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 journalArticlepeer-review

40 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; 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.

Original languageEnglish
Pages (from-to)1863-1867
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume14
Issue number8
DOIs
StatePublished - 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

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