Effects of a 5-HT2A receptor antagonist, sarpogrelate on thermal or inflammatory pain

The effects of intrathecally and systemically administered 5-hydroxytriptamine (5-HT)2A receptor antagonist, sarpogrelate on acute thermal or formalin induced pain were examined. Male Sprague-Dawley rats with lumbar intrathecal catheters were tested with their tail withdrawal response to thermal stimulation (tail flick test) or their paw flinching and shaking response by subcutaneous formalin injection into the hind paw (formalin test) after intrathecal or intraperitoneal administration of sarpogrelate. 5-HT2A receptor agonist was used to antagonize the effects of sarpogrelate. In the tail flick test, only intraperitoneal administration induced analgesia. In the formalin test, both intrathecal and intraperitoneal administration were analgesic. The analgesic effects were inhibited by pretreatment with 5-HT2A receptor agonist. Motor disturbance and behavioral side effects were not observed. In conclusion, sarpogrelate might be analgesic on inflammatory induced acute and facilitated pain by intrathecal or systemic administration. However, only systemic administration could be effective on thermal induced acute pain.