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Molecular characterisation of cloned bradykinin B1receptors from rat and human

Authors
Journal
European Journal of Pharmacology
0014-2999
Publisher
Elsevier
Publication Date
Volume
374
Issue
3
Identifiers
DOI: 10.1016/s0014-2999(99)00315-5
Keywords
  • Bradykinin B1Receptor
  • Bradykinin
  • T-Kinin
  • G-Protein Coupled Receptor
  • Gene
  • (Rat)
Disciplines
  • Biology
  • Pharmacology

Abstract

Abstract This report describes the characterisation of cloned rat and human bradykinin B 1 receptors in African green monkey kidney fibroblast (Cos-7) cells. A ligand binding assay with [ 3 H ]des-Arg 10-kallidin was used to compare their pharmacology with respect to known bradykinin B 1 and B 2 receptor ligands. In addition, the pharmacology of T-kinin and its' derivative des-Arg 11-T-kinin was investigated. The cloned rat receptor had a similar pharmacology to that of the recently described mouse receptor and differs from that described for the human receptor. The rat receptor had a higher affinity for des-Arg 11-T-kinin than the human receptor. These differences in pharmacological properties may relate to the presence of T-kinin, bradykinin and their des-Arg derivatives as the major physiological peptides in rat and the predominance of kallidin and its derivatives in human. We confirm that the rat bradykinin B 1 receptor gene is organised in a two exon structure and differs from the human gene which has a three exon structure and we further examine the inducible expression of this gene in a wide range of tissues using Northern blotting.

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