The effect of 6-substituted-4′,4″-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor
Bioorganic & Medicinal Chemistry LettersPublished 26 April 2004Open access
Peter Grundt, Theresa Kopajtic, Jonathan L. Katz, Amy Hauck Newman
Citations8
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TL;DR
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.
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.
Keywords
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