炔诺酮

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炔诺酮
Norethisterone.svg
Norethisterone molecule ball.png
系统(IUPAC)命名名称
(8R,9S,10R,13S,14S,17R)-17-ethynyl-17-hydroxy-13-methyl-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one
临床数据
商品名 Alone: Aygestin, Camila, Heather, Micronor, Primolut N, others; With EE: Lo Loestrin, Loestrin, Microgestin, Modicon, Norinyl, Ortho-Novum, others; With E2: Activella, Activelle, Estalis, Kliogest, Necon, Novofem, Trisequens, others
Drugs.com 国际药品名称
MedlinePlus a604034
给药途径 By mouth, intramuscular injection (as NETE)
药代动力学数据
生物利用度 47–73% (mean 64%)[1][2]
蛋白结合度 97%:
Albumin: 61%;
SHBG: 36%
代谢 Mainly CYP3A4 (liver);[3] also 5α-/5β-reductase, 3α-/3β-HSD, and aromatase
生物半衰期 5.2–12.8 hours (mean 8.0 hours)[1]
识别信息
CAS注册号68-22-4 ✓
ATC代码 G03AC01 G03DC02
PubChem CID 6230
IUPHAR/BPS英语IUPHAR/BPS 2880
DrugBank DB00717 ✓
ChemSpider 5994 ✓
UNII T18F433X4S ✓
KEGG D00182 ✓
ChEBI CHEBI:7627 ✓
ChEMBL英语ChEMBL CHEMBL1162 ✓
其他名称 NET; Norethindrone; NSC-9564; LG-202; Ethinylnortestosterone; Norpregneninolone; Anhydrohydroxy-norprogesterone; Ethinylestrenolone; 17α-Ethynyl-19-nortestosterone; 17α-Ethynylestra-4-en-17β-ol-3-one; 17α-Hydroxy-19-norpregn-4-en-20-yn-3-one
化学信息
化学式 C20H26O2
摩尔质量 298.419 g/mol
物理性质
熔点 203至204 °C(397至399 °F)

炔诺酮(英語:Norethisterone 或 英語:norethindrone)是一种黄体制剂药物,用做口服避孕药激素替代療法药物以及治疗一些妇科疾病[4]

参考文献[编辑]

  1. ^ 1.0 1.1 Stanczyk, Frank Z. Pharmacokinetics and Potency of Progestins used for Hormone Replacement Therapy and Contraception (PDF). Reviews in Endocrine and Metabolic Disorders. Sep 2002, 3 (3): 211–224. ISSN 1389-9155. PMID 12215716. doi:10.1023/A:1020072325818. 
  2. ^ Fotherby K. Bioavailability of orally administered sex steroids used in oral contraception and hormone replacement therapy. Contraception. August 1996, 54 (2): 59–69. PMID 8842581. doi:10.1016/0010-7824(96)00136-9. 
  3. ^ Korhonen T, Turpeinen M, Tolonen A, Laine K, Pelkonen O. Identification of the human cytochrome P450 enzymes involved in the in vitro biotransformation of lynestrenol and norethindrone. J. Steroid Biochem. Mol. Biol. 2008, 110 (1–2): 56–66. PMID 18356043. doi:10.1016/j.jsbmb.2007.09.025. 
  4. ^ Kathryn Rhodes Alden; Deitra Leonard Lowdermilk; Mary Catherine Cashion; Shannon E. Perry. Maternity and Women's Health Care - E-Book. Elsevier Health Sciences. 27 December 2013: 135–. ISBN 978-0-323-29368-6.