Bradykinin receptors and their antagonists

European Journal of Pharmacology
Domenico RegoliF Gobeil

Abstract

Bradykinin and related kinins act on two receptor types, named B1 and B2. Initially identified in classical bioassays, these receptors have been cloned and characterized in binding assays performed on plasma membranes of cells expressing the native or the transfected human kinin B1 or B2 receptor types. The two classification criteria recommended by Schild, namely the order of potency of agonists and the actual affinity of antagonists have been found to be applicable for receptor classification based not on data only from bioassays but also from other approaches (binding assays, molecular biology techniques). The order of potency for agonists was found with naturally occurring peptides (the kinins, their desArg9-metabolites) and with selective agonists (e.g., [Hyp3]bradykinin, [Aib7]bradykinin): the findings obtained with agonists could be validated with various antagonists. Critical evaluation of the initial compounds, typified by D)-Arg-[Hyp3, D-Phe7]bradykinin, has indicated that they are short-acting, partial agonists, non-selective for the bradykinin B2 receptor because they can be metabolized to desArg9-fragments that act on the kinin B1 receptor. Use of such compounds has given rise to misunderstandings, especially with ...Continue Reading

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