Referenced in: none

Automatically associated channels: Kir2.3

Title: Synthesis and activity of 3-pyridylamine ligands at central nicotinic receptors.

Authors: G Balboni, M Marastoni, S Merighi, P Andrea Borea, R Tomatis

Journal, date & volume: Eur J Med Chem, 2000 Nov , 35, 979-88

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/11137226

Abstract
A series of thirty 2-(3-pyridylaminomethyl)azetidine, pyrrolidine and piperidine analogues as nicotinic acetylcholine receptor (nAChR) ligands was explored. In general, pyrrolidinyl and many azetidinyl compounds were found to bind with enhanced affinity relative to the piperidines. In the three series, the parallel structural changes (stereochemistry, N-methylation and/or chloro substitution) do not consistently lead to parallel shifts in affinity. The more active compounds (K(i) affinity values ranging from 8.9 to 90 nM) were about as analgesic as nicotine in a tail-flick assay in mice after subcutaneous injections.