Subtype-selective nicotinic receptor antagonists: Potential as tobacco use cessation agents

Linda P. Dwoskin; Sangeetha P. Sumithran; Jun Zhu; A. Gabriela Deaciuc; Joshua T. Ayers; Peter A. Crooks

doi:10.1016/j.bmcl.2003.10.073

Subtype-selective nicotinic receptor antagonists: Potential as tobacco use cessation agents

Linda P. Dwoskin, Sangeetha P. Sumithran, Jun Zhu, A. Gabriela Deaciuc, Joshua T. Ayers, Peter A. Crooks

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

38 Scopus citations

Abstract

N-n-Alkylpicolinium and N,N′-alkyl-bis-picolinium analogues were assessed in nicotinic receptor (nAChR) assays. The most potent and subtype-selective analogue, N,N′-dodecyl-bis-picolinium bromide (bPiDDB), inhibited nAChRs mediating nicotine-evoked [³H]dopamine release (IC₅₀=5 nM; I_max of 60%), and did not interact with α4β2* or α7* nAChRs. bPiDDB represents the current lead compound for development as a tobacco use cessation agent.

Original language	English
Pages (from-to)	1863-1867
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	8
DOIs	https://doi.org/10.1016/j.bmcl.2003.10.073
State	Published - Apr 19 2004

Bibliographical note

Funding Information:
This work was supported by grants from the National Institute of Health (DA00399 and DA10934).

ASJC Scopus subject areas

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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.bmcl.2003.10.073

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title = "Subtype-selective nicotinic receptor antagonists: Potential as tobacco use cessation agents",

abstract = "N-n-Alkylpicolinium and N,N′-alkyl-bis-picolinium analogues were assessed in nicotinic receptor (nAChR) assays. The most potent and subtype-selective analogue, N,N′-dodecyl-bis-picolinium bromide (bPiDDB), inhibited nAChRs mediating nicotine-evoked [3H]dopamine release (IC50=5 nM; Imax of 60%), and did not interact with α4β2* or α7* nAChRs. bPiDDB represents the current lead compound for development as a tobacco use cessation agent.",

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T2 - Potential as tobacco use cessation agents

AU - Dwoskin, Linda P.

AU - Sumithran, Sangeetha P.

AU - Zhu, Jun

AU - Deaciuc, A. Gabriela

AU - Ayers, Joshua T.

AU - Crooks, Peter A.

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AB - N-n-Alkylpicolinium and N,N′-alkyl-bis-picolinium analogues were assessed in nicotinic receptor (nAChR) assays. The most potent and subtype-selective analogue, N,N′-dodecyl-bis-picolinium bromide (bPiDDB), inhibited nAChRs mediating nicotine-evoked [3H]dopamine release (IC50=5 nM; Imax of 60%), and did not interact with α4β2* or α7* nAChRs. bPiDDB represents the current lead compound for development as a tobacco use cessation agent.

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Subtype-selective nicotinic receptor antagonists: Potential as tobacco use cessation agents

Abstract

Bibliographical note

ASJC Scopus subject areas

UN SDGs

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