significant cardiac hypertrophy compared to control hearts[5].
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Animal Admin |
Rats: The purpose is to investigate dose effects of chronically infused NOS inhibitor, LNAME on the anabolism, inflammatory responses, and arginine metabolism in parenterally fed rats with cecal puncture-induced subacute peritonitis. Male Wistar rats (8-9 weeks old), initially weighing 250 g, are used in the study. Rats are divided into 4 groups and are administered total parenteral nutrition solutions with 0, 5 (low dose), 25 (medium dose), or 50 (high dose) mg/kg per day of L-NAME for 7 days[3]. Mice: 12-20 week old C57BL/6J mice (5 per group) are administered L-NAME (0.325mg/mL) in the drinking water. Hearts are excised at 1-day, 2-days, 5-days, 2-weeks or 6-weeks; or controls which received no L-NAME. Ventricular cross-sectional wall thickness and individual cardiac myocytes cross-sectional area and cardiomyocyte/nuclear ratio to determine cardiac hypertrophy. Immuno-histochemical staining for c-kit, sca-1 and BCRP undertaken[5].
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Boiling Point | 383.5ºC at 760 mmHg |
Flash Point | 185.8ºC |
Exact Mass | 269.089081 |
PSA | 146.05000 |
LogP | 1.47960 |
Storage condition | 2~8°C |