Burbaeva G Sh, Androsova L V, Klintsova A Iu
Zh Nevropatol Psikhiatr Im S S Korsakova. 1988;88(5):119-23.
Neuroleptics (chlorpromazine, triftazin, haloperidol) inhibited the tubulin polymerization on supernatant of rat brain proteins in vivo at concentrations which corresponded to the therapeutic ones. The electron microscope studies demonstrated that these drugs inhibited the assembly of tubulin in microtubules. As this effect was the same in vivo and in vitro, it was considered specific. Colchicine-binding capacity of tubulin was suppressed only at higher doses of tranquilizers (250 microM). Antidepressant drug melipramine inhibited neither tubulin polymerization in vivo nor its colchicine-binding activity in vivo or in vitro.
抗精神病药物(氯丙嗪、三氟拉嗪、氟哌啶醇)在体内对应于治疗浓度时,可抑制大鼠脑蛋白上清液中的微管蛋白聚合。电子显微镜研究表明,这些药物可抑制微管蛋白组装成微管。由于这种效应在体内和体外相同,因此被认为具有特异性。仅在较高剂量的镇静剂(250微摩尔)作用下,微管蛋白的秋水仙碱结合能力才会受到抑制。抗抑郁药物丙咪嗪在体内既不抑制微管蛋白聚合,在体内或体外也不抑制其秋水仙碱结合活性。