当前位置: X-MOL 学术Pharm. Chem. J. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Experimental Assessment of Additional Hormonal Activity of the Pregnane-Steroid Gestagen Gestobutanoyl
Pharmaceutical Chemistry Journal ( IF 0.9 ) Pub Date : 2021-06-15 , DOI: 10.1007/s11094-021-02400-5
T. A. Fedotcheva , N. I. Sheina , V. A. Parshin , A. V. Semeikin , V. A. Votyakov , N. L. Shimanovsky

The ability of gestobutanoyl, a pregnane steroid with progestogenic activity, to exhibit additional glucocorticoid, mineralocorticoid, antiandrogenic, and estrogenic effects in rats has been studied. It was found that gestobutanoyl did not have estrogenic activity because it did not increase the weight of the uterus with prolonged (30 d) administration at a therapeutic dose of 0.25 mg/kg and doses 10 and 100 times higher. Gestobutanoyl at a dose of 2.5 mg/kg for 30 d did not show glucocorticoid activity because the thymus mass did not change. However, the thymus mass decreased by 25% (p ≤ 0.05) when gestobutanoyl was administered at a dose 100 times higher (25 mg/kg) than the therapeutic dose. Gestobutanoyl at a dose of 2.5 mg/kg reduced the expression of androgen receptor (AR) mRNA in the rat uterus by 3 times and, as previously shown, did not increase the weight of the prostate and levator ani muscle. The mineralocorticoid activity of gestobutanoyl tablets was studied using peroral administration for 14 d to female rats at doses 100 and 1000 times (2.5 and 25 mg/kg, respectively) the therapeutic dose. Diuresis did not decrease, water was not retained in the rat body, and electrolytes were excreted in the urine and were present in the urine at constant concentrations in all experimental groups, indicating the absence of side mineralocorticoid effects of gestobutanoyl tablets.



中文翻译:

孕烷-甾体孕激素 Gestobutanoyl 的额外激素活性的实验评估

已经研究了 gestobutanoyl(一种具有孕激素活性的孕烷类固醇)在大鼠中表现出额外的糖皮质激素、盐皮质激素、抗雄激素和雌激素作用的能力。研究发现,孕酮丁酰基不具有雌激素活性,因为在 0.25 mg/kg 的治疗剂量和 10 倍和 100 倍以上的治疗剂量下长时间(30 天)给药不会增加子宫重量。Gestobutanoyl 以 2.5 mg/kg 的剂量给药 30 天没有显示糖皮质激素活性,因为胸腺质量没有变化。然而,胸腺质量下降了 25% ( p≤ 0.05) 当孕酮丁酰的给药剂量比治疗剂量高 100 倍 (25 mg/kg) 时。Gestobutanoyl 以 2.5 mg/kg 的剂量将大鼠子宫中雄激素受体 (AR) mRNA 的表达降低了 3 倍,并且如先前所示,不会增加前列腺和肛提肌的重量。雌性大鼠以治疗剂量的 100 倍和 1000 倍(分别为 2.5 和 25 mg/kg)口服给药 14 天,研究了孕酮丁酰片的盐皮质激素活性。在所有实验组中,利尿没有减少,水没有保留在大鼠体内,电解质从尿液中排出并以恒定浓度存在于尿液中,表明不存在孕酮丁酰片的盐皮质激素副作用。

更新日期:2021-06-15
down
wechat
bug