This overview paper describes in its introductory part bitter-tasting herbal drugs in the context of their traditional use in the loss of appetite and digestive disorders. Then, it mentions current knowledge on signals origin in bitter taste receptors leading to different, unexpected physiological processes. Newly observed biological effects of bitter tastants are correlated with modern trends of their complex study with an aim to develop new drugs primarily acting on bitter taste receptors.Key words: T2R bitter taste receptors GPCR bitters glucose homeostasis asthma ghrelin GLP-1 solitary chemosensory cells.