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  • Title: Norharman (beta-carboline) as a potent inhibitory ligand for steroidogenic cytochromes P450 (CYP11 and CYP17).
    Author: Kühn-Velten WN.
    Journal: Eur J Pharmacol; 1993 Nov 30; 250(1):R1-3. PubMed ID: 8119304.
    Abstract:
    Norharman (beta-carboline, a so-called mammalian alkaloid) is identified as a high-affinity type II ligand for two steroidogenic cytochromes P450, viz. CYP11 in rat adrenal mitochondria and CYP17 in rat testicular microsomes. Progesterone binding to CYP17 is competitively inhibited, with Ki = 2.6 microM norharman, whereas harman, tetrahydronorharman and tetrahydroharman are nearly ineffective. The potential role of norharman as an endogenous modulator of steroid hormone biosynthesis and as a basic drug for development of more specific cytochrome P450 inhibitors is emphasized.
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