ATP-gated P2X ion-channel receptors are localised throughout the mammalian
nervous system and have been identified on neurones which participate in co
nduction of nociceptive information from the periphery to, and within, the
CNS. This article briefly reviews recently published research describing th
e role that ATP and P2X receptors may play in pain perception, highlighting
the importance of the P2X, receptor in this process. The P2X, receptor sub
unit is almost exclusively expressed on a subset of small and medium diamet
er sensory neurones innervating cutaneous and visceral tissue. Activation o
f P2X receptors present on the peripheral terminals of primary afferents re
sults in neuronal depolarisation and, in conscious animals, leads to the ma
nifestation of acute nociceptive behaviour. Recent animal studies have also
shown that P2X, receptor expression is increased in sensory ganglia follow
ing acute neuronal injury, hinting that similar plasticity in the expressio
n of this receptor subtype could underlie the mechanisms involved in a rang
e of conditions characterised by sensory hypersensitivity in man. It is app
arent from the evidence available that functional antagonists at specific P
2X receptor subtypes could represent an important class of novel analgesic
agents. (C) 2000 Elsevier Science B.V. All rights reserved.