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

D Manetti, C Bellucci, N Chiaramonte… - Future Medicinal …, 2018 - Taylor & Francis
Nicotinic receptors are membrane proteins involved in several physiological processes.
They are considered suitable drug targets for various CNS disorders or conditions, as shown …

Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system

A Taly, PJ Corringer, D Guedin, P Lestage… - Nature reviews Drug …, 2009 - nature.com
Nicotinic receptors—a family of ligand-gated ion channels that mediate the effects of the
neurotransmitter acetylcholine—are among the most well understood allosteric membrane …

Positive and negative modulation of nicotinic receptors

HR Arias - Advances in protein chemistry and structural biology, 2010 - Elsevier
Nicotinic acetylcholine receptors (AChRs) are one of the best characterized ion channels
from the Cys-loop receptor superfamily. The study of acetylcholine binding proteins and …

Cholinergic nicotinic receptors: competitive ligands, allosteric modulators, and their potential applications

MN Romanelli, F Gualtieri - Medicinal research reviews, 2003 - Wiley Online Library
Discovery of the important role played by nicotinic acetylcholine receptors (nAChRs) in
several CNS disorders has called attention to these membrane proteins and to ligands able …

Central nicotinic receptors: structure, function, ligands, and therapeutic potential

MN Romanelli, P Gratteri, L Guandalini… - ChemMedChem …, 2007 - Wiley Online Library
The growing interest in nicotinic receptors, because of their wide expression in neuronal and
non‐neuronal tissues and their involvement in several important CNS pathologies, has …

Recent advances in the discovery of nicotinic acetylcholine receptor allosteric modulators

D Manetti, S Dei, HR Arias, L Braconi, A Gabellini… - Molecules, 2023 - mdpi.com
Positive allosteric modulators (PAMs), negative allosteric modulators (NAMs), silent
agonists, allosteric activating PAMs and neutral or silent allosteric modulators are …

Nicotinic acetylcholine receptors as drug targets

RC Hogg, D Bertrand - Current Drug Targets-CNS & …, 2004 - ingentaconnect.com
While it has long been documented that nicotine contained in tobacco leaves gives rise to
major public health problems it has also been observed that this alkaloid can have …

Nicotinic receptors: From protein allostery to computational neuropharmacology

M Cecchini, JP Changeux - Molecular Aspects of Medicine, 2022 - Elsevier
We propose an extension and further development of the Monod-Wyman-Changeux model
for allosteric transitions of regulatory proteins to brain communications and specifically to …

Nicotinic acetylcholine receptors: from basic science to therapeutics

R Hurst, H Rollema, D Bertrand - Pharmacology & therapeutics, 2013 - Elsevier
Substantial progress in the identification of genes encoding for a large number of proteins
responsible for various aspects of neurotransmitter release, postsynaptic detection and …

[PDF][PDF] Development of a Novel Class of Subtype-Selective Nicotinic Receptor Antagonist: Pyridine-N–Substituted Nicotine Analogs

PA CROOKS - 1999 - academia.edu
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Rose
Street, Lexington, Kentucky 40536-0082, USA n spite of the extensive diversity in neuronal …