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药品详细

Allylestrenol(烯丙雌醇)

化学结构式图
中文名
烯丙雌醇
英文名
Allylestrenol
分子式
C21H32O
化学名
(1S,2R,10R,11S,14R,15S)-15-methyl-14-(prop-2-en-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-14-ol
分子量
Average: 300.4782
Monoisotopic: 300.245315646
CAS号
432-60-0
ATC分类
G03D 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A synthetic steroid with progestational activity. [PubChem]

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference Not Available
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Steroids and Steroid Derivatives
    Substructures
    • Steroids and Steroid Derivatives
    • Hydroxy Compounds
    • Alkanes and Alkenes
    • Alcohols and Polyols
    • Cyclohexenes and Derivatives
    适应症
    药理
    Indication Allylestrenol was designed to be used for miscarriage prevention, prevention of premature labour and has been investigated for possible use in men for treatment for benign prostatic hyperplasia.
    Pharmacodynamics Allylestrenol is a progestogen structurally related to progesterone that has been given in threatened and recurrent miscarriage, and to prevent premature labour. However, with the exception of proven progesterone deficiency, such use is no longer recommended. In threatened miscarriage in progesterone-deficient women a suggested dose is 5 mg three times daily by mouth for 5 to 7 days.
    Mechanism of action Allylestrenol is similar in structure and function to progesterone. Progesterone shares the pharmacological actions of the progestins. Progesterone binds to the progesterone and estrogen receptors. Target cells include the female reproductive tract, the mammary gland, the hypothalamus, and the pituitary. Once bound to the receptor, progestins like Progesterone will slow the frequency of release of gonadotropin releasing hormone (GnRH) from the hypothalamus and blunt the pre-ovulatory LH (luteinizing hormone) surge. In women who have adequate endogenous estrogen, progesterone transforms a proliferative endometrium into a secretory one. Progesterone is essential for the development of decidual tissue and is necessary to increase endometrial receptivity for implantation of an embryo. Once an embryo has been implanted, progesterone acts to maintain the pregnancy. Progesterone also stimulates the growth of mammary alveolar tissue and relaxes uterine smooth muscle. It has little estrogenic and androgenic activity.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination The glucuronide and sulfate conjugates of pregnanediol and pregnanolone are excreted in the urine and bile. Progesterone metabolites which are excreted in the bile may undergo enterohepatic recycling or may be excreted in the feces. Progesterone metabolites are excreted mainly by the kidneys.
    Half life Not Available
    Clearance Not Available
    Toxicity Not Available
    Affected organisms Not Available
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 80 °C PhysProp
    Predicted Properties
    Property Value Source
    water solubility 5.58e-04 g/l ALOGPS
    logP 5.14 ALOGPS
    logP 4.83 ChemAxon
    logS -5.7 ALOGPS
    pKa (strongest basic) -0.17 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 1 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 20.23 ChemAxon
    rotatable bond count 2 ChemAxon
    refractivity 93.14 ChemAxon
    polarizability 37.17 ChemAxon
    药物相互作用
    食物相互作用
    Not Available

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