Plasma kinins are a family of peptides which play an important role in a variety of pathophysiological conditions. As a consequence of the progress in the area of kinin receptors, specific kinin receptor antagonists will be available in near future in order to provide more selective therapeutic modalities for the treatment of diseases such as asthma, cardiovascular diseases, inflammation, pain, etc. Although the initial observation leading to discovery of kinins has been performed in 1909, important progress on the development of specific kinin receptor antagonists has been made in last two decades. This review emphasizes the physiological functions of kinins along with their receptor subtypes and post-receptor events in the cellular signaling. In this article, the latest developments in the kinin receptor antagonists including nonpeptide ones have been reviewed.