Cloning, sequencing and functional expression of a guinea pig lung bradykinin B 2 receptor

• Published in: European journal of pharmacology Vol. 346; no. 2; pp. 291 - 298
• Main Authors: Farmer, Stephen G, Powell, Steve J, Wilkins, Deidre E, Graham, Alexander
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 10-04-1998
• Subjects: Bradykinin; Bradykinin B 2 receptor; Bradykinin receptor; Cloning; Functional expression; Guinea pig; Bradykinin receptor; Guinea pig; Bradykinin B 2 receptor; Functional expression; Bradykinin; Cloning
• DOI: 10.1016/S0014-2999(98)00024-7
• EISSN: 1879-0712
• ISSN: 0014-2999

Kinin receptors are classified as B
1 and B
2 based upon agonist and antagonist potencies and cloning and expression studies. Using sequences from human and rat bradykinin B
2 receptors, polymerase chain reaction (PCR) was utilized to isolate cDNA from guinea pig lung. The receptor obtained is predicted to have 372 amino acids and shares >80% sequence homology with human, rat, rabbit and mouse B
2 receptors. In competition binding experiments in Chinese hamster ovary (CHO-K1) cells in which the guinea pig cDNA was expressed, [
3H]bradykinin was displaced by kinin receptor ligands with an order of potency consistent with a B
2 subtype. In CHO cells expressing the guinea pig receptor, bradykinin caused a concentration
45Ca
2+ efflux. A B
1 receptor agonist, desArg
9-bradykinin, also caused
45Ca
2+ efflux but with a potency several orders of magnitude lower than bradykinin. Curiously, several B
1 and B
2 receptor antagonists induced
45Ca
2+ efflux, indicating that this receptor may be coupled differently in CHO cells than in native tissues.