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Bradykinin receptor antagonists
R M Burch1, S G Farmer, L R Steranka
1Nova Pharmaceutical Corporation, Baltimore, Maryland 21224.
Medicinal Research Reviews
|April 1, 1990
Summary
Bradykinin, a peptide involved in various bodily functions, exerts its effects through specific receptors. New blocking agents are being tested for conditions like the common cold and burn pain.
Area of Science:
- Biochemistry
- Pharmacology
- Physiology
Background:
- Bradykinin and its metabolites, produced by kallikreins, induce diverse physiological responses.
- These responses include hypotension, bronchoconstriction, smooth muscle contraction, and pain.
- Bradykinin's actions are primarily mediated by B2 receptors.
Purpose of the Study:
- To explore the role of kinins in human diseases.
- To utilize novel bradykinin receptor antagonists as research tools.
- To investigate potential therapeutic applications of bradykinin receptor blockade.
Main Methods:
- Development of DPhe7-substituted peptides (Stewart and Vavrek) as specific bradykinin B2 receptor antagonists.
- Competitive blockade of bradykinin B2 receptors.
- Clinical trials to assess therapeutic efficacy.
Main Results:
- Stewart and Vavrek peptides effectively block bradykinin B2 receptors.
- Bradykinin receptor antagonists show promise in managing symptoms of the common cold.
- Antagonists are being evaluated for relief of pain in severe burns.
Conclusions:
- Bradykinin receptor antagonists are valuable tools for studying kinin-mediated effects.
- Clinical trials indicate potential therapeutic benefits for bradykinin antagonists in specific diseases.
- Further trials are planned for conditions like asthma.