Islam F, Watanabe Y, Hayaishi O
Osaka Bioscience Institute, Japan.
Biochem Int. 1990 Nov;22(4):601-5.
The effect of lovastatin, simvastatin and pravastatin, which are competitive inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, was tested on PGD synthase purified to apparent homogeneity from the rat brain. Lovastatin and simvastatin, which reportedly cause insomnia in vivo, inhibited the PGD synthase activity dose-dependently and showed an IC50 value of 100 and 75 microM, respectively. On the other hand, pravastatin, which does not cause insomnia, showed no significant effect at 100 microM and only a slight effect up to 500 microM.
洛伐他汀、辛伐他汀和普伐他汀是3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶的竞争性抑制剂，研究了它们对从大鼠脑中纯化至表观均一性的前列腺素D合成酶（PGD合成酶）的作用。据报道，洛伐他汀和辛伐他汀在体内会导致失眠，它们剂量依赖性地抑制PGD合成酶活性，IC50值分别为100和75微摩尔。另一方面，不会导致失眠的普伐他汀在100微摩尔时无显著作用，在高达500微摩尔时仅有轻微作用。
