Several opiate receptor systems have been identified in the spinal cord. They produce a powerful analgesia when opioid agonists are administered intrathecally in the intact, unanesthetized animal. These effects appear mediated by an action on opioid receptors which are located presynaptically, in the terminals of primary afferents, and postsynaptically on certain dorsal horn neurons. Based on structure-activity relationships in different tests, quantitative studies of naloxone antagonism and selective cross tolerance, it appears that, in the spinal cord, there are three distinguishable populations of opioid receptors: mu, delta and kappa. Aside from the effects on nociception, these receptors are also associated with a variety of spinal mechanisms related to other aspects of sensory, autonomic and motor functions. Though in some cases these represent important side-effects (e.g. inhibition of the micturition reflex), in others, the subtle effects may have important therapeutic benefits (e.g. relieving spasticity in spinal injured patients).