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

Producción científica: Article › revisión exhaustiva

13 Citas (Scopus)

Resumen

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.

Idioma original	English
Páginas (desde-hasta)	4463-4466
Número de páginas	4
Publicación	Bioorganic and Medicinal Chemistry Letters
Volumen	15
N.º	20
DOI	https://doi.org/10.1016/j.bmcl.2005.07.032
Estado	Published - oct 15 2005

Nota bibliográfica

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).

Financiación

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).

Financiadores	Número del financiador
National Institutes of Health (NIH)	DA 13519
National Institutes of Health (NIH)
National Institute of Mental Health	R01MH047611
National Institute of Mental Health

ASJC Scopus subject areas

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

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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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doi = "10.1016/j.bmcl.2005.07.032",

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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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UR - https://www.scopus.com/pages/publications/24344445278#tab=citedBy

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DO - 10.1016/j.bmcl.2005.07.032

M3 - Article

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AN - SCOPUS:24344445278

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EP - 4466

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

Resumen

Nota bibliográfica

Financiación

ASJC Scopus subject areas

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