TABLE 2

Agonist potency for mobilization of intracellular calcium at rodent and primate bradykinin B1 receptors

Potencies for stimulation of calcium mobilization measured using the FLIPR using DAKD as agonist in lung fibroblasts cell lines expressing native B1 receptors from human (IMR-90) and rhesus monkey (DBS-FRhL-2) or using DABK as agonist in HEK293 cells expressing recombinant rat and mouse B1 receptors. Data are means ± S.E.M. of at least four to five experiments.


Species

Agonista

EC50

Hill Slope
nM
Human DAKD 0.88 ± 0.14 1.1 ± 0.1
Rhesus DAKD 0.83 ± 0.10 0.85 ± 0.07
Rat DABK 3.0 ± 0.4 1.0 ± 0.1
Mouse
DABK
1.7 ± 0.3
1.1 ± 0.1
  • a Receptors were activated using the probable physiologic agonist. For reference, the EC50 values for activation of human and rhesus B1 receptors by DABK were 118 and 34 nM, respectively, and for rat and mouse B1 receptors by DAKD were 2.6 and 2.2 nM, respectively (n = 1-4).