in rats: i.v.dose of 2.5 mg/kg or oral dose of 10 mg/kg in monkeys: i.v. at 1 mg/kg in10% polyethyleneglycol 660 hydroxystearate /HCl /saline or orally at 5 mg/kg in10% polyethyleneglycol 660 hydroxystearate /HCl /water or s.c. at 10 mg/kg in 20% Captisol/water

ELN-441958 (0.03 to 30nM) produced a concentration-dependent antagonism of the DAKD (des Arg10-kallidin)-induced calcium mobilization with a KB of 0.12 nM. ELN-441958 does not inhibit the activation of the human bradykinin B2 receptor at concentrations up to 10 μM, showing that it is highly selective for B1 over B2 receptors. It is >500-fold and >2000-fold selective for the B1 receptor over the human μ- and δ-opioid receptors