Cloning and pharmacological characterization of a human bradykinin (BK-2) receptor

Biochem Biophys Res Commun. 1992 Apr 15;184(1):260-8. doi: 10.1016/0006-291x(92)91187-u.


A human BK-2 bradykinin receptor was cloned from the lung fibroblast cell line CCD-16Lu. The cDNA clone encodes a 364 amino acid protein that has the characteristics of a seven transmembrane domain G-protein coupled receptor. The predicted amino acid sequence of the human BK-2 receptor is 81% identical to the smooth muscle rat BK-2 receptor (1). Transfection of the human BK-2 receptor cDNA into COS-7 cells results in the expression of high levels of specific BK binding sites. Saturation binding analysis indicates that the human BK-2 receptor expressed in COS-7 cells binds BK with a KD of 0.13 nM. Pharmacological characterization of the expressed BK receptor is consistent with the cDNA encoding a receptor of the BK-2 subtype. The BK-2 receptor antagonist Hoe 140 (2), D-Arg0[Hyp3, Thi5, D-Tic7, Oic8]BK has a high affinity (IC50 = 65 pM) for the cloned human receptor. The tissue distribution of the human BK-2 receptor was analyzed by competitive PCR with human tissue cDNA and is similar to that determined for the BK-2 receptor in the rat.

Publication types

  • Comparative Study

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Base Sequence
  • Binding, Competitive
  • Bradykinin / metabolism*
  • Cell Line
  • Cell Membrane / metabolism
  • Cloning, Molecular
  • Glycosylation
  • Humans
  • Kinetics
  • Lung
  • Molecular Sequence Data
  • Oligodeoxyribonucleotides
  • Polymerase Chain Reaction / methods
  • Protein Kinases / genetics
  • Protein Kinases / metabolism
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Rats
  • Receptors, Bradykinin
  • Receptors, Neurotransmitter / genetics*
  • Receptors, Neurotransmitter / metabolism
  • Sequence Homology, Nucleic Acid
  • Transfection


  • Oligodeoxyribonucleotides
  • RNA, Messenger
  • Receptors, Bradykinin
  • Receptors, Neurotransmitter
  • Protein Kinases
  • Bradykinin

Associated data

  • GENBANK/M88714
  • GENBANK/M97581
  • GENBANK/M97582
  • GENBANK/M97583
  • GENBANK/M97584
  • GENBANK/M97585
  • GENBANK/M97586
  • GENBANK/M97587
  • GENBANK/M97588
  • GENBANK/M97589