Affordable Access

Antinociceptive activity of the S1P-receptor agonist FTY720

Publication Date
  • Ddc:610


FTY720 is a novel immunosuppressive drug that inhibits the egress of lymphocytes from secondary lymphoid tissues and thymus. In its phosphorylated form FTY720 is a potent S1P receptor agonist. Recently it was also shown that FTY720 can reduce prostaglandin synthesis through the direct inhibition of the cytosolic phospholipase A2 (cPLA2). Since prostaglandins are important mediators of nociception, we studied the effects of FTY720 in different models of nociception. We found that intraperitoneal administration of FTY720 reduced dose-dependently the nociceptive behaviour of rats in the formalin assay. Although the antinociceptive doses of FTY720 were too low to alter the lymphocyte count, prostanoid concentrations in the plasma were dramatically reduced. Surprisingly, intrathecally administered FTY720 reduced the nociceptive behaviour in the formalin assay without altering spinal prostaglandin synthesis, indicating that additional antinociceptive mechanisms beside the inhibition of prostaglandin synthesis are involved. Accordingly, FTY720 reduced also the nociceptive behaviour in the spared nerve injury model for neuropathic pain which does not depend on prostaglandin synthesis. In this model the antinociceptive effect of FTY720 was similar to gabapentin, a commonly used drug to treat neuropathic pain. Taken together we show for the first time that FTY720 possesses antinociceptive properties and that FTY720 reduces nociceptive behaviour during neuropathic pain.

There are no comments yet on this publication. Be the first to share your thoughts.


Seen <100 times

More articles like this

Antinociceptive activity of the S1P-receptor agoni...

on Journal of Cellular and Molecu... June 2008

S1P receptor mediated activity of FTY720 phosphate...

on Bioorganic & Medicinal Chemist... Jan 01, 2010

[Immunosuppressive effect of S1P1 receptor agonist...

on Yao xue xue bao = Acta pharmac... April 2012
More articles like this..