| Literature DB >> 15474055 |
Winnie Deuther-Conrad1, Jörg Thomas Patt, Dominik Feuerbach, Florian Wegner, Peter Brust, Jörg Steinbach.
Abstract
The subtype-specificity of newly synthesised epibatidine-related compounds, norchloro-fluoro-homoepibatidine (NCFHEB) and derivatives, to neuronal nicotinic acetylcholine receptors (nAChR) has been investigated. NCFHEBs were assayed in competitive binding assays to (+/-)-[(3)H]epibatidine-labelled rat thalamic nAChRs and human alpha4beta2, alpha3beta4, and alpha7 nAChRs, expressed in stably transfected HEK-293 and SH-SY5Y cells. The binding affinity of (+)-NCFHEB (K(i): 0.064 nM) and (-)-NCFHEB (K(i): 0.112 nM) to human alpha4beta2 nAChR is in the same order of magnitude as that of epibatidine (K(i): 0.014 nM). However, because the affinity of both NCFHEB-enantiomers to human alpha3beta4 nAChR is up to 65 times lower than that of epibatidine, the alpha4beta2 subtype-specificity of NCFHEB is increased up to 1,400% compared to epibatidine.Entities:
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Year: 2004 PMID： 15474055 DOI： 10.1016/j.farmac.2004.07.004
Source DB: PubMed Journal: Farmaco ISSN： 0014-827X