Herrmann M, Wiegleb J, Leuschner F
Arzneimittelforschung. 1977;27(9a):1758-67.
The tolerance of ethyl (Z)-(3-methyl-4-oxo-5-piperidino-thiazolidin-2-ylidene)acetate (etozolin, Gö 687, Elkapin) has been investigated over 18 months after oral administration in rats and over 1i months after intragastric application in dogs. Further the influence of the compound on pregnant animals and their fetuses after intragastric application has been investigated in rats and rabbits. The investigation of the influence on fertility and breeding capacity as well as on the peri- and postnatal development was carried out in rats after peroral administration. In the course of the chronic experiments a dose related increase of the excretion of fluid and electrolytes was observed. Side-effects, which mainly occurred during the last weeks of the experiment in the highest dosage group, were most probably due to the exhaustion of the fluid and especially of the electrolyte reserves of the animals. The experiments in rats and rabbits did not yield any findings indicating teratogenic properties. Fertility and breeding capacity were likewise not influenced by etozolin. An influence on the peri- and postnatal development could be demonstrated only in the toxic dose range.
对大鼠口服及犬灌胃给予乙酸乙酯(Z)-(3-甲基-4-氧代-5-哌啶基-噻唑烷-2-亚基)酯(依托唑啉,Gö 687,Elkapin)后,对其耐受性进行了长达18个月的研究。此外,还在大鼠和兔子身上研究了该化合物灌胃给药后对妊娠动物及其胎儿的影响。对大鼠口服给药后对生育力、繁殖能力以及围产期和产后发育的影响进行了研究。在慢性实验过程中,观察到液体和电解质排泄量呈剂量相关增加。副作用主要发生在实验最后几周的最高剂量组,很可能是由于动物液体尤其是电解质储备耗尽所致。大鼠和兔子的实验未发现任何表明有致畸特性的结果。依托唑啉对生育力和繁殖能力同样没有影响。仅在中毒剂量范围内可证明对围产期和产后发育有影响。