Fingerprinting heterocellular β-adrenoceptor functional expression in the brain using agonist activity profiles.
GPCR
adrenergic
agonist
biased agonism
desensitization
expression
noradrenergic
receptor
Journal
Frontiers in molecular biosciences
ISSN: 2296-889X
Titre abrégé: Front Mol Biosci
Pays: Switzerland
ID NLM: 101653173
Informations de publication
Date de publication:
2023
2023
Historique:
received:
28
04
2023
accepted:
05
07
2023
medline:
4
9
2023
pubmed:
4
9
2023
entrez:
4
9
2023
Statut:
epublish
Résumé
Noradrenergic projections from the brainstem locus coeruleus drive arousal, attentiveness, mood, and memory, but specific adrenoceptor (AR) function across the varied brain cell types has not been extensively characterized, especially with agonists. This study reports a pharmacological analysis of brain AR function, offering insights for innovative therapeutic interventions that might serve to compensate for locus coeruleus decline, known to develop in the earliest phases of neurodegenerative diseases. First, β-AR agonist activities were measured in recombinant cell systems and compared with those of isoprenaline to generate Δlog(E
Identifiants
pubmed: 37664183
doi: 10.3389/fmolb.2023.1214102
pii: 1214102
pmc: PMC10471193
doi:
Types de publication
Journal Article
Langues
eng
Pagination
1214102Informations de copyright
Copyright © 2023 Matt, Westhorpe, Romuar, Rana, Gever and Ford.
Déclaration de conflit d'intérêts
All authors were employed by CuraSen Therapeutics, Inc., at the time of writing. This study received funding from CuraSen Therapeutics, Inc., a clinical-stage biotechnology company focused on activating noradrenaline targets in the central nervous system. The funder had the following involvement with the study: study design; collection, analysis, and interpretation of data; the writing of this article; and the decision to submit it for publication.
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