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醋酸烯诺孕酮

醋酸烯诺孕酮用途

Nestoron(ST1435; Elcometrine)是19-norprogesterone衍生物,是孕酮受体高亲和力激动剂。

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醋酸烯诺孕酮名称

[ CAS 号 ]:
7759-35-5

[ 中文名 ]:
醋酸烯诺孕酮

[ 英文名 ]:
Nestoron

[英文别名 ]:

NESTORONE
Elcometrine

醋酸烯诺孕酮生物活性

[ 描述 ]:

Nestoron(ST1435; Elcometrine)是19-norprogesterone衍生物,是孕酮受体高亲和力激动剂。

[ 相关类别 ]:

信号通路 >> 其他 >> 孕激素受体

研究领域 >> 内分泌

天然产物 >> 类固醇

[参考文献]

[1]. Ilani N, et al. A New Combination of Testosterone and Nestorone Transdermal Gels for Male Hormonal Contraception.J Clin Endocrinol Metab. 2012 Jul 12.

[2]. Rad M, et al. Discriminant analysis of the metabolic effects of a new combined contraceptive vaginal ring containing Nestorone/EE vs. a second-generation oral contraceptive containing levonorgestrel/EE.Contraception. 2012 Sep;86(3):231-7. Epub 2012 Mar 23

[3]. Hussain R, et al. Progesterone and Nestorone facilitate axon remyelination: a role for progesterone receptors.Endocrinology. 2011 Oct;152(10):3820-31. Epub 2011 Aug 9.

[4]. Prasad PV, et al. Single-dose pharmacokinetics of Nestorone, a potential female-contraceptive.Steroids. 2010 Mar;75(3):252-64. Epub 2010 Jan 11.

[5]. Elsimar M Coutinho et al. Use of a single implant of elcometrine (ST-1435), a nonorally active progestin, as a long acting contraceptive for postpartum nursing women Contraception Volume 59, Issue 2, February 1999, Pages 115-122

[相关活性小分子]

醋酸烯诺孕酮物理化学性质

[ 密度 ]:
1.15g/cm3

[ 沸点 ]:
499.3ºC at 760mmHg

[ 分子式 ]:
C₂₃H₃₀O₄

[ 分子量 ]:
370.48200

[ 闪点 ]:
216.2ºC

[ 精确质量 ]:
370.21400

[ PSA ]:
60.44000

[ LogP ]:
4.18520

[ 折射率 ]:
1.549

[ 储存条件 ]:
2-8℃

醋酸烯诺孕酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RC8960750

CHEMICAL NAME :: 19-Norpregn-4-ene-3,20-dione, 17-hydroxy-16-methylene-, acetate

CAS REGISTRY NUMBER :: 7759-35-5

LAST UPDATED :: 199306

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C23-H30-O4

MOLECULAR WEIGHT :: 370.53

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Administration onto the skin

DOSE :: 240 ug/kg

SEX/DURATION :: female 24 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders

REFERENCE :: FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 58,680,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Implant

DOSE :: 800 ug/kg

SEX/DURATION :: female 56 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - other measures of fertility

REFERENCE :: CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 25,299,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Implant

DOSE :: 2200 ug/kg

SEX/DURATION :: female 43 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

REFERENCE :: CCPTAY Contraception. (Geron-X, Inc., POB 1108, Los Altos, CA 94022) V.1- 1970- Volume(issue)/page/year: 18,411,1978

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Implant

DOSE :: 700 ug/kg

SEX/DURATION :: female 26 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders

REFERENCE :: FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 36,737,1981

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醋酸烯诺孕酮安全信息

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

醋酸烯诺孕酮文献

Nestorone: clinical applications for contraception and HRT.

Steroids 68(10-13) , 907-13, (2003)

The 19-nor derivatives of progesterone are referred to as "pure" progestational molecules as they bind almost exclusively to the progesterone receptor (PR) without interfering with receptors of other ...

Recent developments in contraceptive implants at the Population Council.

Contraception 65(1) , 113-9, (2002)

Development of contraceptive implant methods, when based on established or on new synthetic chemical entities, is a decadal or multi-decadal process. The process often requires the cooperation of nume...

Central modifications of allopregnanolone and beta-endorphin following subcutaneous administration of Nestorone.

J. Steroid Biochem. Mol. Biol. 116(1-2) , 15-20, (2009)

The aim of the present study was to evaluate the potential action of Nestorone (alone or in combination with estradiol valerate) on the level of allopregnanolone and of the opioid beta-endorphin in se...

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