@article {10.3844/ajbbsp.2016.263.269,
article_type = {journal},
title = {A Phenolic Ester of O-Desmethylvenlafaxine (ODV) Improves Uptake of ODV into the Brain},
author = {Zhang, Yang and Yang, Zhichao and Zhao, Sen and Zhou, Hongli},
volume = {12},
number = {4},
year = {2016},
month = {Dec},
pages = {263-269},
doi = {10.3844/ajbbsp.2016.263.269},
url = {https://thescipub.com/abstract/ajbbsp.2016.263.269},
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.},
journal = {American Journal of Biochemistry and Biotechnology},
publisher = {Science Publications}
}