Huwyler J, Gut J
Dept. of Pharmacology, Biocenter of the University, Basel, Switzerland.
Biochem Biophys Res Commun. 1992 May 15;184(3):1344-9. doi: 10.1016/s0006-291x(05)80030-0.
Hydrochlorofluorocarbons (HCFCs) that are structural analogues of the anesthetic agent halothane may follow a common pathway of bioactivation and formation of adducts to cellular targets of distinct tissues. Exposure of rats to a single dose of HCFC 123 (2,2-dichloro- 1,1,1-trifluoroethane) or its structural analogue halothane (2-bromo-2-chloro-1,1,1-trifluoroethane) in vivo resulted in the formation of one prominent trifluoroacetylated protein adduct (TFA-protein adduct) in the heart. In contrast, a variety of distinct TFA-protein adducts were formed in the liver and the kidney of the same animals. The TFA-protein adduct in the heart was processed rapidly; t1/2 of the intact TFA-protein adduct was less than 12 h.
作为麻醉剂氟烷结构类似物的氢氯氟烃（HCFCs）可能遵循共同的生物活化途径，并与不同组织的细胞靶点形成加合物。大鼠在体内单次暴露于一剂HCFC 123（2,2-二氯-1,1,1-三氟乙烷）或其结构类似物氟烷（2-溴-2-氯-1,1,1-三氟乙烷）后，心脏中形成了一种主要的三氟乙酰化蛋白加合物（TFA-蛋白加合物）。相比之下，同一动物的肝脏和肾脏中形成了多种不同的TFA-蛋白加合物。心脏中的TFA-蛋白加合物被迅速处理；完整TFA-蛋白加合物的半衰期小于12小时。
