Nicotinic acetylcholine receptors: Conventional and unconventional ligands and signaling

RL Papke, JM Lindstrom - Neuropharmacology, 2020 - Elsevier
Postsynaptic nAChRs in the peripheral nervous system are critical for neuromuscular and
autonomic neurotransmission. Pre-and peri-synaptic nAChRs in the brain modulate …

[HTML][HTML] Silent agonists for α7 nicotinic acetylcholine receptors

RL Papke, M Quadri, A Gulsevin - Pharmacological Research, 2023 - Elsevier
We discuss models for the activation and desensitization of α7 nicotinic acetylcholine
receptors (nAChRs) and the effects of efficacious type II positive allosteric modulators …

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 …

Differential interactions of resting, activated, and desensitized states of the α7 nicotinic acetylcholine receptor with lipidic modulators

Y Zhuang, CM Noviello, RE Hibbs… - Proceedings of the …, 2022 - National Acad Sciences
The α7 nicotinic acetylcholine receptor is a pentameric ligand-gated ion channel that
modulates neuronal excitability, largely by allowing Ca2+ permeation. Agonist binding …

[HTML][HTML] Potentiation and allosteric agonist activation of α7 nicotinic acetylcholine receptors: binding sites and hypotheses

VR Sanders, NS Millar - Pharmacological Research, 2023 - Elsevier
Considerable progress has been made in recent years towards the identification and
characterisation of novel subtype-selective modulators of nicotinic acetylcholine receptors …

[HTML][HTML] Pharmacology and molecular modeling studies of sulfoxaflor, flupyradifurone and neonicotinoids on the human neuronal α7 nicotinic acetylcholine receptor

A Cartereau, Z Bouchouireb, S Kaaki… - Toxicology and Applied …, 2024 - Elsevier
We conducted electrophysiological and molecular docking studies using a heterologous
expression system (Xenopus oocytes) to compare the effects of four neonicotinoids …

Cholinergic receptors and addiction

RL Papke, DH Brunzell, M De Biasi - Behavioral Pharmacology of the …, 2020 - Springer
Human behavior can be controlled by physical or psychological dependencies associated
with addiction. One of the most insidious addictions in our society is the use of tobacco …

Design, synthesis, and electrophysiological evaluation of NS6740 derivatives: Exploration of the structure-activity relationship for alpha7 nicotinic acetylcholine …

MC Pismataro, NA Horenstein, C Stokes… - European journal of …, 2020 - Elsevier
The α7 nicotinic acetylcholine receptor (nAChR) silent agonists, able to induce receptor
desensitization and promote the α7 metabotropic function, are emerging as new promising …

Synthesis, Pharmacological Characterization, and Structure–Activity Relationships of Noncanonical Selective Agonists for α7 nAChRs

GA Camacho-Hernandez, C Stokes… - Journal of medicinal …, 2019 - ACS Publications
A lack of selectivity of classical agonists for the nicotinic acetylcholine receptors (nAChR)
has prompted us to identify and develop a distinct scaffold of α7 nAChR-selective ligands …

Lessons from nature: Structural studies and drug design driven by a homologous surrogate from invertebrates, AChBP

GA Camacho-Hernandez, P Taylor - Neuropharmacology, 2020 - Elsevier
It has been almost 20 years since the discovery and crystallization of a structural surrogate,
the Lymnaea stagnalis acetylcholine binding protein (Ls-AChBP), comprising the …