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A cDNA encoding a functional bradykinin receptor was isolated from a rat uterus library by a clonal selection strategy using Xenopus laevis oocytes to assay for expression of bradykinin responses. The predicted protein is homologous to the seven transmembrane G protein-coupled superfamily of receptors. Bradykinin and its analogs stimulate a Cl- current oocytes expressing the receptor with the rank order of potency: bradykinin approximately Lys-bradykinin greater than [Tyr8]-bradykinin much greater than [Phe6]bradykinin. This is the rank order of potency observed for these compounds in competitive binding assays on soluble receptor from rat uterus. Des-Arg9-bradykinin (10 microM) elicits no response when applied to oocytes expressing the receptor; thus, the cDNA encodes a B2 type bradykinin receptor. [Thi5,8,DPhe7]bradykinin, where Thi is beta-(2-thienyl)-alanine, is a very weak partial agonist and inhibits the bradykinin-mediated ion flux, suggesting the cDNA encodes a smooth muscle, rather than a neuronal, B2 receptor subtype. Receptor message has a distribution consistent with previous reports of bradykinin function and/or binding in several tissues and is found in rat uterus, vas deferens, kidney, lung, heart, ileum, testis, and brain. Receptor subtypes are a possibility because several tissues contain two or three message species (4.0, 5.7, and 6.5 kilobases). Southern blot high-stringency analysis demonstrated that the rat, guinea pig, and human genomes contain a single gene. As bradykinin is a key mediator of pain, knowledge of the primary structure of this receptor will allow a molecular understanding of the receptor and aid the design of antagonists for pain relief.
A E McEachern, and
E R Shelton, and
S Bhakta, and
R Obernolte, and
C Bach, and
P Zuppan, and
J Fujisaki, and
R W Aldrich, and
K Jarnagin
September 1994,
Biochimica et biophysica acta,
A E McEachern, and
E R Shelton, and
S Bhakta, and
R Obernolte, and
C Bach, and
P Zuppan, and
J Fujisaki, and
R W Aldrich, and
K Jarnagin
June 2002,
The Biochemical journal,
A E McEachern, and
E R Shelton, and
S Bhakta, and
R Obernolte, and
C Bach, and
P Zuppan, and
J Fujisaki, and
R W Aldrich, and
K Jarnagin
April 1998,
European journal of pharmacology,
A E McEachern, and
E R Shelton, and
S Bhakta, and
R Obernolte, and
C Bach, and
P Zuppan, and
J Fujisaki, and
R W Aldrich, and
K Jarnagin
September 1992,
Biochemical and biophysical research communications,
A E McEachern, and
E R Shelton, and
S Bhakta, and
R Obernolte, and
C Bach, and
P Zuppan, and
J Fujisaki, and
R W Aldrich, and
K Jarnagin
December 2002,
Biology of reproduction,
A E McEachern, and
E R Shelton, and
S Bhakta, and
R Obernolte, and
C Bach, and
P Zuppan, and
J Fujisaki, and
R W Aldrich, and
K Jarnagin
November 1998,
Biochimica et biophysica acta,
A E McEachern, and
E R Shelton, and
S Bhakta, and
R Obernolte, and
C Bach, and
P Zuppan, and
J Fujisaki, and
R W Aldrich, and
K Jarnagin
November 2000,
The Journal of comparative neurology,
A E McEachern, and
E R Shelton, and
S Bhakta, and
R Obernolte, and
C Bach, and
P Zuppan, and
J Fujisaki, and
R W Aldrich, and
K Jarnagin
November 1994,
Gene,
A E McEachern, and
E R Shelton, and
S Bhakta, and
R Obernolte, and
C Bach, and
P Zuppan, and
J Fujisaki, and
R W Aldrich, and
K Jarnagin
December 1995,
The Journal of pharmacology and experimental therapeutics,
A E McEachern, and
E R Shelton, and
S Bhakta, and
R Obernolte, and
C Bach, and
P Zuppan, and
J Fujisaki, and
R W Aldrich, and
K Jarnagin
August 1997,
British journal of pharmacology,
