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Bradykinin receptor antagonists: therapeutic implications.
Jagdish N Sharma1, Ghadeer S Al-Dhalmawi
1Kuwait University, Department of Applied Therapeutics, Faculty of Pharmacy, Health Science Center, PO Box 24923, Safat 13110, Kuwait. j.n.sharma@hsc.kuniv.edu.kw
Idrugs : the Investigational Drugs Journal
|June 18, 2003
Summary
Bradykinin (BK) is a key mediator in pain and inflammation. Novel BK receptor antagonists show promise for treating diseases linked to the kinin system.
Area of Science:
- Pharmacology
- Biochemistry
Background:
- Bradykinin (BK) is a pro-inflammatory polypeptide involved in hyperalgesia, inflammation, asthma, and cancer.
- It exerts its effects by stimulating B(1) and B(2) receptors, which are implicated in various physiological and pathological processes.
- B(1) receptors are induced during injury and inflammation, while B(2) receptors are widespread in vascular and non-vascular smooth muscle and the heart.
Purpose of the Study:
- To review the development and therapeutic potential of bradykinin (BK) antagonists.
- To highlight the characteristics of effective BK receptor antagonists for clinical application.
Main Methods:
- Review of recent research on BK antagonists.
- Analysis of the properties required for clinically useful BK antagonists, including stability, oral activity, and half-life.
Main Results:
- Numerous peptide and non-peptide BK antagonists have been developed.
- Non-peptide B(2) receptor antagonists are currently under intense investigation.
- Ideal antagonists should be stable against BK-inactivating enzymes, orally active, and possess a long half-life with minimal side effects.
Conclusions:
- BK receptor antagonists represent a promising therapeutic strategy for conditions associated with the kinin system.
- Further research into these antagonists may lead to novel treatments for various pathological conditions.