Open access
Oct 2026
Discovery of a Peripherally Directed CB1 Receptor Antagonist That Restores Insulin Signaling in Adipocytes
Piperazine-1-ium derivative 24a stands out as the first permanently charged CB1R antagonist, exhibiting nanomolar affinity and high CB1R/CB2R selectivity with a favorable physicochemical profile consistent with peripheral restriction and limited blood-brain barrier penetration.
J. Azuaje, Rubén Prieto-Díaz, Claudia Gioé-Gallo et al.
· ACS Omega · 0 citations