| 词条 | Mespirenone |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = S-[(4aR,4bS,6aS,7S,7aS,8aS,8bS,8cR,9R)-4a,6a-Dimethyl-2,5'-dioxo-2,4',4b,5,5',6,6a,7a,8,8a,8b,8c,9,10-tetradecahydro-3'H,4aH-spiro[cyclopropa[4,5]cyclopenta[1,2-a]phenanthrene-7,2'-furan]-9-yl] ethane thioate | image = Mespirenone.svg | width = | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = Oral | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 87952-98-5 | CAS_supplemental = | ATC_prefix = None | ATC_suffix = | PubChem = 65660 | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 59095 | ChEMBL = 1908314 | UNII = E91TME2I23 | C=25 | H=30 | O=4 | S=1 | molecular_weight = 426.5683 g/mol | smiles = CC(=O)SC1CC2=CC(=O)C=CC2(C3C1C4C5CC5C6(C4(CC3)C)CCC(=O)O6)C | StdInChI_Ref = | StdInChI = InChI=1S/C25H30O4S/c1-13(26)30-19-11-14-10-15(27)4-7-23(14,2)17-5-8-24(3)22(21(17)19)16-12-18(16)25(24)9-6-20(28)29-25/h4,7,10,16-19,21-22H,5-6,8-9,11-12H2,1-3H3/t16-,17+,18+,19-,21+,22+,23+,24+,25+/m1/s1 | StdInChIKey_Ref = | StdInChIKey = CPHJTSJQUQZOLJ-ISIDMKFXSA-N | synonyms = }}Mespirenone (INN) (developmental code name ZK-94679), also known as Δ1-15β,16β-methylenespironolactone, is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone that was never marketed.[1][2] Animal research found that it was 3.3-fold more potent as an antimineralocorticoid relative to spironolactone.[3] In addition to its antimineralocorticoid properties, mespirenone is also a progestogen, antigonadotropin, and antiandrogen.[2][4] It is 2- to 3-fold as potent as spironolactone as a progestogen and antigonadotropin but its antiandrogenic activity is markedly reduced and weak (though still of significance) in comparison.[4][5] Mespirenone is also a potent and specific enzyme inhibitor of 18-hydroxylase and thus of mineralocorticoid biosynthesis.[6] The drug was under development by Schering (now Bayer Schering Pharma) and reached phase II clinical trials but was discontinued in 1989.[7] See also
References1. ^{{cite book|author=J. Elks|title=The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies|url=https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA775|date=14 November 2014|publisher=Springer|isbn=978-1-4757-2085-3|pages=775–}} {{Androgen receptor modulators}}{{Mineralocorticoid receptor modulators}}{{Progesterone receptor modulators}}{{steroid-stub}}2. ^1 {{cite journal | vauthors = Losert W, Bittler D, Buse M, Casals-Stenzel J, Haberey M, Laurent H, Nickisch K, Schillinger E, Wiechert R | title = Mespirenone and other 15,16-methylene-17-spirolactones, a new type of steroidal aldosterone antagonists | journal = Arzneimittelforschung | volume = 36 | issue = 11 | pages = 1583–600 | year = 1986 | pmid = 3028435 | doi = | url = }} 3. ^{{cite book|title=Arzneimittel-Forschung|url=https://books.google.com/books?id=QtcTAQAAMAAJ|year=1991|publisher=Editio Cantor}} 4. ^1 {{cite journal | vauthors = Nishino Y, Schröder H, el Etreby MF | title = Experimental studies on the endocrine side effects of new aldosterone antagonists | journal = Arzneimittelforschung | volume = 38 | issue = 12 | pages = 1800–5 | year = 1988 | pmid = 3245852 | doi = | url = }} 5. ^{{cite journal | vauthors = Opoku J, Kalimi M, Agarwal M, Qureshi D | title = Effect of a new mineralocorticoid antagonist mespirenone on aldosterone-induced hypertension | journal = Am. J. Physiol. | volume = 260 | issue = 2 Pt 1 | pages = E269–71 | year = 1991 | pmid = 1996630 | doi = | url = }} 6. ^{{cite journal | vauthors = Weindel K, Lewicka S, Vecsei P | title = Inhibitory effects of the novel anti-aldosterone compound mespirenone on adrenocortical steroidogenesis in vitro | journal = Arzneimittelforschung | volume = 41 | issue = 9 | pages = 946–9 | year = 1991 | pmid = 1796922 | doi = | url = }} 7. ^{{cite book|author1=Eckhard Ottow|author2=Hilmar Weinmann|title=Nuclear Receptors as Drug Targets|url=https://books.google.com/books?id=iATfLbPgRugC&pg=PA410|date=8 September 2008|publisher=John Wiley & Sons|isbn=978-3-527-62330-3|pages=410–}} 6 : Aldosterone synthase inhibitors|Antimineralocorticoids|Cyclopropanes|Pregnanes|Spiro compounds|Steroidal antiandrogens |
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