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Frequency: Quarterly
ISSN: 1553-3468 (Print)
ISSN: 1558-6332 (Online)
Research Article Open Access

A Phenolic Ester of O-Desmethylvenlafaxine (ODV) Improves Uptake of ODV into the Brain

Yang Zhang1, Zhichao Yang2, Sen Zhao2 and Hongli Zhou1
  • 1 Jilin Institute of Chemical Technology, China
  • 2 Jilin University, China

Abstract

In this study, the in vitro stabilities of a promising O-Desmethylvenlafaxine (ODV) phenolic ester prodrug O-19 in aqueous solution, rat whole blood and rat liver microsomes were investigated. In addition, the in vivo drug metabolites were determined using LC-TOFMS-IDA-MS/MS. O-19 exhibits high stabilities at any pH encountered in the gastrointestinal tract, its half live (t1/2) spans the range 5.0±0.18 d ~ 686±29.5 d. However, O-19 experiences rapid enzymatic hydrolysis in rat whole blood (t1/2 = 3.6±0.53 min) and rat liver microsomes (t1/2 = 9.5±1.53 min). The metabolic profile of O-19 is similar to that of ODV. Besides ODV itself, five metabolites are identified in rat urine (M1~M5) and faeces (M1, M4), no obvious toxic metabolite is detected.

American Journal of Biochemistry and Biotechnology
Volume 12 No. 4, 2016, 263-269

DOI: https://doi.org/10.3844/ajbbsp.2016.263.269

Submitted On: 22 October 2016 Published On: 11 December 2016

How to Cite: Zhang, Y., Yang, Z., Zhao, S. & Zhou, H. (2016). A Phenolic Ester of O-Desmethylvenlafaxine (ODV) Improves Uptake of ODV into the Brain. American Journal of Biochemistry and Biotechnology, 12(4), 263-269. https://doi.org/10.3844/ajbbsp.2016.263.269

Open AccessCopyright: © 2016 Yang Zhang, Zhichao Yang, Sen Zhao and Hongli Zhou. This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

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Keywords

  • O-Desmethylvenlafaxine
  • Ester
  • O-19
  • Stabilities
  • Metabolites