ELN441958 is a potent, selective Bradykinin B1 receptor (B1R) antagonist with Ki of 0.26 nM, highly selective for B1 over B2 receptors. ELN441958 is up to 120-fold more potent at primate than at rodent B1 receptors. ELN441958 potently antagonized DAKD (but not bradykinin)-induced calcium mobilization in IMR-90 cells. ELN441958 dose-dependently reduced carrageenan-induced thermal hyperalgesia in a rhesus monkey tail-withdrawal model, with an ED50 ∼3 mg/kg s.c. in primate pain model.
