Determination of Rat 5α-Reductase Type 1 Isozyme Activity and Its Inhibition by Novel Steroidal Oxazolines

August 2010 in “ Acta Biologica Hungarica ”

Mihály Szécsi, Dóra Ondré, Istvan Toth, S. Magony, János Wölfling, Gy-Y. Schneider, J. Julesz

5α-reductase type 1 steroidal oxazolines finasteride rat liver microsomes 2-chlorophenyl substituent fluorine IC50 Propecia

TLDR New steroidal compounds moderately block an enzyme related to testosterone conversion, less effectively than finasteride.

In the 2010 study, researchers developed an in vitro method to measure the activity of the 5α-reductase type 1 isozyme using rat liver microsomes and tested the inhibitory effects of novel steroidal oxazolines on this enzyme. These compounds, with derivatized phenyl substituents, showed moderate inhibitory activity compared to finasteride, with the most potent novel inhibitor having an IC50 value of 0.72 µM versus finasteride's 0.0080 µM. The study found that a 2-chlorophenyl substituent increased inhibitory potential, while fluorine decreased it, suggesting these steroidal compounds could be further researched as potential 5α-reductase type 1 inhibitors. The research was supported by the Hungarian Scientific Research Fund and acknowledged contributions from Dr. Zoltán Tuba and Mihály Szécsi.

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Determination of Rat 5α-Reductase Type 1 Isozyme Activity and Its Inhibition by Novel Steroidal Oxazolines

Research cited in this study

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