Soine W H, Brady K T, Balster R L, Underwood J Q
Res Commun Chem Pathol Pharmacol. 1980 Oct;30(1):59-70.
In vitro and in vivo studies of piperidinocyclohexanecarbonitrile (PCC): evidence for cyanide involvement in toxicity. The decomposition profile of piperidinocyclohexanecarbonitrile (PCC) was determined under simulated physiological conditions in vitro and in normal saline using gas chromatography. In normal saline, PCC undergoes pseudo first order decomposition with a k = 2.2 x 10(-2) min-1 (t 1/2 = 31.6 min). In 0.05 M phosphate buffer, pH 7.4 at 37 degrees C, k = 0.19 min-1 (t 1/2 = 3.7 min), and in human serum incubations, k = 0.15 min-1 (t 1/2 = 4.6 min). The median effective doses (ED50's) of PCC and NaCN for motor impairment in mice were determined using the screen test (PCC = 48.5 micrometers/kg; NaCN = 36.7 micrometers/kg). The median lethal doses (LD50's) of PCC and NaCN in mice were also determined (PCC = 133.6 micrometers/kg; NaCN = 130.6 micrometers/kg). Observations of the behavioral effects and gross appearance of the animals after NaCN and PCC injections revealed marked similarities. This study supports the hypothesis that many of the effects of PCC are probably due to the release of cyanide in vivo.
哌啶环己烷甲腈(PCC)的体外和体内研究:氰化物参与毒性作用的证据。采用气相色谱法在体外模拟生理条件下和生理盐水中测定了哌啶环己烷甲腈(PCC)的分解曲线。在生理盐水中,PCC发生准一级分解,k = 2.2×10⁻² min⁻¹(半衰期t₁/₂ = 31.6分钟)。在37℃、pH 7.4的0.05 M磷酸盐缓冲液中,k = 0.19 min⁻¹(半衰期t₁/₂ = 3.7分钟),在人血清孵育中,k = 0.15 min⁻¹(半衰期t₁/₂ = 4.6分钟)。使用筛选试验测定了PCC和NaCN对小鼠运动功能损害的半数有效剂量(ED50)(PCC = 48.5微克/千克;NaCN = 36.7微克/千克)。还测定了PCC和NaCN在小鼠中的半数致死剂量(LD50)(PCC = 133.6微克/千克;NaCN = 130.6微克/千克)。对注射NaCN和PCC后动物的行为影响和总体外观的观察显示出明显的相似性。本研究支持以下假设:PCC的许多作用可能是由于其在体内释放氰化物所致。