PSNCBAM-1 analogs: Structural evolutions and allosteric properties at cannabinoid CB1 receptor.
Allosteric modulator
CB1 receptors
Diaryl urea
Endocannabinoid system
GTP
PSNCBAM-1
S
Journal
European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510
Informations de publication
Date de publication:
01 Oct 2020
01 Oct 2020
Historique:
received:
15
04
2020
revised:
17
06
2020
accepted:
18
06
2020
pubmed:
19
7
2020
medline:
23
4
2021
entrez:
19
7
2020
Statut:
ppublish
Résumé
Allosteric modulation of the CB1Rs could represent an alternative strategy for the treatment of diseases in which these receptors are involved, without the undesirable effects associated with their orthosteric stimulation. PSNCBAM-1 is a reference diaryl urea derivative that positively affects the binding affinity of orthosteric ligands (PAM) and negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs. In this work we reported the design, synthesis and biological evaluation of three different series of compounds, derived from structural modifications of PSNCBAM-1 and its analogs reported in the recent literature. Almost all the new compounds increased the percentage of binding affinity of CP55940 at CB1Rs, showing a PAM profile. When tested alone in the [
Identifiants
pubmed: 32682199
pii: S0223-5234(20)30578-X
doi: 10.1016/j.ejmech.2020.112606
pii:
doi:
Substances chimiques
1-(4-chlorophenyl)-3-(3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl)urea
0
Ligands
0
Phenylurea Compounds
0
Pyridines
0
Receptor, Cannabinoid, CB1
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
112606Informations de copyright
Copyright © 2020 Elsevier Masson SAS. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of competing interest The authors declare no competing financial interest.