The Transient Receptor Potential (TRP) channel superfamily is comprised of a large group of cation-permeable channels, which display an extraordinary diversity of roles in sensory signaling and are involved in a plethora of animal behaviors. These channels are activated through a wide variety of mechanisms and participate in virtually every sensory modality. Although the physiological functions of most TRP channels are not well known, their wide distribution indicates that the biological roles and activation mechanisms for these channels are diverse. TRP channels are best recognized for their contributions to sensory transduction, response to temperature, nociceptive stimuli, touch, osmolarity, chemical substances such as pheromones or odorants, pungent natural compounds, and other stimuli from both within and outside the cell. This data clearly indicates that the specific and selective inhibition of TRP channels can be used to relieve pain and thus these channels represent promising targets for the development of further generations of novel analgesic drugs.