N-8-substituted benztropinamine analogs as selective dopamine transporter ligands

Peter Grundt, Theresa A. Kopajtic, Jonathan L. Katz, Amy Hauck Newman

Research output: Contribution to journalArticlepeer-review

6 Scopus citations


A series of N-8-substituted benztropinamines was synthesized and evaluated for binding at the dopamine (DAT), serotonin (SERT), norepinephrine (NET) transporters, and muscarinic M1 receptors. In general, the isosteric replacement of the C-3 benzhydrol ether of benztropine by a benzhydryl amino group was well tolerated at the DAT. However, for certain N-8 substituted derivatives, selectivity over muscarinic M1 receptor affinity was reduced.

Original languageEnglish (US)
Pages (from-to)5419-5423
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number24
StatePublished - Dec 15 2005

Bibliographical note

Funding Information:
This work was funded by the National Institute on Drug Abuse-Intramural Research Program. P.G. was supported by a NIH Visiting Fellowship.


  • Benztropinamine
  • Benztropine
  • Cocaine
  • Dopamine transporters
  • Ligand binding
  • Monoamine transporters
  • Muscarinic M1 receptor


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