The effect of 6-substituted-4′,4″- difluorobenztropines on monoamine transporters and the muscarinic M1 receptor

Peter Grundt; Theresa A. Kopajtic; Jonathan L. Katz; Amy Hauck Newman

doi:10.1016/j.bmcl.2004.03.075

The effect of 6-substituted-4^′,4″- difluorobenztropines on monoamine transporters and the muscarinic M1 receptor

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

Chemistry & Biochemistry

Research output: Contribution to journal › Article › peer-review

10 Scopus citations

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 [³H]WIN 35,428 (DAT) with a range of affinities from 5.81 to 175nM and [³H]pirenzepine (M1), with a range of affinities (K _i=27.0-8430nM). Binding affinities at the SERT and the NET were generally low.

Original language	English (US)
Pages (from-to)	3295-3298
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	12
DOIs	https://doi.org/10.1016/j.bmcl.2004.03.075
State	Published - Jun 21 2004

Bibliographical note

Funding Information:
This work was funded by the National Institute on Drug Abuse-Intramural Research Program. P.G. was supported by a NIH Visiting Fellowship.

Keywords

Benztropine
Ligand binding
Monoamine transporters
Muscarinic M1 receptor

Publisher link

10.1016/j.bmcl.2004.03.075

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Cite this

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title = "The effect of 6-substituted-4′,4″- difluorobenztropines on monoamine 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 [3H]WIN 35,428 (DAT) with a range of affinities from 5.81 to 175nM and [3H]pirenzepine (M1), with a range of affinities (K i=27.0-8430nM). Binding affinities at the SERT and the NET were generally low.",

keywords = "Benztropine, Ligand binding, Monoamine transporters, Muscarinic M1 receptor",

author = "Peter Grundt and Kopajtic, \{Theresa A.\} and Katz, \{Jonathan L.\} and Newman, \{Amy Hauck\}",

note = "Funding Information: This work was funded by the National Institute on Drug Abuse-Intramural Research Program. P.G. was supported by a NIH Visiting Fellowship. ",

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AU - Katz, Jonathan L.

AU - Newman, Amy Hauck

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KW - Benztropine

KW - Ligand binding

KW - Monoamine transporters

KW - Muscarinic M1 receptor

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