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Methopyrapone

CAS No.: 54-36-4

  • Molecular Formula: C₁₄H₁₄N₂O
  • Molecular Weight: 226.27 g/mol

Chemical type

  • Steroidogenesis inhibitor
[1]
  • Pharmacological inhibitor (11β-hydroxylase inhibitor)
[2]

Key properties

  • Selectively inhibits CYP11B1 and CYP11B2
  • No effect on CYP7A
  • Less potent inhibition of CYP3A4
  • Can increase deoxycorticosterone and androgen levels (hypokalemia, hypertension, edema risks)
  • Considered second-line in women due to hyperandrogenic effects
  • Less potent than osilodrostat
  • Shorter half-life, more frequent dosing
[1]
  • Inhibits the enzyme 11β-hydroxylase, which is crucial for the final step of cortisol synthesis.
[2]
  • Medical therapy for Cushing syndrome
  • Alternative to osilodrostat
[1]
  • Experimental research: Used as a pharmacological treatment in zebrafish larvae to block cortisol production. This allowed researchers to rule out the involvement of endogenous cortisol in the observed effects of CRH on leukocyte migration.
[2]

Classification by use

  • Medications for Cushing syndrome
  • Steroidogenesis inhibitors
[1]
  • Research chemical (pharmacological tool in endocrinology)
[2]

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  1. [Cite:1] Osilodrostat for Cyclic Cushing Disease, AACE Endocrinology and Diabetes, Volume 13, Issue 1, January–February 2026, Pages 17-21
  2. [Cite:2] Corticotropin-releasing hormone enhances the responsivity of macrophages to inflammation in zebrafish, General and Comparative Endocrinology, Volume 373, October 2025, 114815