The cloning of the vanilloid receptor 1 opened a floodgate for discoveries regarding the function of this complex molecule. It has been found that, in addition to heat, protons and vanilloids, this receptor also responds to various endogenous ligands. Furthermore, it has been also emerged that, through associations with other molecules, the vanilloid receptor 1 plays an important role in the integration of various stimuli and modulation of cellular excitability. Although, originally, the vanilloid receptor 1 was associated with nociceptive primary afferent fibres, it has been gradually revealed that it is broadly expressed in the brain, epidermis and visceral cells. The expression pattern of the vanilloid receptor 1 indicates that it could be involved in various physiological functions and in the pathomechanisms of diverse diseases. Here, we summarise the molecular, pharmacological and physiological characteristics, and putative functions, of the vanilloid receptor 1, and discuss the therapeutic potential of this molecule.