Metabolism and Renal Elimination of Gaboxadol in Humans: Role of UDP-Glucuronosyltransferases and Transporters

  title={Metabolism and Renal Elimination of Gaboxadol in Humans: Role of UDP-Glucuronosyltransferases and Transporters},
  author={Xiaoyan Chu and Yuexia Liang and Xiaoxin Cai and Karla G. Cuevas-Licea and Ronda K. Rippley and Kelem Kassahun and Magang Shou and Matthew P. Braun and George A. Doss and M. Reza Anari and Raymond Evers},
  journal={Pharmaceutical Research},
PurposeGaboxadol, a selective extrasynaptic agonist of the delta-containing γ-aminobutyric acid type A (GABAA) receptor, is excreted in humans into the urine as parent drug and glucuronide conjugate. The goal of this study was to identify the UDP-Glucuronosyltransferase (UGT) enzymes and the transporters involved in the metabolism and active renal secretion of gaboxadol and its metabolite in humans.Methods. The structure of the glucuronide conjugate of gaboxadol in human urine was identified by… 
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