Samson F, Donoso J A, Heller-Bettinger I, Watson D, Himes R H
J Pharmacol Exp Ther. 1979 Mar;208(3):411-7.
The action of a synthetic antitubulin agent, nocodazole, on tubulin self-assembly, preformed microtubules, fast axoplasmic transport and axonal ultrastructure was studied. Nocodazole completely blocks the self-assembly of tubulin containing or lacking associated proteins. This inhibition is readily reversible. At similar concentrations, nocodazole also depolymerizes preformed microtubules in vitro. Fast axoplasmic transport in cat vagus nerve is disrupted by bathing the nerve fivers in a medium containing 10 micrometer nocodazole for periods of 2.5 hr or longer. A 4-hr exposure results in extensive inhibition. The nocodazole action on fast axoplasmic transport appears to be reversible but with a high degree of variability. After 2.5 hr of exposure to 10 micrometers nocodazole, there is a slight decrease in axonal microtubules and an increase in 10 nm neurofilaments. A 4 hr exposure results in a marked reduction in microtubules. These results suggest that nocodazole has a mode of action similar to other antimicrotubule agents.
研究了一种合成抗微管蛋白剂诺考达唑对微管蛋白自组装、预先形成的微管、快速轴浆运输和轴突超微结构的作用。诺考达唑完全阻断含有或缺乏相关蛋白的微管蛋白的自组装。这种抑制作用很容易逆转。在相似浓度下，诺考达唑在体外也能使预先形成的微管解聚。将猫迷走神经的神经纤维浸泡在含有10微米诺考达唑的培养基中2.5小时或更长时间，会破坏快速轴浆运输。4小时的暴露会导致广泛抑制。诺考达唑对快速轴浆运输的作用似乎是可逆的，但具有高度变异性。暴露于10微米诺考达唑2.5小时后，轴突微管略有减少，10纳米神经丝增加。4小时的暴露导致微管显著减少。这些结果表明，诺考达唑的作用模式与其他抗微管药物相似。
