Cavazos R, Farooqui M Y, Day W W, Villarreal M I, Massa E
Department of Biological Sciences, Pan American University, Edinburg, TX 78539.
J Appl Toxicol. 1989 Feb;9(1):53-7. doi: 10.1002/jat.2550090110.
The interaction of 2[14C]methyl-2,3[14C]acrylonitrile (MeAN) with the components of blood and its disposition in male Sprague-Dawley rats has been investigated. Following an oral administration of 100 mg/kg (0.5 LD50, 8 microCi/kg), the rats excreted 43% of the [14C] in the urine, 15% in the feces and 2.5% in the expired air as 14CO2 in 5 days. Hydrogen cyanide (H14CN) was not detectable. The red blood cells retained significant amounts of radioactivity for more than five days after administration, whereas the [14C]-activity in plasma declined sharply. More than 50% of the radioactivity in erythrocytes was detected as covalently bound to cytoplasmic (hemoglobin) and membrane proteins. A small amount of radioactivity was also found in the heme fraction. About 13% of the total dose administered was recovered as thiocyanate in the plasma and the urine. These results suggest that the toxicity of MeAN may be attributable to the whole molecule and not entirely to the in vivo liberation of cyanide.
对2-[¹⁴C]甲基-2,3-[¹⁴C]丙烯腈（MeAN）与血液成分的相互作用及其在雄性斯普拉格-道利大鼠体内的处置情况进行了研究。口服给予100mg/kg（0.5 LD₅₀，8μCi/kg）后，大鼠在5天内将43%的[¹⁴C]经尿液排出，15%经粪便排出，2.5%以¹⁴CO₂形式经呼出气体排出。未检测到氰化氢（H¹⁴CN）。给药后，红细胞保留了大量放射性超过五天，而血浆中的[¹⁴C]活性急剧下降。红细胞中超过50%的放射性被检测为与细胞质（血红蛋白）和膜蛋白共价结合。在血红素部分也发现了少量放射性。给予的总剂量中约13%以硫氰酸盐形式在血浆和尿液中回收。这些结果表明，MeAN的毒性可能归因于整个分子，而不完全归因于体内氰化物的释放。
