Antagonists of B2 bradykinin receptors

Bradykinin and its active metabolites, produced by kallikreins at their sites of action, potently elicit a variety of biological effects: hypotension, bronchoconstriction, gut and uterine contraction, epithelial secretion in airway, gut, and exocrine glands, vascular permeability, pain, connective t...

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Bibliographic Details
Published inThe FASEB journal Vol. 3; no. 9; p. 2019
Main Authors Steranka, L R, Farmer, S G, Burch, R M
Format Journal Article
LanguageEnglish
Published United States 01.07.1989
Subjects
Airway Resistance
Animals
Bradykinin - antagonists & inhibitors
Hemodynamics
Humans
Inflammation - physiopathology
Receptors, Bradykinin
Receptors, Neurotransmitter - classification
Receptors, Neurotransmitter - drug effects
Shock, Septic - physiopathology
Structure-Activity Relationship
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Summary:Bradykinin and its active metabolites, produced by kallikreins at their sites of action, potently elicit a variety of biological effects: hypotension, bronchoconstriction, gut and uterine contraction, epithelial secretion in airway, gut, and exocrine glands, vascular permeability, pain, connective tissue proliferation, cytokine release, and eicosanoid formation. These effects are mediated by at least two broad classes of receptors. The most common is the B2 subtype. The availability of competitive antagonists of B2 receptors has provided powerful tools for the study of bradykinin's actions. The significance of kinins in certain human diseases is being explored by using these agents as potential therapeutic agents. Human clinical trials are under way to test the usefulness of bradykinin receptor antagonists to treat symptoms of the common cold and the pain associated with severe burns. Trials are also being comtemplated for use in treatment of asthma.
ISSN:0892-6638
DOI:10.1096/fasebj.3.9.2545496