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.
Bibliographical noteFunding Information:
This work was funded by the National Institute on Drug Abuse-Intramural Research Program. P.G. was supported by a NIH Visiting Fellowship.
- Dopamine transporters
- Ligand binding
- Monoamine transporters
- Muscarinic M1 receptor