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Kinin B1 receptors: a review
1Centre de Recherche, l'Hôtel-Dieu de Québec, Canada.
Immunopharmacology
|June 1, 1995
Summary
The kinin B1 receptor, activated by bradykinin metabolites, plays a role in immunopathology. Research is advancing understanding of its function, regulation, and therapeutic potential.
Area of Science:
- Pharmacology
- Immunology
- Molecular Biology
Background:
- The kinin B1 receptor mediates bradykinin (BK)-related peptide effects, particularly contractile responses in the rabbit aorta.
- It is selectively activated by kinin metabolites lacking the C-terminal arginine residue, such as des-Arg9-BK.
- The B1 receptor is upregulated in immunopathology by cytokines and influenced by growth factors.
Purpose of the Study:
- To review progress in understanding the kinin B1 receptor.
- To cover the development of B1 receptor agonists and antagonists.
- To discuss binding assays, physiopathological roles, and receptor cloning.
Main Methods:
- Review of existing literature on kinin B1 receptor pharmacology.
- Analysis of studies on B1 receptor agonists and antagonists.
- Examination of data from binding assays and physiopathological investigations.
- Inclusion of information on receptor cDNA cloning and sequencing.
Main Results:
- The B1 receptor's sensitivity to specific kinin metabolites is confirmed.
- Its rapid upregulation in immunopathology by cytokines is a key finding.
- Growth factors also play a regulatory role in B1 receptor activity.
Conclusions:
- Significant progress has been made in understanding the kinin B1 receptor.
- Development of agonists and antagonists offers therapeutic avenues.
- Cloning and sequencing provide molecular insights into receptor function.