Title of article
Subtype-selective nicotinic receptor antagonists: potential as tobacco use cessation agents
Author/Authors
Linda P. Dwoskin، نويسنده , , Sangeetha P. Sumithran، نويسنده , , Jun Zhu، نويسنده , , A. Gabriela Deaciuc، نويسنده , , Joshua T. Ayers، نويسنده , , Peter A. Crooks، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
1863
To page
1867
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794300
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