Pharmacology, Pharmacokinetics, and Metabolism of Acetothiolutamide, a Novel Nonsteroidal Agonist for the Androgen Receptor

@article{Yin2003PharmacologyPA,
  title={Pharmacology, Pharmacokinetics, and Metabolism of Acetothiolutamide, a Novel Nonsteroidal Agonist for the Androgen Receptor},
  author={Donghua Yin and Huiping Xu and Yali He and Leonid I. Kirkovsky and Duane D. Miller and James T Dalton},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2003},
  volume={304},
  pages={1323 - 1333}
}
  • D. Yin, Huiping Xu, J. Dalton
  • Published 1 March 2003
  • Biology, Chemistry, Medicine
  • Journal of Pharmacology and Experimental Therapeutics
The present study characterized the in vitro androgen receptor (AR) binding affinity, in vitro and in vivo pharmacological activity, and in vivo pharmacokinetics and metabolism of acetothiolutamide, a nonsteroidal AR ligand. AR binding was determined by a competitive binding assay. In vitro AR agonist activity was examined by a cotransfection assay. Acetothiolutamide displayed high AR binding affinity (K i = 4.9 ± 0.2 nM) and full agonist activity in the in vitro studies. Next, the androgenic… 

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