525596-64-9Relevant academic research and scientific papers
bis-Azaaromatic quaternary ammonium analogues: Ligands for α4β2* and α7* subtypes of neuronal nicotinic receptors
Ayers, Joshua T.,Dwoskin, Linda P.,Deaciuc,Grinevich, Vladimir P.,Zhu, Jun,Crooks, Peter A.
, p. 3067 - 3071 (2002)
A series of bis-nicotinium, bis-pyridinium, bis-picolinium, bis-quinolinium and bis-isoquinolinium compounds was evaluated for their binding affinity at nicotinic acetylcholine receptors (nAChRs) using rat brain membranes. N,N′-Decane-1,12-diyl-bis-nicoti
Subtype-selective nicotinic receptor antagonists: Potential as tobacco use cessation agents
Dwoskin, Linda P.,Sumithran, Sangeetha P.,Zhu, Jun,Deaciuc, A. Gabriela,Ayers, Joshua T.,Crooks, Peter A.
, p. 1863 - 1867 (2004)
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.
BIS-PYRIDINO CONTAINING COMPOUNDS FOR USE IN THE TREATMENT OF CNS PATHOLOGIES
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Page/Page column 23, (2008/06/13)
N-n-Alkylation of nicotine converts nicotine from an agonist into an antagonist specifically for neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogs 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.
