2-Substituted 3β-Aryltropane Cocaine Analogs Produce Atypical Effects without Inducing Inward-Facing Dopamine Transporter Conformations.

@article{Hong20162Substituted3C,
  title={2-Substituted 3β-Aryltropane Cocaine Analogs Produce Atypical Effects without Inducing Inward-Facing Dopamine Transporter Conformations.},
  author={Weimin Conrad Hong and Theresa A. Kopajtic and Lifen Xu and Stacey A. Lomenzo and Bernandie Jean and Jeffry D. Madura and Christopher K. Surratt and Mark L. Trudell and Jonathan Katz},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2016},
  volume={356 3},
  pages={624-34}
}
Previous structure-activity relationship studies indicate that a series of cocaine analogs, 3β-aryltropanes with 2β-diarylmethoxy substituents, selectively bind to the dopamine transporter (DAT) with nanomolar affinities that are 10-fold greater than the affinities of their corresponding 2α-enantiomers. The present study compared these compounds to cocaine with respect to locomotor effects in mice, and assessed their ability to substitute for cocaine (10 mg/kg, i.p.) in rats trained to… CONTINUE READING

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