| 词条 | Estradiol decanoate |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = [(8R,9S,13S,14S,17S)-3-Hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl] decanoate | image = Estradiol decanoate.svg | width = 250px | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = By mouth[1][2] | class = Estrogen; Estrogen ester | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 61748-93-4 | CAS_supplemental = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 66409 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 59783 | UNII = | KEGG = | ChEBI = | ChEMBL = | synonyms = E2D; Estradiol decylate; Estradiol 17β-decanoate; Estra-1,3,5(10)-triene-3,17β-diol 17β-decanoate | C=28 | H=42 | O=3 | SMILES = CCCCCCCCCC(=O)O[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CCC4=C3C=CC(=C4)O)C | StdInChI_Ref = | StdInChI = 1S/C28H42O3/c1-3-4-5-6-7-8-9-10-27(30)31-26-16-15-25-24-13-11-20-19-21(29)12-14-22(20)23(24)17-18-28(25,26)2/h12,14,19,23-26,29H,3-11,13,15-18H2,1-2H3/t23-,24-,25+,26+,28+/m1/s1 | StdInChIKey_Ref = | StdInChIKey = YYFQNZXJGOTFRX-VMBLQBCYSA-N }}Estradiol decanoate (E2D), or estradiol decylate, also known as estradiol 17β-decanoate, is a synthetic steroidal estrogen and an estrogen ester – specifically, the 17β-decanoate (decylate) ester of estradiol – which was studied for use in hormone replacement therapy for ovariectomized women in the late 1970s but was never marketed.[1][2][3] Oral estradiol decanoate in oil at a dosage of 0.25 to 0.5 mg/day for 14 days has been studied in ovariectomized women and found to produce levels of estrone and estradiol with a ratio of about 1:2 (0.5) to 1:1.7 (0.6).[1][2] This is in contrast to oral micronized estradiol, which has an estrone to estradiol ratio of about 5:1 (an 8- to 10-fold difference in ratio relative to oral estradiol decanoate in oil).[4] The normal ratio of estrone to estradiol in women is about 1:2 (0.5) in premenopausal women and about 2:1 in postmenopausal women.[4] As such, oral estradiol decanoate in oil may provide a more physiological and favorable profile of estrone and estradiol levels than oral micronized estradiol.[1][2] The improved estrone to estradiol ratio of oral estradiol decanoate in oil is likely related to absorption via the intestinal lymphatic system, which allows for bypassing of first-pass metabolism in the liver.[5] This is dependent on the fatty acid decanoate ester of estradiol decanoate, and in accordance, oral estradiol decanoate not dissolved in oil has less or absent effects in rodents.[5] Absorption of oral estradiol decanoate in oil via the lymphatic system is analogous to the case of oral testosterone undecanoate in oil.[6] See also
References1. ^1 2 3 {{cite journal | vauthors = Kicovic PM, Luisi M, Franchi F, Alicicco E | title = Effects of orally administered oestradiol decanoate on plasma oestradiol, oestrone and gonadotrophin levels, vaginal cytology, cervical mucus and endometrium in ovariectomized women | journal = Clin. Endocrinol. (Oxf) | volume = 7 | issue = 1 | pages = 73–7 | date = July 1977 | pmid = 880735 | doi = 10.1111/j.1365-2265.1977.tb02941.x | url = }} {{Estrogen receptor modulators}}{{Steroid-stub}}{{Genito-urinary-drug-stub}}2. ^1 2 3 {{cite journal | vauthors = Luisi M, Kicovic PM, Alicicco E, Franchi F | title = Effects of estradiol decanoate in ovariectomized women | journal = J. Endocrinol. Invest. | volume = 1 | issue = 2 | pages = 101–6 | year = 1978 | pmid = 755846 | doi = 10.1007/BF03350355 | url = }} 3. ^{{cite book|author=Ranjit Roy Chaudhury|title=Pharmacology of Estrogens|url=https://books.google.com/books?id=ZIQTAQAAMAAJ|date=1 January 1981|publisher=Elsevier Science & Technology Books|isbn=978-0-08-026869-9|page=36}} 4. ^1 {{cite journal | vauthors = Kuhl H | title = Pharmacology of estrogens and progestogens: influence of different routes of administration | journal = Climacteric | volume = 8 Suppl 1 | issue = | pages = 3–63 | year = 2005 | pmid = 16112947 | doi = 10.1080/13697130500148875 | url = http://hormonebalance.org/images/documents/Kuhl%2005%20%20Pharm%20Estro%20Progest%20Climacteric_1313155660.pdf}} 5. ^1 {{cite journal | vauthors = de Visser J, van der Vies J | title = Oestrogenic activity of oestradiol-decanoate after oral administration to rodents | journal = Acta Endocrinol. | volume = 85 | issue = 2 | pages = 422–8 | date = June 1977 | pmid = 577331 | doi = | url = }} 6. ^{{cite book|author=Alexandre Hohl|title=Testosterone: From Basic to Clinical Aspects|url=https://books.google.com/books?id=Et6TDgAAQBAJ&pg=PA207|date=30 March 2017|publisher=Springer|isbn=978-3-319-46086-4|pages=207–}} 5 : Abandoned drugs|Estradiol esters|Estranes|Prodrugs|Synthetic estrogens |
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