Chronic Exposure to SCO-267, an Allosteric GPR40 Full Agonist, Is Effective in Improving Glycemic Control in Rats.
Animals
Blood Glucose
/ drug effects
CHO Cells
Cricetinae
Cricetulus
Diabetes Mellitus, Experimental
/ blood
Dose-Response Relationship, Drug
Glycemic Control
/ methods
Humans
Male
Piperidines
/ administration & dosage
Pyridines
/ administration & dosage
Rats
Rats, Inbred WKY
Receptors, G-Protein-Coupled
/ agonists
Journal
Molecular pharmacology
ISSN: 1521-0111
Titre abrégé: Mol Pharmacol
Pays: United States
ID NLM: 0035623
Informations de publication
Date de publication:
04 2021
04 2021
Historique:
received:
17
09
2020
accepted:
15
01
2021
pubmed:
7
2
2021
medline:
10
4
2021
entrez:
6
2
2021
Statut:
ppublish
Résumé
Full agonist-mediated activation of free fatty acid receptor 1 (FFAR1/GPR40) alleviates diabetes in rodents. Considering that diabetes is a chronic disease, assessment of treatment durability of chronic exposure to a GPR40 full agonist is pivotal for treating patients with diabetes. However, the physiologic significance of chronic in vitro and in vivo exposure to GPR40 full agonists is largely unclear. Here, we evaluated the in vitro and in vivo effects of chronic treatment with SCO-267, a GPR40 full agonist, on signal transduction and glucose control. In vitro experiments showed that SCO-267 is an allosteric full agonist for GPR40, which activates the G
Identifiants
pubmed: 33547250
pii: molpharm.120.000168
doi: 10.1124/molpharm.120.000168
doi:
Substances chimiques
Blood Glucose
0
G-protein-coupled receptor 40, rat
0
Piperidines
0
Pyridines
0
Receptors, G-Protein-Coupled
0
SCO-267
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
286-293Informations de copyright
Copyright © 2021 by The Author(s).