[Involvement of peripheral 5-HT2A receptor activation in inflammatory pain]

Serotoninergic neuron is concerned as an one of the pivotal factor of the tissue inflammation which lead to pain behavior. Sarpogrelate HCl is a novel compound which may modulate inflammatory reaction through 5-HT2A receptor antagonist. We show the involvement of the 5-HT2A receptor activity in the inflammatory and neuropathic pain. Systemic or local sarpogrelate administration provokes antinociceptive effect on 5-HT- or formalin-produced inflammatory pain behaviour in relation to spinal glutamate. Local sarpogrelate inhibits apoptosis and neuronal degeneration after chronic construction injury(CCI). These effects are reversed by 5-HT2A receptor agonist. These results suggests sarpogrelate has a beneficial effect on hyperalgesia and neuropathic pain via inhibiting 5-HT2A receptor.