Pharmacokinetic Parameters and Mechanisms of Inhibition of Rat Type 1 and 2 Steroid 5α-Reductases: Determinants for Different In Vivo Activities of GI198745 and Finasteride in the Rat

    October 2001 in “ Biochemical Pharmacology ”
    J. Darren Stuart, Frank X. Lee, Deborah Simpson Noel … H. Neal Bramson
    Studysummary This study found that GI198745 acts as a time-dependent inhibitor of rat 5α-reductase type 2 but a rapid-equilibrium inhibitor of type 1, potentially making it more effective than finasteride in preventing rat prostate growth.
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    Research cited in this study 3

    1. Inhibition of Rat Alpha-Reductases by Finasteride: Evidence for Isozyme Differences in the Mechanism of Inhibition The Journal of Steroid Biochemistry and Molecular Biology · 1997
    2. Mechanism-Based Inhibition of Human Steroid 5α-Reductase by Finasteride: Enzyme-Catalyzed Formation of NADP-Dihydrofinasteride, a Potent Bisubstrate Analog Inhibitor Journal of the American Chemical Society · 1996
    3. Finasteride: A Slow-Binding 5-Alpha-Reductase Inhibitor Biochemistry · 1993

    Related research 4

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    2. Synthesis and Evaluation of 2'-Substituted 4-(4'-Carboxy- or 4'-Carboxymethylbenzylidene)-N-Acylpiperidines: Highly Potent and In Vivo Active Steroid 5α-Reductase Type 2 Inhibitors Journal of Medicinal Chemistry · 2002
    3. Pharmacokinetic Parameters and Mechanisms of Inhibition of Rat Type 1 and 2 Steroid 5α-Reductases: Determinants for Different In Vivo Activities of GI198745 and Finasteride in the Rat Biochemical Pharmacology · 2001
    4. Mechanism-Based Inhibition of Human Steroid 5α-Reductase by Finasteride: Enzyme-Catalyzed Formation of NADP-Dihydrofinasteride, a Potent Bisubstrate Analog Inhibitor Journal of the American Chemical Society · 1996