Mayer B, Schmid M, Klatt P, Schmidt K
Institut für Pharmakologie und Toxikologie, Karl-Franzens-Universität Graz, Austria.
FEBS Lett. 1993 Oct 25;333(1-2):203-6. doi: 10.1016/0014-5793(93)80405-j.
NG-Methyl-L-arginine (L-NMA) and NG-nitro-L-arginine (L-NNA) inhibited NO-induced cGMP accumulation in porcine aortic endothelial cells with half-maximally effective concentrations of 15 and 3.4 microM, respectively. The effects of both compounds were reversible, but the L-NNA-induced inhibition was only reversed by wash-out in the presence of 1 mM L-arginine. In short-term incubations (45 s) of membrane fractions, L-NMA and L-NNA exhibited similar potencies to inhibit endothelial NO synthase, but L-NNA was markedly more potent than L-NMA after prolonged incubation periods (> or = 3 min) due to induction of a pronounced, reversible enzyme inactivation.
NG-甲基-L-精氨酸（L-NMA）和NG-硝基-L-精氨酸（L-NNA）抑制了一氧化氮（NO）诱导的猪主动脉内皮细胞中环鸟苷酸（cGMP）的积累，其半数有效浓度分别为15和3.4微摩尔。两种化合物的作用都是可逆的，但L-NNA诱导的抑制作用只有在1毫摩尔L-精氨酸存在下通过洗脱才能逆转。在膜组分的短期孵育（45秒）中，L-NMA和L-NNA表现出相似的抑制内皮型一氧化氮合酶的效力，但在延长孵育期（≥3分钟）后，由于诱导了明显的、可逆的酶失活，L-NNA比L-NMA的效力明显更强。
