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氟他胺作为雄激素拮抗剂对大鼠附睾功能的影响。

Flutamide as an androgen antagonist on epididymal function in the rat.

作者信息

Dhar J D, Srivastava S R, Setty B S

出版信息

Andrologia. 1982 Jan-Feb;14(1):55-61. doi: 10.1111/j.1439-0272.1982.tb03095.x.

Abstract

The purpose of this study was to investigate whether flutamide (alpha-alpha-alpha--Trifluro-2-methyl-4'-nitro-m-propionatoluidide), a nonsteroidal compound acts as an androgen antagonist at the level of the epididymis. For comparison, cyproterone acetate was also evaluated under identical experimental conditions. The levels of glycerylphosphorylcholine (GPC), sialic acid, total phospholipids were used as functional indices of epididymis and, in addition, weights of the accessory sex organs were recorded. Adult male rats castrated and maintained on testosterone therapy (TP: 250 microgram/rat: i.m.) were treated with flutamide (25 mg/kg, oral) or cyproterone acetate (25 mg/kg, s.c.). Castration caused a reduction in the weight and secretory activity of the epididymis which was restored to near normal following TP replacement therapy. GPC level was found to be the most sensitive index of epididymal secretory function. The two antiandorgens antagonised the action of TP on all the accessory sex organs. These findings are discussed in relation to our previous study which demonstrated the lack of effect of flutamide on the epididymal function of intact rats.

摘要

本研究的目的是调查非甾体化合物氟他胺(α-α-α-三氟-2-甲基-4'-硝基-间丙酰甲苯胺)在附睾水平是否作为雄激素拮抗剂发挥作用。为作比较,在相同实验条件下对醋酸环丙孕酮也进行了评估。甘油磷酸胆碱(GPC)、唾液酸、总磷脂的水平被用作附睾的功能指标,此外,还记录了附属生殖器官的重量。成年雄性大鼠去势后接受睾酮治疗(TP:250微克/只大鼠,肌肉注射),并用氟他胺(25毫克/千克,口服)或醋酸环丙孕酮(25毫克/千克,皮下注射)进行处理。去势导致附睾重量和分泌活性降低,TP替代治疗后恢复至接近正常水平。发现GPC水平是附睾分泌功能最敏感的指标。这两种抗雄激素药物拮抗了TP对所有附属生殖器官的作用。结合我们之前的研究对这些发现进行了讨论,之前的研究表明氟他胺对完整大鼠的附睾功能没有影响。

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