Curtis_2000_Eur.J.Pharmacol_393_155

Reference

Title : A new look at the neuronal nicotinic acetylcholine receptor pharmacophore - Curtis_2000_Eur.J.Pharmacol_393_155
Author(s) : Curtis L , Chiodini F , Spang JE , Bertrand S , Patt JT , Westera G , Bertrand D
Ref : European Journal of Pharmacology , 393 :155 , 2000
Abstract :

Interest in the field of nicotinic receptors has been recently stimulated both by the discovery of the potential therapeutic effects of new agonists, and by the discovery of an association between nicotinic receptor mutations and human neurological diseases. Expression of human receptors in an exogenous system allows their study in isolation. Receptors reconstituted by pairwise injection of either alpha4 or alpha3 with beta2 or beta4 subunits displayed important differences between the resulting receptor subtypes. These results were further compared with those obtained with alpha3:alpha4 fusion proteins. The modifications of either the ligand-binding site in the N-terminal domain or in the ionic pore domain were found to affect the pharmacological properties of the receptors. Finally, the analysis of non-natural derivatives of epibatidine demonstrates how an agonist can be modified to be selective at one receptor subtype or to become an antagonist. These data are well explained on the basis of a three-state allosteric model.

PubMedSearch : Curtis_2000_Eur.J.Pharmacol_393_155
PubMedID: 10771009

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Citations formats

Curtis L, Chiodini F, Spang JE, Bertrand S, Patt JT, Westera G, Bertrand D (2000)
A new look at the neuronal nicotinic acetylcholine receptor pharmacophore
European Journal of Pharmacology 393 :155

Curtis L, Chiodini F, Spang JE, Bertrand S, Patt JT, Westera G, Bertrand D (2000)
European Journal of Pharmacology 393 :155