|
|||||
|
|
N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands |
|
| Authors: | Grundt Peter Kopajtic Theresa A Katz Jonathan L Newman Amy Hauck |
| Institution: | aMedicinal Chemistry Section, National Institute on Drug Abuse—Intramural Research Program, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA bPsychobiology Section, National Institute on Drug Abuse—Intramural Research Program, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA |
| Abstract: | 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. |
| Keywords: | Monoamine transporters Dopamine transporters Cocaine Muscarinic M1 receptor Benztropine Benztropinamine Ligand binding |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |