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trans-Clomiphene Hydrochloride

trans-Clomiphene Hydrochloride用途

盐酸恩氯米芬((E)-氯米芬)是一种口服有效的非甾体雌激素受体拮抗剂,具有抗雌激素作用。盐酸恩氯米芬可用于研究卵巢功能障碍、睾酮缺乏、男性性腺功能减退和2型糖尿病[1]。

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trans-Clomiphene Hydrochloride名称

[ CAS 号 ]:
14158-65-7

[ 英文名 ]:
trans-Clomiphene Hydrochloride

[英文别名 ]:

Enclomiphene hydrochloride

trans-Clomiphene Hydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 其他 >> 雌激素受体/ERR

研究领域 >> 内分泌

研究领域 >> 代谢疾病

[体外研究]

盐酸恩氯米芬(0-100μM,6小时)剂量依赖性地抑制基础和促性腺激素刺激的小型和大型绵羊黄体细胞孕酮分泌[2]。盐酸恩氯米芬(0-100μg/mL,24小时)剂量依赖性地抑制小鼠卵母细胞的受精率、囊胚形成率和变性率[3]。盐酸恩氯米芬(1 nM-10μM,6 h)剂量依赖性地降低E2诱导的对原代羊垂体细胞中促卵泡激素(FSH)分泌的抑制[4]。

[体内研究]

盐酸恩氯米芬(皮下注射,0.25和0.5 mg/只,每日)抑制完整或去势大鼠的精子发生,降低血清黄体生成素(LH)和睾酮水平[5]。盐酸恩氯米芬(口服给药,0.03-3 mg/kg,每日90天)将体重降低至假手术水平,并降低血清胆固醇[6]。动物模型：21日龄Charles River雄性大鼠[5]剂量：0.25和0.5 mg/只,每日24天。给药：皮下注射结果：血清中LH和睾酮水平降低。动物模型：OVX(卵巢切除)大鼠模型[6]剂量：0.03、1和3 mg/kg,每日90天。给药：口服给药结果：体重降低至假手术水平,血清胆固醇降低。对胫骨近端显示剂量依赖性效应,BMD和BMC接近治疗后假手术水平。

[参考文献]

[1]. Rodriguez KM, et al. Enclomiphene citrate for the treatment of secondary male hypogonadism. Expert Opin Pharmacother. 2016 Aug;17(11):1561-7.

[2]. M S Opsahl, et al. Effects of enclomiphene and zuclomiphene on basal and gonadotrophin-stimulated progesterone secretion by isolated subpopulations of small and large ovine luteal cells. Hum Reprod. 1996 Jun;11(6):1250-5.

[3]. G E Schmidt, et al. The effects of enclomiphene and zuclomiphene citrates on mouse embryos fertilized in vitro and in vivo. Am J Obstet Gynecol. 1986 Apr;154(4):727-36.

[4]. E S Huang, et al. Estrogenic and antiestrogenic effects of enclomiphene and zuclomiphene on gonadotropin secretion by ovine pituitary cells in culture. Endocrinology. 1983 Feb;112(2):442-8.

[5]. R Weissenberg, et al. The effect of clomiphene citrate and its Zu or En isomers on the reproductive system of the immature male rat. Andrologia. 1992 May-Jun;24(3):161-5.

[6]. R T Turner, et al. Differential responses of estrogen target tissues in rats including bone to clomiphene, enclomiphene, and zuclomiphene. Endocrinology. 1998 Sep;139(9):3712-20.

trans-Clomiphene Hydrochloride物理化学性质

[ 分子式 ]:
C₂₆H₂₉Cl₂NO

[ 分子量 ]:
442.42100

[ 精确质量 ]:
441.16300

[ PSA ]:
12.47000

[ LogP ]:
7.36460

trans-Clomiphene HydrochlorideMSDS

详细MSDS(安全技术说明书)

trans-Clomiphene Hydrochloride安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

trans-Clomiphene Hydrochloride文献

Bone Mineral Density and Response to Treatment in Men Younger Than 50 Years with Testosterone Deficiency and Sexual Dysfunction or Infertility

J. Urol. 191(4) , 1072-6, (2014)

Purpose Testosterone deficiency is a known risk factor for osteopenia and osteoporosis in older men. Less is known about the impact of testosterone deficiency on bone mineral density in younger men.

Progesterone luteal support after ovulation induction and intrauterine insemination: a systematic review and meta-analysis

Fertil. Steril. 100(5) , 1373-80, (2013)

Objective To evaluate the effect of luteal phase P support after ovulation induction IUI.

Re: Optimization of Spermatogenesis-Regulating Hormones in Patients with Non-Obstructive Azoospermia and its Impact on Sperm Retrieval: A Multicentre Study

J. Urol. 190(6) , 2209, (2013)

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