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7α-甲基-19-去甲睾酮(一种不会发生5α-还原的雄激素)诱导大鼠的雄性性行为。

Induction of male sexual behavior in the rat by 7 alpha-methyl-19-nortestosterone, an androgen that does not undergo 5 alpha-reduction.

作者信息

Moralí G, Lemus A E, Munguía R, Arteaga M, Pérez-Palacios G, Sundaram K, Kumar N, Bardin C W

机构信息

Division of Pharmacology, UAM-Iztapalapa, Mexico City, Mexico.

出版信息

Biol Reprod. 1993 Sep;49(3):577-81. doi: 10.1095/biolreprod49.3.577.

Abstract

The synthetic steroid 7 alpha-methyl-19-nortestosterone (MENT) binds with high affinity to the androgen receptor and exerts biological effects at some peripheral target tissues with a potency greater than that of naturally occurring androgens. In vivo, MENT does not undergo enzymatic 5 alpha-reduction and as a consequence, its biologic action on prostate and other organs of the male reproductive tract is not amplified as is that of testosterone (T). Thus, in castrated rats, a dose of MENT that will maintain normal muscle mass and gonadotropin levels will not maintain normal prostate and seminal vesicle weights. To investigate the ability of MENT to restore male sexual behavior in castrated rats, varying doses of MENT acetate were administered for 4 wk by use of s.c. mini-osmotic pumps. Animals treated with T acetate (200 micrograms/day) and nontreated intact animals served as positive controls, while a group of animals receiving vehicle alone were the negative controls. Steroid acetates are rapidly converted to T and MENT in blood. Appropriate steroid delivery was assessed by measurement of serum androgen concentrations. Male behavioral parameters were recorded twice per week. At the end of treatment, the weights of sex accessory organs were also recorded. The administration of MENT acetate at daily doses of 100 micrograms and 10 micrograms induced full copulatory behavior in a manner similar to that observed with doses of 200 micrograms T acetate.(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

合成类固醇7α-甲基-19-去甲睾酮(MENT)与雄激素受体具有高亲和力,并在一些外周靶组织发挥生物学效应,其效力大于天然存在的雄激素。在体内,MENT不会发生酶促5α-还原,因此,其对前列腺和男性生殖道其他器官的生物学作用不会像睾酮(T)那样被放大。因此,在去势大鼠中,能维持正常肌肉质量和促性腺激素水平的MENT剂量并不能维持前列腺和精囊的正常重量。为了研究MENT恢复去势大鼠雄性性行为的能力,通过皮下植入微型渗透泵给予不同剂量的醋酸MENT,持续4周。用醋酸T(200微克/天)治疗的动物和未治疗的完整动物作为阳性对照,而一组仅接受赋形剂的动物为阴性对照。醋酸类固醇在血液中迅速转化为T和MENT。通过测量血清雄激素浓度评估适当的类固醇递送情况。每周记录两次雄性行为参数。在治疗结束时,还记录性附属器官的重量。每天给予100微克和10微克醋酸MENT可诱导完全交配行为,其方式与给予200微克醋酸T时观察到的相似。(摘要截短于250字)

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