The effect of 6-substituted-4',4"-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor |
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| Authors: | Grundt Peter Kopajtic Theresa A Katz Jonathan L Hauck Newman Amy |
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| Institution: | Medicinal Chemistry, National Institute on Drug Abuse--Intramural Research Program, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA. pgrundt@intra.nida.nih.gov |
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| Abstract: | A series of racemic 6-hydroxy and carboalkoxy substituted-4('),4"-difluorobenztropines was synthesized and evaluated for binding at the dopamine (DAT), the serotonin (SERT), the norepinephrine (NET) transporters, and the muscarinic M1 receptor. Each of the analogues displaced (3)H]WIN 35,428 (DAT) with a range of affinities from 5.81 to 175 nM and (3)H]pirenzepine (M1), with a range of affinities ( K(i)= -8430 nM). Binding affinities at the SERT and the NET were generally low. |
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