Tetrahydroindazole derivatives as potent and peripherally selective cannabinoid-1 (CB1) receptor inverse agonists.
Bioorg Med Chem Lett
; 26(21): 5346-5349, 2016 11 01.
Article
en En
| MEDLINE
| ID: mdl-27671496
ABSTRACT
A series of potent and receptor-selective cannabinoid-1 (CB1) receptor inverse agonists has been discovered. Peripheral selectivity of the compounds was assessed by a mouse tissue distribution study, in which the concentrations of a test compound in both plasma and brain were measured. A number of peripherally selective compounds have been identified through this process. Compound 2p was further evaluated in a 3-week efficacy study in the diet-induced obesity (DIO) mouse model. Beneficial effects on plasma glucose were observed from the compound-treated mice.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Receptor Cannabinoide CB1
/
Agonismo Inverso de Drogas
/
Indazoles
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2016
Tipo del documento:
Article