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British Medical Bulletin 43:270-284 (1987)
© 1987 The British Council

research-article

Kinins

D Regoli

Department of Pharmacology, University of Sherbrooke Canada

Abstract

Kinins are a group of peptides released in blood by kallikreins to exert a variety of biological actions by activating at least two different receptor types. B1 and B2 receptors for kinins have been identified with agonists and antagonists, in classical pharmacological assays. The existence of the two receptor types has been confirmed with binding assays, using labelled bradykinin and des Arg9 bradykinin.

Antagonists for kinins active on B1 receptors have been identified and further developed to fairly potent, specific and competitive blockers. B2 receptors antagonists have recently been found and they are specific, but rather weak and nonselective, since they also block B1 receptors.

B2 receptors mediate a large number of rapidly occurring biological effects, particularly the symptoms and signs of inflammation, while B1 receptors appear to be involved in some retarded, long lasting effects of kinins, such as collagen synthesis and cell multiplication.

Kinins are among the naturally occurring agents involved in inflammatory reactions. All the processes of kinin generation appear to be accentuated: the expression of prekininogen mRNA; the production of kinin precursors (kinonogens) by the liver; the activation of the generating enzymes, the kallikreins; and the local production of kinins in inflammatory exudates. The kinins generated locally contribute to the acute and possibly the chronic phase of the inflammatory reaction by producing vasodilation, local oedema and pain. Kinins may also modulate migration of white blood and tissue cells that take part to the inflammatory process.


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