Ye L, Huang R H
Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing, China.
Zhongguo Yao Li Xue Bao. 1990 Nov;11(6):560-3.
By measuring the methemoglobin formation, the permeabilities of some cyanide antidotes passing through mouse erythrocyte membrane were studied. K3Fe(CN)6(0.1 mol/L) did not permeate the red cell and no methemoglobin formed. To the red cell suspension, adding PAPP 0.07 mmol/L, an useful cyanide antidote, no methemoglobin was found. On the contrary, PHAPP, the metabolite of PAPP, transported into the cell readily and reacted with hemoglobin to form methemoglobin quickly. DMAP and NaNO2 passed through the red cell membrane easily. With comparable amount of methemoglobin formation, the concentration of NaNO2 was about 200 times as much as that of DMAP. A comparison of the anticyanide potency of DMAP and NaNO2, the permeability rate constant, the half time and activation energy were measured as: 0.217 and 0.0506/min; 3.2 and 13.7 min; 17.1 and 50.2 kJ/mol, respectively. Owing to its ready permeability and formation of methemoglobin, DMAP is a better antidote than NaNO2 against cyanide poisoning.
通过测定高铁血红蛋白的形成，研究了一些氰化物解毒剂透过小鼠红细胞膜的通透性。K3Fe(CN)6（0.1 mol/L）不能透过红细胞，也未形成高铁血红蛋白。向红细胞悬液中加入0.07 mmol/L的有效氰化物解毒剂PAPP，未发现高铁血红蛋白。相反，PAPP的代谢产物PHAPP很容易转运到细胞内，并与血红蛋白反应迅速形成高铁血红蛋白。DMAP和NaNO2很容易透过红细胞膜。在形成相当量高铁血红蛋白的情况下，NaNO2的浓度约为DMAP的200倍。测定了DMAP和NaNO2的抗氰效力、通透速率常数、半衰期和活化能，结果分别为：0.217和0.0506/min；3.2和13.7 min；17.1和50.2 kJ/mol。由于DMAP易于通透并形成高铁血红蛋白，因此在对抗氰化物中毒方面，它是比NaNO2更好的解毒剂。
