| 词条 | 16α-LE2 |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = 3,17β-Dihydroxy-16α,21-epoxy-19-nor-17α-pregna-1,3,5(10)-trien-21-one | image = 16aLE2_structure.png | width = 250 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 406483-39-4 | CAS_supplemental = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 8037946 | UNII = | KEGG = | ChEBI = | ChEMBL = | C=20 | H=24 | O=4 | molecular_weight = 328.402 g/mol | smiles = O=C1O[C@@]2([H])[C@]([C@@]3(C)CC[C@]4([H])C5=CC=C(C=C5CC[C@@]4([H])[C@]3([H])C2)O)(C1)O | StdInChI_Ref = | StdInChI = InChI=1S/C20H24O4/c1-19-7-6-14-13-5-3-12(21)8-11(13)2-4-15(14)16(19)9-17-20(19,23)10-18(22)24-17/h3,5,8,14-17,21,23H,2,4,6-7,9-10H2,1H3/t14-,15-,16+,17-,19+,20+/m1/s1 | StdInChIKey_Ref = | StdInChIKey = NLUGVTJBNRSIKH-UQZPWQSVSA-N | synonyms = }}16α-LE2, or 16α-lactone-estradiol, also known as 3,17β-dihydroxy-19-nor-17α-pregna-1,3,5-(10)-triene-21,16α-lactone, is a synthetic, steroidal estrogen featuring a estradiol core. It is a highly potent and selective agonist of the ERα that is used in scientific research to study the function of the ERα.[1][2] It has 265-fold higher potency in transactivation assays of the ERα relative to the ERβ and 70-fold preference in binding affinity for the ERα over the ERβ.[2] In rodents, 16α-LE2 has no effect on ovarian follicle development, whereas the highly ERβ-selective agonist 8β-VE2 stimulates follicular growth and to a comparable extent as estradiol, indicating that the ERβ and not the ERα is involved in the effects of estrogen on ovarian follicles.[2][3] In contrast, 16α-LE2 stimulates uterine weight, whereas 8β-VE2 has no effect, indicating that the ERα and not the ERβ is involved in the effects of estrogen on the uterus.[2] Research has determined through experimental rodent studies with estradiol, 16α-LE2, and 8β-VE2 that the positive, protective effects of estrogens on bone formation resorption and bone mineral density are mediated via the ERα, whereas the ERβ does not appear to be involved.[4] See also
References1. ^{{cite book|author=I Shaw|title=Endocrine-Disrupting Chemicals in Food|url=https://books.google.com/books?id=x6ejAgAAQBAJ&pg=PA550|date=31 March 2009|publisher=Elsevier|isbn=978-1-84569-574-3|pages=550–}} {{Estrogen receptor modulators}}{{steroid-stub}}{{genito-urinary-drug-stub}}2. ^1 2 3 {{cite journal | vauthors = Hegele-Hartung C, Siebel P, Peters O, Kosemund D, Müller G, Hillisch A, Walter A, Kraetzschmar J, Fritzemeier KH | title = Impact of isotype-selective estrogen receptor agonists on ovarian function | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 101 | issue = 14 | pages = 5129–34 | year = 2004 | pmid = 15037755 | pmc = 387385 | doi = 10.1073/pnas.0306720101 | url = }} 3. ^{{cite book|author1=Tony M. Plant|author2=Anthony J. Zeleznik|title=Knobil and Neill's Physiology of Reproduction|url=https://books.google.com/books?id=I1ACBAAAQBAJ&pg=PA1150|date=15 November 2014|publisher=Academic Press|isbn=978-0-12-397769-4|pages=1150–}} 4. ^{{cite journal | vauthors = Hertrampf T, Schleipen B, Velders M, Laudenbach U, Fritzemeier KH, Diel P | title = Estrogen receptor subtype-specific effects on markers of bone homeostasis | journal = Mol. Cell. Endocrinol. | volume = 291 | issue = 1-2 | pages = 104–8 | year = 2008 | pmid = 18433985 | doi = 10.1016/j.mce.2008.03.003 | url = }} 3 : Estranes|Lactones|Synthetic estrogens |
| 随便看 |
|
开放百科全书收录14589846条英语、德语、日语等多语种百科知识，基本涵盖了大多数领域的百科知识，是一部内容自由、开放的电子版国际百科全书。