Literature DB >> 15149693

The effect of 6-substituted-4',4"-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor.

Peter Grundt1, Theresa A Kopajtic, Jonathan L Katz, Amy Hauck Newman.   

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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Year:  2004        PMID: 15149693     DOI: 10.1016/j.bmcl.2004.03.075

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Substrate Conformation Correlates with the Outcome of Hyoscyamine 6β-Hydroxylase Catalyzed Oxidation Reactions.

Authors:  Richiro Ushimaru; Mark W Ruszczycky; Wei-Chen Chang; Feng Yan; Yung-Nan Liu; Hung-Wen Liu
Journal:  J Am Chem Soc       Date:  2018-06-11       Impact factor: 15.419

2.  Comparative structure-activity relationships of benztropine analogues at the dopamine transporter and histamine H(1) receptors.

Authors:  Santosh S Kulkarni; Theresa A Kopajtic; Jonathan L Katz; Amy Hauck Newman
Journal:  Bioorg Med Chem       Date:  2006-02-03       Impact factor: 3.641

3.  New Drugs, Old Targets: Tweaking the Dopamine System to Treat Psychostimulant Use Disorders.

Authors:  Amy Hauck Newman; Therese Ku; Chloe J Jordan; Alessandro Bonifazi; Zheng-Xiong Xi
Journal:  Annu Rev Pharmacol Toxicol       Date:  2021-01-06       Impact factor: 16.459

  3 in total

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