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 plethora of animal behaviors. These channels are activated through a wide variety of mechanisms and participate in virtually every sensory modality. Modulating TRP channel activity provides an important way to regulate membrane excitability and intracellular calcium levels. This is reflected by the fact that small molecule compounds modulating different TRPs have all entered clinical trials for a variety of diseases. The role of TRPs will be further elucidated in complex diseases of the nervous, intestinal, renal, urogenital, respiratory, and cardiovascular systems in diverse therapeutic areas including pain and itch, headache, pulmonary function, oncology, neurology, visceral organs, and genetic diseases. This review focuses on recent developments in the TRP ion channel-related area and highlights evidence supporting TRP channels as promising targets for new analgesic drugs for therapeutic intervention. This review presents a variety of: (1) phylogeny aspects of TRP channels; (2) some structural and functional characteristics of TRPs; (3) a general view and short characteristics of main seven subfamilies of TRP channels; (4) the evidence for consider TRP channels as therapeutic and analgesic targets; and finally (5) further perspectives of TRP channels research.