The cannabinoid ligands SR141716A and AM251 enhance human and mouse islet function via GPR55-independent signalling.
Animals
Cannabinoids
/ metabolism
Cell Proliferation
/ drug effects
Endocannabinoids
/ metabolism
Female
Humans
Insulin
Insulin Secretion
/ drug effects
Insulin-Secreting Cells
/ drug effects
Islets of Langerhans
/ drug effects
Ligands
Male
Mice
Mice, Inbred C57BL
Mice, Knockout
Middle Aged
Piperidines
/ pharmacology
Pyrazoles
/ pharmacology
Receptors, Cannabinoid
/ metabolism
Receptors, G-Protein-Coupled
/ metabolism
Rimonabant
/ pharmacology
Signal Transduction
/ drug effects
Apoptosis
Cannabinoids
Insulin secretion
Islets
Proliferation
β-Cell function
Journal
Cellular and molecular life sciences : CMLS
ISSN: 1420-9071
Titre abrégé: Cell Mol Life Sci
Pays: Switzerland
ID NLM: 9705402
Informations de publication
Date de publication:
Nov 2020
Nov 2020
Historique:
received:
15
08
2019
accepted:
18
12
2019
revised:
02
12
2019
pubmed:
12
1
2020
medline:
11
11
2020
entrez:
12
1
2020
Statut:
ppublish
Résumé
Endocannabinoids are lipid mediators involved in the regulation of glucose homeostasis. They interact with the canonical cannabinoid receptors CB Islets isolated from Gpr55 Our results provide the first evidence that SR141716A and AM251 are not GPR55 agonists in islets, as their effects are maintained in islets isolated from Gpr55 These observations may be useful in directing development of peripherally restricted novel therapeutics that are structurally related to SR141716A and AM251, and which potentiate glucose-induced insulin secretion and stimulate β-cell proliferation.
Identifiants
pubmed: 31925452
doi: 10.1007/s00018-019-03433-6
pii: 10.1007/s00018-019-03433-6
pmc: PMC7599183
doi:
Substances chimiques
Cannabinoids
0
Endocannabinoids
0
GPR55 protein, human
0
GPR55 protein, mouse
0
Insulin
0
Ligands
0
Piperidines
0
Pyrazoles
0
Receptors, Cannabinoid
0
Receptors, G-Protein-Coupled
0
AM 251
3I4FA44MAI
Rimonabant
RML78EN3XE
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
4709-4723Subventions
Organisme : Diabetes UK
ID : 11/0004397
Pays : United Kingdom
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