Analgesic effects of the somatostatin sst4 receptor selective agonist J-2156 in acute and chronic pain models

Eur J Pharmacol. 2006 Jun 6;539(1-2):71-5. doi: 10.1016/j.ejphar.2006.03.082. Epub 2006 Apr 18.

Abstract

Somatostatin released from capsaicin-sensitive afferents exerts systemic anti-nociceptive actions, presumably via somatostatin receptor subtype 4 (sst4). In the present study, the antinociceptive effects of a novel somatostatin sst4 receptor selective peptidomimetic compound, J-2156 (1-100 microg/kg i.p.), were examined. J-2156 inhibited nocifensive behaviour of mice in the second phase of the formalin test. Adjuvant-evoked chronic inflammatory mechanical allodynia was decreased in rats treated with J-2156 for 21 days. Sciatic nerve ligation-induced neuropathic mechanical hyperalgesia was inhibited by J-2156 on the seventh postoperative day. Results obtained using this highly selective agonist suggest that somatostatin sst4 receptors represent a promising target for new perspectives in analgesic therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acute Disease
  • Analgesics / pharmacology*
  • Analgesics / therapeutic use
  • Animals
  • Butanes / pharmacology*
  • Butanes / therapeutic use
  • Chronic Disease
  • Hyperalgesia / drug therapy
  • Male
  • Membrane Proteins / agonists*
  • Mice
  • Mice, Inbred BALB C
  • Naphthalenes / pharmacology*
  • Naphthalenes / therapeutic use
  • Pain / drug therapy*
  • Pain Measurement
  • Pain Threshold
  • Physical Stimulation
  • Rats
  • Rats, Wistar
  • Receptors, Somatostatin / agonists*
  • Sulfones / pharmacology*
  • Sulfones / therapeutic use
  • Touch

Substances

  • Analgesics
  • Butanes
  • Membrane Proteins
  • Naphthalenes
  • Receptors, Somatostatin
  • Sulfones
  • somatostatin receptor subtype-4
  • (1'S, 2S)-4-amino-N-(1'-carbamoyl-2'-phenylethyl)-2-(4''-methyl-1''-naphthalenesulfonylamino)butanamide