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枸橼酸恩氯米芬

枸橼酸恩氯米芬用途

Enclomiphene((E)-克罗米芬)是一种有效的口服活性非甾体雌激素受体拮抗剂,具有抗雌激素特性。Enclomiphene可用于研究卵巢功能障碍、睾酮缺乏、男性性腺机能减退和2型糖尿病[1]。

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枸橼酸恩氯米芬名称

[ CAS 号 ]:
15690-57-0

[ 中文名 ]:
恩氯米芬

[ 英文名 ]:
enclomifene

[中文别名 ]:

顺氯米芬(氯米芬)

[英文别名 ]:

Clomiphene
Zuclomiphene
Isomer A
Transclomifenum
zuclomifene
cis-clomifene
cis-clomiphene
enclomiphene
Transclomiphene
Clomiphene B

枸橼酸恩氯米芬生物活性

[ 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]

包体霉素(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]。包体霉素(0-100μg/mL,24小时)剂量依赖性地抑制小鼠卵母细胞中的受精率、囊胚形成率和变性率[3]。Enclomiphene(1 nM-10μM,6 h)剂量依赖性地减少E2诱导的对原代绵羊垂体细胞中卵泡刺激素(FSH)分泌的抑制[4]。

[体内研究]

Enclomiphene(皮下注射,每天0.25和0.5毫克/只)抑制完整或去势大鼠的精子生成,降低血清促黄体生成激素(LH)和睾酮水平[5]。Enclomiphene(口服,0.03-3 mg/kg,每天90天)可将体重降至假手术水平,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,每天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,每天90天。给药：口服给药结果：将体重降至假手术水平,并降低血清胆固醇。随着BMD和BMC接近治疗后假手术水平,对胫骨近端表现出剂量依赖性影响。

[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.

枸橼酸恩氯米芬物理化学性质

[ 密度 ]:
1.1±0.1 g/cm3

[ 沸点 ]:
509.0±50.0 °C at 760 mmHg

[ 分子式 ]:
C₂₆H₂₈ClNO

[ 分子量 ]:
405.960

[ 闪点 ]:
261.6±30.1 °C

[ 精确质量 ]:
405.185944

[ PSA ]:
12.47000

[ LogP ]:
8.01

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.588

枸橼酸恩氯米芬毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: YE0810000

CHEMICAL NAME :: Triethylamine, 2-(p-(2-chloro-1,2-diphenylvinyl)phenoxy)-, (E)-

CAS REGISTRY NUMBER :: 15690-57-0

LAST UPDATED :: 198910

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C26-H28-Cl-N-O

MOLECULAR WEIGHT :: 406.00

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 2 mg/kg

SEX/DURATION :: female 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - uterus, cervix, vagina

REFERENCE :: AEMBAP Advances in Experimental Medicine and Biology. (Plenum Pub. Corp., 233 Spring St., New York, NY 10013) V.1- 1967- Volume(issue)/page/year: 138,87,1982