Functional studies of bradykinin receptors in Chinese hamster ovary cells stably expressing the human B2 bradykinin receptor

Int Immunopharmacol. 2001 May;1(5):955-65. doi: 10.1016/s1567-5769(01)00032-7.


Bradykinin B1 and B2 receptors, members of the G-protein coupled receptor superfamily, are involved in inflammation and pain. Chinese hamster ovary (CHO) cells stably expressing the human B2 bradykinin receptor (CHO-B2) were used to characterize the signal transduction pathways associated with this receptor and its regulation. The selective B2 antagonist [3H]NPC17731 but not the selective B1 antagonist [3,4-prolyl-3,4-(3)H(N)]-[des-Arg10,Leu9]kallidin ([3H]DALKD) bound to CHO-B2 cell membranes with a Kd of 0.77 nM and a Bmax of 1087 fmol/mg protein. [3H]NPC17731 binding was inhibited by bradykinin ligands in the order: NPC17731 > bradykinin > kallidin >> DALKD > [des-Arg10] kallidin (DAKD), consistent with the pharmacological profile of B2 bradykinin receptors. The B2 agonist bradykinin and the B1/B2 agonist kallidin, but not the B1 agonist DAKD, increased [35S]GTP gamma S binding to the CHO-B2 cell membranes. The B2 bradykinin receptors were co-immunoprecipitated with G alpha q/11. In response to bradykinin stimulation, coupling of the B2 receptors to G alpha q/11 was increased by 10-fold. Bradykinin and kallidin, but not DAKD, induced intracellular calcium release in CHO-B2 cells, which was blocked by NPC17731 but not by DALKD. These results demonstrate that B2 bradykinin receptors directly coupled to G alpha q/11 to regulate intracellular calcium release. CHO-B2 cell is a useful system that can be applied to study the effect of potential agents that may influence the B2 receptor function.

MeSH terms

  • Animals
  • Bradykinin Receptor Antagonists
  • CHO Cells
  • Calcium Signaling / drug effects
  • Cell Membrane / physiology
  • Cricetinae
  • Gene Expression
  • Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
  • Humans
  • Kallidin / analogs & derivatives*
  • Kallidin / metabolism
  • Kallidin / pharmacology
  • Kinetics
  • Ligands
  • Oligopeptides / metabolism
  • Oligopeptides / pharmacology
  • Receptor, Bradykinin B2
  • Receptors, Bradykinin / agonists
  • Receptors, Bradykinin / genetics*
  • Receptors, Bradykinin / physiology*
  • Signal Transduction / drug effects


  • Bradykinin Receptor Antagonists
  • Ligands
  • Oligopeptides
  • Receptor, Bradykinin B2
  • Receptors, Bradykinin
  • bradykinin, Lys-Leu(8)-desArg(9)-
  • NPC 17731
  • Kallidin
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • kallidin, des-Arg(10)-