L-NMMA acetate is a potent inhibitor of Nitric-Oxide Synthase (NOS), with an IC50 of 2μM[1]. L-NMMA acetate has been widely used to regulate the vascular tension and blood pressure of arterial rings in animals[2].
In vitro, L-NMMA acetate treatment at 4000μM for 96 hours significantly reduced the proliferation and migration of the MDA-MB-231 and SUM159 cell lines[3]. L-NMMA acetate treatment (4000μM) for 72 hours inhibited the upregulation of inducible nitric oxide synthase (iNOS) induced by docetaxel in MDA-MB-468 cells and enhanced the Docetaxel-induced cell apoptosis[4]. L-NMMA acetate treatment (10000μM) for 42 hours significantly inhibited the expansion of porcine cumulus cells, without affecting nuclear or cytoplasmic maturation[5].
In vivo, L-NMMA acetate treatment via intravitreal injection (0.02μM/5μL; once every other day) for 4 weeks inhibited the NO signaling pathway and slowed down the progression of choroidal fibrosis in myopic guinea pigs[6]. In endotoxemic dogs, 22-hours intravenous infusion of L-NMMA acetate (10mg/kg/h) increased systemic and pulmonary vascular resistance, marginally increased mean arterial pressure, and decreased oxygen delivery[7].
References:
[1] Jung C S, Lange B, Zimmermann M, et al. Role of endogenous monomethylated L-arginine (L-NMMA) after subarachnoid hemorrhage[J]. Neurological Research, 2013, 35(7): 709-712.
[2] Rees D D, Palmer R M, Schulz R, et al. Characterization of three inhibitors of endothelial nitric oxide synthase in vitro and in vivo[J]. British journal of pharmacology, 1990, 101(3): 746.
[3] Granados-Principal S, Liu Y, Guevara M L, et al. Inhibition of iNOS as a novel effective targeted therapy against triple-negative breast cancer[J]. Breast Cancer Research, 2015, 17(1): 25.
[4] Dávila-González D, Choi D S, Rosato R R, et al. Pharmacological inhibition of NOS activates ASK1/JNK pathway augmenting docetaxel-mediated apoptosis in triple-negative breast cancer[J]. Clinical Cancer Research, 2018, 24(5): 1152-1162.
[5] Romero-Aguirregomezcorta J, Santa Á P, García-Vázquez F A, et al. Nitric oxide synthase (NOS) inhibition during porcine in vitro maturation modifies oocyte protein S-nitrosylation and in vitro fertilization[J]. PLoS One, 2014, 9(12): e115044.
[6] Li T, Bao B, Hao Y, et al. Suppressive effect of nitric oxide synthase (NOS) inhibitor L-NMMA acetate on choroidal fibrosis in experimental myopic guinea pigs through the nitric oxide signaling pathway[J]. European Journal of Pharmacology, 2023, 960: 176111.
[7] Cobb J P, Natanson C, Quezado Z M, et al. Differential hemodynamic effects of L-NMMA in endotoxemic and normal dogs[J]. American Journal of Physiology-Heart and Circulatory Physiology, 1995, 268(4): H1634-H1642.
L-NMMA acetate是一种强效一氧化氮合酶（NOS）抑制剂，IC50值为2μM[1]。L-NMMA acetate广泛应用于调节动物动脉环血管张力及血压[2]。
在体外，4000μM浓度的L-NMMA acetate处理96小时可显著抑制MDA-MB-231和SUM159细胞系的增殖与迁移[3]。4000μM浓度的L-NMMA acetate处理72小时能抑制多西他赛诱导的MDA-MB-468细胞中诱导型一氧化氮合酶（iNOS）上调，并增强多西他赛诱导的细胞凋亡[4]。10000μM浓度的L-NMMA acetate处理42小时可显著抑制猪卵丘细胞扩张，而不影响细胞核或细胞质成熟[5]。
在体内，玻璃体内注射0.02μM/5μL剂量的L-NMMA acetate（隔日一次，持续4周）可抑制NO信号通路，延缓近视豚鼠模型中的脉络膜纤维化进展[6]。在内毒素血症犬模型中，以10mg/kg/小时速率静脉输注L-NMMA acetate 22小时，可增加全身及肺血管阻力，轻微升高平均动脉压，并降低氧输送能力[7]。