Therapeutic targeting of α7 nicotinic acetylcholine receptors

RL Papke, NA Horenstein, H Khoshbouei - Pharmacological Reviews, 2021 - Elsevier
The α7-type nicotinic acetylcholine receptor is one of the most unique and interesting of all
the members of the cys-loop superfamily of ligand-gated ion channels. Since it was first …

[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 …

Comparison of the Anti-inflammatory Properties of Two Nicotinic Acetylcholine Receptor Ligands, Phosphocholine and pCF3-diEPP

K Richter, RL Papke, C Stokes, DC Roy… - Frontiers in cellular …, 2022 - frontiersin.org
Activation of nicotinic acetylcholine receptors (nAChRs) expressed by innate immune cells
can attenuate pro-inflammatory responses. Silent nAChR agonists, which down-modulate …

[HTML][HTML] Small molecule ligands for α9* and α7 nicotinic receptors: A survey and an update, respectively

A Giraudo, M Pallavicini, C Bolchi - Pharmacological Research, 2023 - Elsevier
Abstract The α9-and α7-containing nicotinic acetylcholine receptors (nAChRs) mediate
numerous physiological and pathological processes by complex mechanisms that are …

The mechanisms mediated by α7 acetylcholine nicotinic receptors may contribute to peripheral nerve regeneration

MS Salazar Intriago, R Piovesana, A Matera, M Taggi… - Molecules, 2021 - mdpi.com
Due to the microenvironment created by Schwann cell (SC) activity, peripheral nerve fibers
are able to regenerate. Inflammation is the first response to nerve damage and the removal …

Synthesis, biological evaluation and structure-activity relationships of self-assembled and solubilization properties of amphiphilic quaternary ammonium derivatives of …

EA Burilova, TN Pashirova, SS Lukashenko… - Journal of molecular …, 2018 - Elsevier
This work deals with development of polyfunctional biocompatible cationic surfactant
systems based on bioactive saturated bicyclic alkaloid quinuclidine. It is focused on the …

New Alpha9 nAChR Ligands Based on a 5-(Quinuclidin-3-ylmethyl)-1, 2, 4-oxadiazole Scaffold

C Dallanoce, K Richter, C Stokes… - ACS Chemical …, 2024 - ACS Publications
Several lines of evidence have indicated that nicotinic acetylcholine receptors (nAChR) that
contain α9 subunits, probably in combination with α10 subunits, may be valuable targets for …

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 …

ICH3, a selective alpha7 nicotinic acetylcholine receptor agonist, modulates adipocyte inflammation associated with obesity

G Scabia, R Cancello, C Dallanoce, S Berger… - Journal of …, 2020 - Springer
Purpose The alpha7 nicotinic acetylcholine receptor (α7nAChR), involved in the modulation
of inflammation and insulin sensitivity, is downregulated in white adipose tissue (WAT) of …