Nicotinic receptors aremembrane proteins involved in several physiological processes. They are considered suitable drug targets for various CNS disorders or conditions, as shown by the large number of compounds which have entered clinical trials. In recent years, nonconventional agonists have been discovered: positive allosteric modulators, allosteric agonists, site-specific agonists and silent desensitizers are compounds able to modulate the receptor interacting at sites different from the orthodox one, or to desensitize the receptor without prior opening. While these new findings can further complicate the pharmacology of these proteins and the design and optimization of ligands, they undoubtedly offer new opportunities to find drugs for the many therapeutic indications involving nicotinic receptors.

Designing selective modulators for the nicotinic receptor subtypes: challenges and opportunities / Dina Manetti, Cristina Bellucci, Niccolo` Chiaramonte, Silvia Dei, Elisabetta Teodori, Maria Novella Romanelli. - In: FUTURE MEDICINAL CHEMISTRY. - ISSN 1756-8919. - STAMPA. - (2018), pp. 433-459. [10.4155/fmc-2017-0169]

Designing selective modulators for the nicotinic receptor subtypes: challenges and opportunities

Dina Manetti;Cristina Bellucci;Niccolo` Chiaramonte;Silvia Dei;Elisabetta Teodori;Maria Novella Romanelli
2018

Abstract

Nicotinic receptors aremembrane proteins involved in several physiological processes. They are considered suitable drug targets for various CNS disorders or conditions, as shown by the large number of compounds which have entered clinical trials. In recent years, nonconventional agonists have been discovered: positive allosteric modulators, allosteric agonists, site-specific agonists and silent desensitizers are compounds able to modulate the receptor interacting at sites different from the orthodox one, or to desensitize the receptor without prior opening. While these new findings can further complicate the pharmacology of these proteins and the design and optimization of ligands, they undoubtedly offer new opportunities to find drugs for the many therapeutic indications involving nicotinic receptors.
2018
433
459
Dina Manetti, Cristina Bellucci, Niccolo` Chiaramonte, Silvia Dei, Elisabetta Teodori, Maria Novella Romanelli
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1112204
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