Novel ligands for neuronal nicotinic receptor subtypes: synthetic, pharmacological and molecular docking studies
Poster
Data di Pubblicazione:
2012
Citazione:
Novel ligands for neuronal nicotinic receptor subtypes: synthetic, pharmacological and molecular docking studies / C. Matera, D.Y. Pomè, C.M.L. Dallanoce, G. Grazioso, L. Pucci, S. Fucile, C. Gotti, F. Clementi, M. De Amici - In: NPCF6 : nuove prospettive in chimica farmaceutica[s.l] : Società Chimica Italiana, 2012 Apr 16. - pp. 27-27 (( Intervento presentato al 6. convegno Nuove Prospettive in chimica farmaceutica tenutosi a Riccione nel 2012.
Abstract:
Neuronal nicotinic acetylcholine receptors (nAChRs) are pentameric proteins made up
of homomeric or heteromeric combinations of α and α/β subunits, whose differential
association confers specific structural and functional properties to the resulting
subtypes. The α4β2 and the α7 nAChRs are by far the most expressed in the central
nervous system (CNS), whereas the α3β4 subtype is predominant in the sensory and
autonomic ganglia and in a subpopulation of neurons in the medial habenula (MHN)
and interpeduncular nucleus (IPN) in the CNS [1]. Recently, behavioral and functional
studies have further indicated the crucial role of nAChRs in nicotine reward, addiction
and expression of withdrawal. The α4 and β2 subunits appear to be crucial for nicotine
dependence and the α3β4 nAChR subtype seems to be implicated in addiction to
nicotine and other drugs of abuse [2]. As an extension of our research in this field [3],
we aimed at deepening the investigation on the involvement of nAChR subtypes in
each of the aspects of tobacco addiction. To such an end, we designed and
synthesized the set of novel compounds 4-9, which may be related to Nicotine 1,
Epibatidine 2 and Anabaseine 3.
In the new derivatives, the pyridine ring featuring the parent ligands was replaced by a
3-hydroxybenzene or a 3-hydroxymethylbenzene moiety. The synthetic approach to the
target compounds, the data of their pharmacological screening as well as the results of
molecular modeling investigations will be presented and discussed.
Tipologia IRIS:
03 - Contributo in volume
Elenco autori:
C. Matera, D.Y. Pomè, C.M.L. Dallanoce, G. Grazioso, L. Pucci, S. Fucile, C. Gotti, F. Clementi, M. De Amici
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Titolo del libro:
NPCF6 : nuove prospettive in chimica farmaceutica