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亮丙瑞林

亮丙瑞林用途

Leuprolide是一种垂体GnRH受体激动剂。

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亮丙瑞林名称

[ CAS 号 ]:
53714-56-0

[ 中文名 ]:
亮丙瑞林

[ 英文名 ]:
Leuprolide TFA

[中文别名 ]:

[英文别名 ]:

Enantone
Leuprorelin
Leuplin
Leuprolide
nghormone
MFCD00167544
LH-RH LEUPROLIDE
Carcinil
pGlu-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHC2H5
Lucrin

亮丙瑞林生物活性

[ 描述 ]:

Leuprolide是一种垂体GnRH受体激动剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> GNRH受体

研究领域 >> 神经疾病

多肽产品

[参考文献]

[1]. Plosker GL, Leuprorelin. A review of its pharmacology and therapeutic use in prostatic cancer, endometriosis and other sex hormone-related disorders. Drugs.1994 Dec;48(6):930-967.

[2]. Leuprorelin

[相关活性小分子]

亮丙瑞林物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 分子式 ]:
C₅₉H₈₄N₁₆O₁₂

[ 分子量 ]:
1209.40

[ PSA ]:
466.34000

[ LogP ]:
0.41

[ 外观性状 ]:
绒毛状固体。旋光度：-31.7°

[ 折射率 ]:
1.682

[ 储存条件 ]:
−20°C

亮丙瑞林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OK6700000

CHEMICAL NAME :: Luteinizing hormone-releasing hormone (pig), 6-D-leucine-9-(N-ethyl-L-prolinamide)- 10-deglycinamide-

CAS REGISTRY NUMBER :: 53714-56-0

LAST UPDATED :: 199201

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C59-H84-N16-O12

MOLECULAR WEIGHT :: 1209.59

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 5214 ug/kg

SEX/DURATION :: male 1 year(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct

REFERENCE :: FESTAS Fertility and Sterility. (American Fertility Soc., 608 13th Ave. S, Birmingham, AL 35282) V.1- 1950- Volume(issue)/page/year: 42,765,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 280 ug/kg

SEX/DURATION :: female 28 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Maternal Effects - uterus, cervix, vagina 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: 27,853,1976

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 50 ug/kg

SEX/DURATION :: female 15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 152,29,1976

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 25 ug/kg

SEX/DURATION :: female 11 day(s) after conception

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

REFERENCE :: PSEBAA Proceedings of the Society for Experimental Biology and Medicine. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1903/04- Volume(issue)/page/year: 152,29,1976

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亮丙瑞林安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H360

[ 警示性声明 ]:
P201-P280-P308 + P313

[ 安全声明 (欧洲) ]:
S22-S24/25

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

[ WGK德国 ]:
2

[ RTECS号 ]:
OH6390000

亮丙瑞林合成路线

详细合成路线

亮丙瑞林制备

苯酚和光气反应，生成氯甲酸苯酯，再和叔丁醇反应，生成叔丁氧基甲酸苯酯，接着和肼反应后，再亚硝化生成叠氮甲酸叔丁酯，然后和亮氨酸反应，得到亮氨酸侧链。
同样可以得到脯氨酸侧链。

丝氨酸和氯化苄反应以保护羟基，再和叠氮甲酸叔丁酯反应得到丝氨酸侧链。
和丝氨酸相似，可以得到酪氨酸及组氨酸的侧链。
叠氮甲酸叔丁酯和色氨酸反应后，再和2，4，6-三甲氧基苯磺酰氯反应成酯，得到色氨酸侧链。
叠氮甲酸叔丁酯和精氨酸反应，再和对甲苯磺酰氯反应，得到精氨酸侧链。
得到上述的侧链后，再进行接肽，然后和乙胺反应，再水解或氢解脱去保扩基后，精制提纯得到利普安。

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亮丙瑞林文献

Estradiol, but not testosterone, heightens cortisol-mediated negative feedback on pulsatile ACTH secretion and ACTH approximate entropy in unstressed older men and women.

Am. J. Physiol. Regul. Integr. Comp. Physiol. 306(9) , R627-35, (2014)

How sex steroids modulate glucocorticoid feedback on the hypothalamic-pituitary-corticotrope (HPC) unit is controversial in humans. We postulated that testosterone (T) in men and estradiol (E2) in wom...

Two different formulations with equivalent effect? Comparison of serum estradiol suppression with monthly goserelin and trimonthly leuprolide in breast cancer patients.

Med. Oncol. 30(1) , 354, (2013)

Data comparing the efficacy of monthly and trimonthly formulations of LHRH agonists are lacking. The aim of this study was to compare the effects of monthly goserelin and trimonthly leuprolide on estr...

Novasure as a mechanical endometrial preparation agent in large uteri.

JSLS 16(4) , 537-41, (2012)

We evaluated Novasure ablation as a mechanical endometrial preparation agent before Roller Ball endometrial ablation in lieu of GnRH agonists in large uteri.A retrospective chart review of 20 consecut...

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亮丙瑞林

亮丙瑞林用途

亮丙瑞林名称

亮丙瑞林生物活性

亮丙瑞林物理化学性质

亮丙瑞林毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

亮丙瑞林安全信息

亮丙瑞林合成路线

详细合成路线

亮丙瑞林制备

亮丙瑞林文献

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