Asakura T, Ohnishi S T, Adachi K, Ozguc M, Hashimoto K, Singer M, Russell M O, Schwartz E
Proc Natl Acad Sci U S A. 1980 May;77(5):2955-9. doi: 10.1073/pnas.77.5.2955.
The antisickling effect of cetiedil, alpha-cyclohexyl-3-thiopheneacetic acid 2-(hexahydro-1H-azepin-1-yl)-ethyl ester, has been investigated. The concentration of cetiedil required for 50% inhibition of erythrocyte sickling was about 140 micro M. An antisickling effect was achieved regardless of whether cetiedil was added before or after deoxygenation. The minimal gelling concentration of deoxy Hb S was increased by less than 10% in the presence of 218 micro M cetiedil. The oxygen equilibrium curves of Hb S were not significantly affected by cetiedil. Erythrocytes treated with high concentrations of cetiedil were swollen and became spheroidal. The antisickling effects of cetiedil might be due to an effect on erythrocyte membranes.
已对塞替地尔(α-环己基-3-噻吩乙酸2-(六氢-1H-氮杂环庚烷-1-基)乙酯)的抗镰变作用进行了研究。抑制50%红细胞镰变所需的塞替地尔浓度约为140微摩尔。无论在脱氧前还是脱氧后添加塞替地尔,均能产生抗镰变作用。在218微摩尔塞替地尔存在的情况下,脱氧血红蛋白S的最小胶凝浓度增加不到10%。塞替地尔对血红蛋白S的氧平衡曲线没有显著影响。用高浓度塞替地尔处理的红细胞会肿胀并变成球形。塞替地尔的抗镰变作用可能是由于对红细胞膜的作用。