Luzzani F, Galliani G
Contraception. 1981 Mar;23(3):325-33. doi: 10.1016/0010-7824(81)90052-4.
Studies have been carried out to evaluate the effects of 3-(2-ethyl-phenyl)-5-(3-methoxyphenyl)-1H-1,2,4 triazole (DL 111-IT) a new non-hormonal post-implantation anti-fertility agent, on metabolism of prostaglandin F2 alpha (PGF2 alpha MET) by the utero-placental unit (UPU) and the lung. In rats treated with a single (100 mg/kg) subcutaneous minimal 100%-effective dose, DL 111-IT showed a slight and transient inhibitory effect on UPU PGF2 alpha MET, whereas after multiple (2.5 mg/kg/day for 3-5 days), equally effective doses, no effect was observed. In addition, PGF2 alpha levels in both plasma and the UPU were not changed. In rat lung, PGF2 alpha MET was markedly inhibited either after single or multiple injections and the inhibition was prolonged for at least 5-6 days after administration. In hamster, on the contrary, doses up to twenty times greater than 100%-effective ones caused only a slight inhibition of PGF2 alpha MET. The effects of DL 111-IT seem therefore to be dose and species dependent, but not to be related to its pregnancy-terminating activity, thus excluding the involvement of this effect as a part of its mechanism of action.
已有研究评估新型非激素植入后抗生育剂3-(2-乙基苯基)-5-(3-甲氧基苯基)-1H-1,2,4-三唑(DL 111-IT)对子宫胎盘单位(UPU)和肺中前列腺素F2α代谢(PGF2α MET)的影响。在用单次(100 mg/kg)皮下最小100%有效剂量处理的大鼠中,DL 111-IT对UPU的PGF2α MET表现出轻微且短暂的抑制作用,而在多次(2.5 mg/kg/天,持续3 - 5天)同等有效剂量处理后,未观察到影响。此外,血浆和UPU中的PGF2α水平均未改变。在大鼠肺中,单次或多次注射后PGF2α MET均受到显著抑制,且给药后抑制作用持续至少5 - 6天。相反,在仓鼠中,高达100%有效剂量二十倍的剂量仅引起PGF2α MET的轻微抑制。因此,DL 111-IT的作用似乎取决于剂量和物种,但与其终止妊娠的活性无关,从而排除了这种作用作为其作用机制一部分的参与。