Twigg L E, Mead R J, King D R
Aust J Biol Sci. 1986;39(1):1-15.
Administration of 100 mg sodium fluoroacetate (compound 1080) per kilogram body weight to T. rugosa resulted in a 3.4-fold increase in plasma citrate levels 48 h after dosing while administration of 3 mg sodium fluoroacetate per kilogram body weight to R. norvegicus produced a fivefold increase in plasma citrate levels within 4 h. Administration of 300 mg sodium fluoroacetate per kilogram body weight reduced the oxygen consumption of the skink by between 2.5 and 11% while in the rat, 2 mg sodium fluoroacetate per kilogram body weight reduced oxygen consumption by between 28 and 57%. Aconitate hydratase activity in extracts of liver acetone powders from T. rugosa was less inhibited by (-)erythrofluorocitrate (Ki: 0.065 mM) than that in extracts derived from R. norvegicus (Ki: 0.026 mM). The rate of defluorination of fluoroacetate in erythrocytes and in extracts of liver acetone powders of T. rugosa was 8- and 4.5-fold greater, respectively, than that found in similar preparations from R. norvegicus. A rapid rate of defluorination together with a low reliance on aerobic respiration favoured detoxification of fluoroacetate in T. rugosa rather than its conversion into fluorocitrate. Though defluorination in this species helped to minimize the immediate effects of fluoroacetate on aerobic respiration, it resulted in rapid depletion of liver glutathione levels.
每千克体重给南非褶尾蜥施用100毫克氟乙酸钠（化合物1080），给药48小时后血浆柠檬酸水平增加了3.4倍；而每千克体重给褐家鼠施用3毫克氟乙酸钠，4小时内血浆柠檬酸水平增加了五倍。每千克体重给南非褶尾蜥施用300毫克氟乙酸钠，其耗氧量降低了2.5%至11%；而在大鼠中，每千克体重施用2毫克氟乙酸钠，耗氧量降低了28%至57%。与源自褐家鼠的提取物（Ki：0.026 mM）相比，(-)赤型氟柠檬酸对南非褶尾蜥肝脏丙酮粉提取物中乌头酸水合酶活性的抑制作用较小（Ki：0.065 mM）。南非褶尾蜥红细胞和肝脏丙酮粉提取物中氟乙酸的脱氟速率分别比褐家鼠类似制剂中的脱氟速率高8倍和4.5倍。快速的脱氟速率以及对有氧呼吸的低依赖性有利于南非褶尾蜥体内氟乙酸的解毒，而不是将其转化为氟柠檬酸。虽然该物种的脱氟有助于将氟乙酸对有氧呼吸的即时影响降至最低，但它导致肝脏谷胱甘肽水平迅速耗尽。
