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

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Keywords

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