Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release

Peter A. Crooks; Joshua T. Ayers; Rui Xu; Sangeetha P. Sumithran; Vladimir P. Grinevich; Lincoln H. Wilkins; A. Gabriela Deaciuc; David D. Allen; Linda P. Dwoskin

doi:10.1016/j.bmcl.2003.10.074

Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release

Peter A. Crooks
, Joshua T. Ayers
, Rui Xu
, Sangeetha P. Sumithran
, Vladimir P. Grinevich
, Lincoln H. Wilkins
, A. Gabriela Deaciuc
, David D. Allen
, Linda P. Dwoskin

Producción científica: Article › revisión exhaustiva

32 Citas (Scopus)

Resumen

N-n-Alkylation of nicotine converts it from an agonist into an antagonist at neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogues exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter.

Idioma original	English
Páginas (desde-hasta)	1869-1874
Número de páginas	6
Publicación	Bioorganic and Medicinal Chemistry Letters
Volumen	14
N.º	8
DOI	https://doi.org/10.1016/j.bmcl.2003.10.074
Estado	Published - abr 19 2004

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.2003.10.074

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Crooks, P. A., Ayers, J. T., Xu, R., Sumithran, S. P., Grinevich, V. P., Wilkins, L. H., Deaciuc, A. G., Allen, D. D., & Dwoskin, L. P. (2004). Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release. Bioorganic and Medicinal Chemistry Letters, 14(8), 1869-1874. https://doi.org/10.1016/j.bmcl.2003.10.074

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AU - Xu, Rui

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AU - Grinevich, Vladimir P.

AU - Wilkins, Lincoln H.

AU - Deaciuc, A. Gabriela

AU - Allen, David D.

AU - Dwoskin, Linda P.

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AB - N-n-Alkylation of nicotine converts it from an agonist into an antagonist at neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogues exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter.

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ER -

Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release

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ASJC Scopus subject areas

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