Molecular characterisation of cloned bradykinin B-1 receptors from rat andhuman

Citation
C. Jones et al., Molecular characterisation of cloned bradykinin B-1 receptors from rat andhuman, EUR J PHARM, 374(3), 1999, pp. 423-433
Citations number
30
Categorie Soggetti
Pharmacology & Toxicology
Journal title
EUROPEAN JOURNAL OF PHARMACOLOGY
ISSN journal
00142999 → ACNP
Volume
374
Issue
3
Year of publication
1999
Pages
423 - 433
Database
ISI
SICI code
0014-2999(19990625)374:3<423:MCOCBB>2.0.ZU;2-K
Abstract
This report describes the characterisation of cloned rat and human bradykin in B-1 receptors in African green monkey kidney fibroblast (Cos-7) cells. A ligand binding assay with [H-3]des-Arg(10)-kallidin was used to compare th eir pharmacology with respect to known bradykinin B-1 and B-2 receptor liga nds. In addition, the pharmacology of T-kinin and its' derivative des-Arg(1 1)-T-kinin was investigated. The cloned rat receptor had a similar pharmaco logy to that of the recently described mouse receptor and differs from that described for the human receptor. The rat receptor had a higher affinity f or des-Arg(11)-T-kinin than the human receptor. These differences in pharma cological properties may relate to the presence of T-kinin, bradykinin and their des-Arg derivatives as the major physiological peptides in rat and th e predominance of kallidin and its derivatives in human. We confirm that th e 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 furthe r examine the inducible expression of this gene in a wide range of tissues using Northern blotting. (C) 1999 Elsevier Science B.V. All rights reserved .