Agonists, Antagonists, and Modulators of P2X7 Receptors.
Agonists
Allosteric modulators
Antagonists
Binding site
Depression
Inflammation
Ligands
P2X receptors
Purine receptors
Purinergic signaling
Structure
Tool compounds
Journal
Methods in molecular biology (Clifton, N.J.)
ISSN: 1940-6029
Titre abrégé: Methods Mol Biol
Pays: United States
ID NLM: 9214969
Informations de publication
Date de publication:
2022
2022
Historique:
entrez:
1
7
2022
pubmed:
2
7
2022
medline:
8
7
2022
Statut:
ppublish
Résumé
The P2X7 receptor has been proposed as a novel drug target for different types of diseases associated with inflammation, including brain diseases, peripheral inflammation, and cancers. Structurally diverse P2X7 receptor antagonists, mainly negative allosteric modulators (NAMs), have been developed in recent years, and several P2X7 receptor antagonists are currently evaluated in clinical trials. The P2X7 receptor requires high micro- to even millimolar ATP concentrations to be activated. Selective agonists for the P2X7 receptor are not available. Positive allosteric modulators (PAMs) have been described, but PAMs with high potency and selectivity are still lacking. This chapter discusses medicinal chemistry approaches toward the development of P2X7 receptor modulators and presents a selection of recommended tool compounds for studying P2X7 receptors in humans and rodents.
Identifiants
pubmed: 35776318
doi: 10.1007/978-1-0716-2384-8_2
doi:
Substances chimiques
Purinergic P2X Receptor Antagonists
0
Receptors, Purinergic P2X7
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
31-52Informations de copyright
© 2022. The Author(s), under exclusive license to Springer Science+Business Media, LLC, part of Springer Nature.
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