1.
Bioorg Med Chem Lett
; 21(12): 3805-8, 2011 Jun 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21570840
RESUMO
Structure-activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X(7) receptor antagonists with improved pharmacokinetic profiles. These compounds were potent and selective at the P2X(7) receptor in both human and rodent. Compound (entry 31) exhibited oral efficacy in the rat MIA and CCI pain models.