莫克雌醇(英语:Moxestrol)是一种雌激素类药物,商品名Surestryl,化学名为11β-甲氧基乙炔雌二醇,与RU-16117是11β-差向异构体,用于治疗更年期综合症月经失调,在欧洲有上市销售[3][4][2][5][6]

莫克雌醇
临床资料
商品名英语Drug nomenclatureSurestryl
其他名称R-2858, RU-2858, NSC-118191; 11β-Methoxy-17α-ethynylestradiol; 11β-MeO-EE 11β-Methoxy-17α-ethynylestra-1,3,5(10)-triene-3,17β-diol
怀孕分级
  • X (Contraindicated)
给药途径口服
药物类别英语Drug classEstrogen; Estrogen ether
ATC码
法律规范状态
法律规范
  • 处方药(-only)
药物动力学数据
生物利用度33%[1]
血浆蛋白结合率Minimal[1]
药物代谢Liver[2]
生物半衰期8.2 hours[1]
识别信息
  • (8S,9S,11S,13S,14S,17R)-17-ethynyl-11-methoxy-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthrene-3,17-diol
CAS号34816-55-2  checkY
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C21H26O3
摩尔质量326.44 g·mol−1
3D模型(JSmol英语JSmol
  • CC12CC(C3C(C1CCC2(C#C)O)CCC4=C3C=CC(=C4)O)OC
  • InChI=1S/C21H26O3/c1-4-21(23)10-9-17-16-7-5-13-11-14(22)6-8-15(13)19(16)18(24-3)12-20(17,21)2/h1,6,8,11,16-19,22-23H,5,7,9-10,12H2,2-3H3/t16-,17-,18-,19+,20-,21-/m0/s1
  • Key:MTMZZIPTQITGCY-OLGWUGKESA-N

参考资料

编辑
  1. ^ 1.0 1.1 1.2 Salmon, J.; Coussediere, D.; Cousty, C.; Raynaud, J.P. Pharmacokinetics and metabolism of moxestrol in animals—rat, dog and monkey. Journal of Steroid Biochemistry. 1983, 19 (2): 1223–1234. ISSN 0022-4731. PMID 6887930. doi:10.1016/0022-4731(83)90421-1. 
  2. ^ 2.0 2.1 Jonathan J. Li; Satyabrata Nandi; Sara A. Li. Hormonal Carcinogenesis: Proceedings of the First International Symposium. Springer Science & Business Media. 6 December 2012: 184– [2021-11-30]. ISBN 978-1-4613-9208-8. (原始内容存档于2021-11-30). 
  3. ^ J. Elks. The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. 14 November 2014: 841– [2021-11-30]. ISBN 978-1-4757-2085-3. (原始内容存档于2021-11-30). 
  4. ^ Dr. Ian Morton; I.K. Morton; Judith M. Hall. Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. 31 October 1999: 186– [2021-11-30]. ISBN 978-0-7514-0499-9. (原始内容存档于2021-11-30). 
  5. ^ Adrain D. Nunn. Radiopharmaceuticals: Chemistry and Pharmacology. CRC Press. 19 June 1992: 342– [2021-11-30]. ISBN 978-0-8247-8624-3. (原始内容存档于2021-11-30). 
  6. ^ William Martindale; Royal Pharmaceutical Society of Great Britain. Dept. of Pharmaceutical Sciences. The Extra Pharmacopoeia. Pharmaceutical Press. 1993: 1188 [2021-11-30]. ISBN 978-0-85369-300-0. (原始内容存档于2021-11-30). Moxestrol is a synthetic oestrogen with actions and uses similar to thosre described for the oestrogens in general. Moxestrol is reponed to have a prolonged duration of action. It has been given by mouth in the treatment of menopausal, postmenopausal, and menstrual symptoms. Dose have ranged from 50 to 100 µg weekly for long-term therapy to 25 to 250 µg daily for short-term use.