1.
Bioorg Med Chem Lett
; 21(7): 2011-6, 2011 Apr 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21354795
RESUMO
A high-throughput screening campaign has identified 1,4-diazepane compounds which are potent Cannabinoid receptor 2 agonists with excellent selectivity against the Cannabinoid receptor 1. This class of compounds suffered from low metabolic stability. Following various strategies, compounds with a good stability in liver microsomes and rat PK profile have been identified.
Assuntos
Azepinas/farmacologia , Receptor CB2 de Canabinoide/agonistas , Animais , Azepinas/química , Microssomos Hepáticos/metabolismo , Ratos , Ratos Wistar
2.
Bioorg Med Chem Lett
; 18(5): 1725-9, 2008 Mar 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-18255291
RESUMO
A high-throughput screening campaign resulted in the discovery of a highly potent dual cannabinoid receptor 1 (CB1) and 2 (CB2) agonist. Following a thorough SAR exploration, a series of selective CB2 full agonists were identified.