Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands

Guangrong Zheng; Linda P. Dwoskin; Agripina G. Deaciuc; Peter A. Crooks

doi:10.1016/j.bmcl.2005.07.032

Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands

Guangrong Zheng, Linda P. Dwoskin, Agripina G. Deaciuc, Peter A. Crooks

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

13 Scopus citations

Abstract

A series of tropane derivatives has been synthesized as lobelane analogues and evaluated for their binding affinity at the vesicular monoamine transporter-2 (VMAT2), and at α4β2* and α7* nicotinic acetylcholine receptors. The trop-2-ene analogues 4a and 4b exhibited good affinity and high selectivity for VMAT2.

Original language	English
Pages (from-to)	4463-4466
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	20
DOIs	https://doi.org/10.1016/j.bmcl.2005.07.032
State	Published - Oct 15 2005

Bibliographical note

Funding Information:
This research was supported by NIH Grant DA 13519. The authors also gratefully acknowledge the generous gift of [ 3 H]DTBZ from Dr. Michael R. Kilbourn (supported by NIH Grant MH 47611).

Keywords

Psychostimulant abuse
Tropane analogues
VMAT2 ligands

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2005.07.032

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title = "Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands",

abstract = "A series of tropane derivatives has been synthesized as lobelane analogues and evaluated for their binding affinity at the vesicular monoamine transporter-2 (VMAT2), and at α4β2* and α7* nicotinic acetylcholine receptors. The trop-2-ene analogues 4a and 4b exhibited good affinity and high selectivity for VMAT2.",

keywords = "Psychostimulant abuse, Tropane analogues, VMAT2 ligands",

author = "Guangrong Zheng and Dwoskin, {Linda P.} and Deaciuc, {Agripina G.} and Crooks, {Peter A.}",

note = "Funding Information: This research was supported by NIH Grant DA 13519. The authors also gratefully acknowledge the generous gift of [ 3 H]DTBZ from Dr. Michael R. Kilbourn (supported by NIH Grant MH 47611). ",

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AU - Zheng, Guangrong

AU - Dwoskin, Linda P.

AU - Deaciuc, Agripina G.

AU - Crooks, Peter A.

N1 - Funding Information: This research was supported by NIH Grant DA 13519. The authors also gratefully acknowledge the generous gift of [ 3 H]DTBZ from Dr. Michael R. Kilbourn (supported by NIH Grant MH 47611).

PY - 2005/10/15

Y1 - 2005/10/15

N2 - A series of tropane derivatives has been synthesized as lobelane analogues and evaluated for their binding affinity at the vesicular monoamine transporter-2 (VMAT2), and at α4β2* and α7* nicotinic acetylcholine receptors. The trop-2-ene analogues 4a and 4b exhibited good affinity and high selectivity for VMAT2.

AB - A series of tropane derivatives has been synthesized as lobelane analogues and evaluated for their binding affinity at the vesicular monoamine transporter-2 (VMAT2), and at α4β2* and α7* nicotinic acetylcholine receptors. The trop-2-ene analogues 4a and 4b exhibited good affinity and high selectivity for VMAT2.

KW - Psychostimulant abuse

KW - Tropane analogues

KW - VMAT2 ligands

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 20

ER -

Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

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