Kinins are peptide hormones that transmit their biological effects via G protein-coupled receptors. They are generated by kallikrein-mediated proteolysis of their precursors, the kininogens. Kinins have been implicated in the regulation of blood pressure, pain sensation and cell growth. Interestingly, all components of the kallikrein-kinin system have also been localized in testis. Effects of kallikrein and bradykinin on pre-spermatogonial cell proliferation and on sperm motility suggest a regulatory function of kinins and their cognate receptors in the male reproductive system. This review is dedicated to summarize the current knowledge about structure, signal transduction and regulation of kinin receptors. Particular emphasis will be given to the kinin-induced activation of the mitogen-activated protein kinase cascade which might represent an important signalling pathway involved in regulation of spermatogenesis and sperm function.