The metabolism reactions mechanisms of 3-ethoxozepam in rat liver homogenates

Authors

  • N. Ya. Golovenko
  • V. B. Larionov
  • I. P. Valivodz
  • N. A. Zhukova

DOI:

https://doi.org/10.14739/2310-1210.2015.4.50250

Keywords:

Ethoxazepam, Metabolism, In Vitro

Abstract

7-bromo-5-phenyl-3-ethoxy-1,2-dihydro-3H-1,4-benzdiazepine-2-on (ethoxozepam) is one of promising possible drugs with analgesic activity.

The aim of the work was studying of 14C-ethoxozepam possible metabolism pathways in vitro and estimating their efficacy in rat liver homogenate.

Methods and results. Using preparative thin-layer radiochromatography the fact of radioizotope label (in alcoxy group) elimination from molecule had been found.

Conclusions. The process intensity is in range 37,1±11,7% of the total maximal biotransformation of lipophilic metabolites. The possible metabolism scheme, through intermediate, hydroxylated in the heteroring 3 position, been suggested.

References

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Bogatskij, A. V., Golovenko, N. Ya., Andronati, S. A., Kolomojchenko, G. Yu., & Zhilina, Z.I. (1978). Uchastie redoks-cepi mikrosom pecheni krys v suzhenii kol'ca 1,4-benzdiazepinov [Participating of rat liver microsome redox-chain in reduction of the ring of 1.4-benzdiazepines]. Doklady Akademii nauk SSSR, 1(234), 215–218. [in Russian].

How to Cite

1.
Golovenko NY, Larionov VB, Valivodz IP, Zhukova NA. The metabolism reactions mechanisms of 3-ethoxozepam in rat liver homogenates. Zaporozhye Medical Journal [Internet]. 2015Sep.16 [cited 2024Nov.23];17(4). Available from: http://zmj.zsmu.edu.ua/article/view/50250

Issue

Section

Problems of pharmacy