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Protease Activated Receptor-2 as an Imperative Target in Nociceptive Responses: A Minireview

Nilesh Mahajan, Vaidhyalingam V



PARs (protease-activated receptors) are a family of seven-transmembrane G-protein coupled receptor for proteases from circulation, inflammatory cells and endothelial tissues. To date, four members of PAR family have been cloned, namely PAR1 to PAR4. This minireview focuses on role of PAR2 receptor in inflammatory and nociceptive processes. Numerous studies documented for activation of PAR2 receptors through several proteases suggests its role in pain and inflammation. However, mechanism of PAR2 underlying its downregulation is poorly understood. Several screening tools for study of receptor mechanism with agonist and antagonist have been developed. Moreover, study with knockout and transgenic mice so far contributed in this regard suggests possibility of PAR2 selective antagonist as a useful drug for the treatment of pain and inflammatory disorders.

Keywords: antagonist, hyperalgesia, inflammation, nociceptive, receptors, targets

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