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  • Novel Imidazol-1-ylmethyl Substituted 1,2,5,6-Tetrahydropyrrolo[3,2,1-ij]quinolin-4-ones as Potent and Selective CYP11B1 Inhibitors for the Treatment of Cushing's Syndrome.
  • Yin L, Lucas S, Maurer F, Kazmaier U, Hu Q, Hartmann RW.SourcePharmaceutical and Medicinal Chemistry, Saarland University and Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) , Campus C2-3, D-66123 Saarbrücken, Germany.
  • Journal of medicinal chemistry.J Med Chem.2012 Jul 26;55(14):6629-33. Epub 2012 Jul 12.
  • CYP11B1 inhibition is a promising therapy for Cushing's syndrome. Starting from etomidate, references I and II, the title compounds were designed and synthesized. Cyclopropyl analogue 4 was identified as a CYP11B1 inhibitor more potent (IC(50) = 2.2 nM) than leads and more selective (SF = 11) than I
  • PMID 22788843
  • Screening for modulatory effects on steroidogenesis using the human H295R adrenocortical cell line: a metabolomics approach.
  • Rijk JC, Peijnenburg AA, Blokland MH, Lommen A, Hoogenboom LR, Bovee T.AbstractThe recently OECD validated H295R steroidogenesis assay provides an in vitro alternative to evaluate the potential interference of exogenous compounds with endogenous steroid hormone synthesis. Currently this assay is used for a simple 'negative-positive' screening of compounds using testosterone and estradiol levels as endpoints, measured with specific enzyme immunoassays (EIAs) or targeted liquid chromatography (LC) and gas chromatography (GC) mass spectrometry (MS) methods. However, recent developments in LC-MS and bioinformatics allow more comprehensive approaches to evaluate changes in steroid profiles. In the current work, the H295R cell model was combined with a metabolomics approach to monitor changes in metabolite profiles in both a targeted and untargeted way. H295R cells were exposed for 48 hours to model compounds, i.e. forskolin, abiraterone, prochloraz, ketoconazole, trilostane, formestane, aminoglutethimide, fadrozole, etomidate and metyrapone, known to affect steroidogenesis. After exposure, the levels of 9 natural steroids were determined by a quantitative targeted GC-MS/MS method and compared to a metabolomics method using Ultra Performance Liquid Chromatography Time-Of-Flight Mass Spectrometry (UPLC-ToF-MS). Like the EIAs, both methods were suited for 'negative-positive' screening, but the MS methods also generated specific fingerprints, allowing chemical class prediction of the compound under investigation. Although the targeted GC-MS/MS was more sensitive, which was an advantage regarding analysis of the estrogens 17ß-estradiol and estrone, the untargeted UPLC-ToF-MS was able to evaluate effects on the synthesis of the corticosteroids. Moreover, untargeted comparison of the aligned chemical profiles allowed identification of all signals that are differential between exposed and non-exposed H295R cells. In conclusion, application of a comprehensive metabolite profiling methodology not only provides a tool to screen compounds for steroidogenic modulating properties, but also allows chemical class prediction. As such, steroid profiling methodologies in conjunction with the H295R assay can contribute to the prioritization of chemicals for additional safety testing.
  • Chemical research in toxicology.Chem Res Toxicol.2012 Jul 6. [Epub ahead of print]
  • The recently OECD validated H295R steroidogenesis assay provides an in vitro alternative to evaluate the potential interference of exogenous compounds with endogenous steroid hormone synthesis. Currently this assay is used for a simple 'negative-positive' screening of compounds using testosterone an
  • PMID 22768806


  • Effects of Cortisol on Pregnancy Rate and Corpus Luteum Function in Heifers : An In Vivo Study
  • DUONG Hai Thanh,PIOTROWSKA-TOMALA Katarzyna Karolina,ACOSTA Tomas Javier [他],BAH Mamadou Mousa,SINDEREWICZ Emilia,MAJEWSKA Magdalena,JANKOWSKA Katarzynna,OKUDA Kiyoshi,SKARZYNSKI Dariusz Jan
  • The Journal of reproduction and development 58(2), 223-230, 2012-04-01
  • … In preliminary experiments, doses of cortisol and metyrapone (an inhibitor of cortisol synthesis) were established (n=33). … Metyrapone in effective doses of 500 mg increased the P4 concentration. … Moreover, metyrapone increased P4 and prolonged the CL lifespan in comparison to control animals (P<0.05). …
  • NAID 10030753904
  • 副腎腫瘍の治療 薬物治療 Cushing症候群 (内分泌腺腫瘍--基礎・臨床研究のアップデート) -- (副腎腫瘍)
  • 飯野 和美,沖 隆
  • 日本臨床 69(-) (995), 550-554, 2011-03
  • NAID 40018749433
  • Clinical features and management of ectopic ACTH syndrome at a single institute in Japan
  • Endocrine journal 57(12), 1061-1069, 2010-12-01
  • NAID 10029587142


Buy Metyrapone (CAS 54-36-4), an inhibitor of cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1, from Santa Cruz. Purity: ≥96% ... Metyrapone inhibits the biosynthesis of corticosteroids. Studies report that ...
metyrapone /me·tyr·a·pone/ (mĕ-tēr´ah-pōn) a synthetic compound that selectively inhibits an enzyme responsible for the biosynthesis of corticosteroids; it is used as a diagnostic aid for determination of hypothalamicopituitary ...








  • 下垂体機能検査薬。下垂体ACTH分泌予備能の検査薬。
  • 副腎でのコルチゾール産生を阻害する。



  • 11β-hydroxylase阻害作用によりコルチゾール産生減少 → ネガティブフィードバック機構によりATCH産生亢進 → コルチゾール前駆体 11-deoxycortisol産生↑ → 11-deoxycortisolの代謝産物である17-OHCSの尿中排泄↑
  • 血中ATCHと尿17-OHCSを測定


  • **メトピロンカプセル250mg


  [★] メチラポン metyrapone