Kinin B1receptors as novel anti-inflammatory targets

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Abstract
The kinin peptides exert their pro-inflammatory effects by the selective activation of two distinct G-protein coupled receptors, termed B1 and B2. The principle kinin peptides involved in the acute inflammatory response are bradykinin (BK) and Lys-BK, which produce their effects via the selective activation of constitutively expressed B2 receptors. The B1 receptor in contrast is not normally expressed, but is induced selectively by certain inflammatory stimuli. Additionally, the B1 receptor is selectively activated by the des-Arg9kinin metabolites, namely des-Arg9BK and Lys-des-Arg9BK, the synthesis of which are also increased during inflammation. Recent investigations into the molecular mechanisms of B1 receptor induction and their distribution and function have shown that, following an inflammatory stimulus, the B1 receptor is induced and may play an important role in the progression of an acute inflammatory response to a more sustained chronic inflammatory state characterised by leukocyte recruitment. ...