CAS |
51298-62-5 |
Chinese Name |
N'-硝基-L-精氨酸甲酯盐酸盐 |
English Name |
L-NAME Hydrochloride |
Synonyms |
NG-Nitroarginine methyl ester hydrochloride;N(G)-Nitro-L-arginine methyl ester |
Molecular Formula |
C7H15N5O4·HCl |
Molecular Weight |
269.69 |
Solubility |
Soluble in Water ≥10mg/mL |
Purity |
HPLC≥98% |
Appearance |
White to off-white Solid |
Storage |
Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC |
EINECS 257-116-1 |
MDL |
MFCD00039052 |
SMILES |
N[C@@H](CCCNC(N[N+]([O-])=O)=N)C(OC)=O.[H]Cl |
InChIKey |
QBNXAGZYLSRPJK-JEDNCBNOSA-N |
InChI |
InChI=1S/C7H15N5O4.ClH/c1-16-6(13)5(8)3-2-4-10-7(9)11-12(14)15;/h5H,2-4,8H2,1H3,(H3,9,10,11);1H/t5-;/m0./s1 |
PubChem CID |
135193 |
Target Point |
NO Synthase |
Passage |
Immunology & Inflammation |
Background |
L-NAME hydrochloride is an inhibitor of NOS. |
Biological Activity |
L-NAME hydrochloride是 NOS 的抑制剂,IC50 为70 μM。[1-5] |
In Vitro |
L-精氨酸类似物是广泛使用的一氧化氮合酶(NOS)活性抑制剂,其中Nw-硝基-L-精氨酸甲酯(L-NAME)处于头部[2]。新鲜溶解的L-NAME是比L-NOARG(IC50 =1.4μM)低50倍的纯化脑NOS抑制剂(平均IC50 =70μM),但L-NAME的明显抑制效力接近L-NOARG的抑制效力。在中性或碱性pH下延长温育。 HPLC分析显示L-NAME对NOS的抑制与药物水解为L-NOARG密切相关[1]。 |
In Vivo |
L-NAME输注显著降低T细胞和巨噬细胞的NKT-白细胞水平,肿瘤坏死因子(TNF)-α产生,以及T-白细胞,单核细胞和T-脾细胞产生干扰素-γ,以及白细胞介素增加由T-白细胞和单核细胞产生的-6和由T-白细胞产生的硝酸盐/亚硝酸盐[3]。越来越多的证据表明,一氧化氮可能参与学习和记忆。 l-NAME产生恐惧灭绝的任务依赖性损伤,并暗示一氧化氮信号传导涉及某些恐惧灭绝任务的记忆过程[4]。慢性L-NAME给药在啮齿动物模型中诱导心脏肥大。与对照心脏相比,六周L-NAME给药诱导显著的心脏肥大[5]。 |
Animal Experiment |
大鼠:目的是研究长期输注的NOS抑制剂LNAME对肠道穿刺诱导的亚急性腹膜炎的肠胃外喂养大鼠的合成代谢,炎症反应和精氨酸代谢的剂量效应。最初重250g的雄性Wistar大鼠(8-9周龄)用于该研究。将大鼠分成4组,给予全胃肠外营养液,每天0,5(低剂量),25(中剂量)或50(高剂量)mg/kg L-NAME,持续7天[3]。小鼠:在饮用水中给予12-20周龄的C57BL/6J小鼠(每组5只)L-NAME(0.325mg/mL)。心脏在1天,2天,5天,2周或6周切除;或没有收到L-NAME的控件。心室横断面壁厚与个体心肌细胞横截面积和心肌细胞/核比值决定心肌肥厚。进行c-kit,sca-1和BCRP的免疫组织化学染色[5]。 |
Data Literature Source |
[1]. Pfeiffer S,et al. Inhibition of nitric oxide synthesis by NG-nitro-L-arginine methyl ester (L-NAME): requirement forbioactivation to the free acid,NG-nitro-L-arginine. Br J Pharmacol. 1996 Jul;118(6):1433-40. [2]. Kopincová J,et al. L-NAME in the cardiovascular system - nitric oxide synthase activator Pharmacol Rep. 2012;64(3):511-20. [3]. Lo HC,et al. The Nitric Oxide Synthase Inhibitor NG-Nitro-L-Arginine Methyl Ester Diminishes the Immunomodulatory Effects of Parental Arginine in Rats with Subacute Peritonitis. PLoSOne. 2016 Mar 23;11(3):e0151973. [4]. Luo H,et al. Effect of nitric oxide synthase inhibitor L-NAME on fear extinction in rats: a task-dependent effect. Neurosci Lett. 2014 Jun 20;572:13-8. [5]. Ocsan RJ,et al. Chronic NG-nitro-l-arginine methyl ester (L-NAME) administration in C57BL/6J mice induces a sustained decrease in c-kit positive cells during development of cardiac hypertrophy. J Physiol Pharmacol. 2013 Dec;64(6):727-36. |
Unit |
Bottle |
Specification |
200mg 10mM*1mL in Water 500mg 1g |