The metabolism reactions mechanisms of 3-ethoxozepam in rat liver homogenates
DOI:
https://doi.org/10.14739/2310-1210.2015.4.50250Keywords:
Ethoxazepam, Metabolism, In VitroAbstract
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
Bogatskij, A.V., Andronati, S. A., & Golovenko, N. Ya. (1980). Trankvilizatory (1,4-benzdiazepiny i rodstvennye struktury) [Tranquilizers (1.4-benzdiazepines and relative structures)] Kyiv: Naukova Dumka. [in Ukrainian].
Holovenko, M. Ya., Larionov, V. B., & Pavlovskyi, V. I. (2009). Farmakolohichni vlastyvosti preparatu «Levana IS» [Pharmacological properties of drug “Levana IC”]. Visnyk psykhiatrii ta psykhofarmakoterapii, 2(16), 70–73. [in Ukrainian].
Kravchenko, I. A., Radaeva, I. N., & Zhukova, N. A. (2011). Farmakologicheskaya aktivnost' novykh proizvodnykh 1,4-benzdiazepina [Pharmacological activity of new 1.4-benzdiazepine derivatives.] Ukrainskyi naukovo-medychnyi molodizhnyi zhurnal, 4, 60–62. [in Ukrainian].
Zhukova, N. O., Holovenko, M. Ya., & Larionov, V. B. (2012). Farmakokinetychnyi profil ta metabolizm 14S-etoksozepamu v orhanizmi myshei pislia vnutrishnovennoho vvedennia [Pharmacological profile and metabolism of 14C-ethoxazepam in mice after intravenous administration] Klinichna farmatsiia, 16(4), 32–38. [in Ukrainian].
Pavlovskyi, V. I., Semenishina, K. O., Larionov, V. B., & Zhukova, N. O. (2012). Syntez 14С-etoksozepamu ta vyznachennia yoho osnovnykh fizyko-khimichnykh ta radiolohichnykh pokaznykiv [14C-Ethoxazepam synthesis and determination of its main physics-chemical and radiological parameters]. Farmatsevtychnyi zhurnal, 2, 43–49. [in Ukrainian].
Golovenko, N. Ya., Zin'kovskij, V. G. (1978). Opredelenie trankvilizatorov 1,4-benzdiazepinonovogo ryada i ikh metabolitov v biologicheskikh sredakh [Determination of 1.4-benzdiazepine derivatives and their metabolites in biologic medium] Khimiko-farmacevticheskij zhurnal, 12(1), 3–14. [in Russian].
Todeschini, R., & Consonni, V. (2009) Molecular Descriptors for Chemoinformatics. (Vol. 41 (2 Volume Set)). John Wiley & Sons.
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].
Downloads
How to Cite
Issue
Section
License
Authors who publish with this journal agree to the following terms:- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution License that allows others to share the work with an acknowledgement of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgement of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access)