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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, N.I.H., Intramural
MeSH terms
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Amines
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Benztropine / chemistry*
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Binding Sites
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Citalopram / chemistry
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Cocaine / chemistry
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Dopamine Plasma Membrane Transport Proteins / chemistry*
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Dopamine Plasma Membrane Transport Proteins / metabolism
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Fluoxetine / analogs & derivatives
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Fluoxetine / chemistry
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Kinetics
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Ligands
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Models, Molecular
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Molecular Conformation
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Muscarinic Antagonists / chemistry
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Parasympatholytics / chemistry
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Pirenzepine / chemistry
Substances
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Amines
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Dopamine Plasma Membrane Transport Proteins
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Ligands
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Muscarinic Antagonists
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Parasympatholytics
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Fluoxetine
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Citalopram
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nisoxetine
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Benztropine
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Pirenzepine
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Cocaine