Analgesic effects of the somatostatin sst4 receptor selective agonist J-2156 in acute and chronic pain models.
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.
Sándor
Katalin
K
Department of Pharmacology and Pharmacotherapy, Faculty of Medicine, University of Pécs, Pécs-7624 Szigeti str. 12, Hungary.
Elekes
Krisztián
K
Szabó
Arpád
A
Pintér
Erika
E
Engström
Mia
M
Wurster
Siegfried
S
Szolcsányi
János
J
Helyes
Zsuzsanna
Z
D000208:Acute Disease; D000700:Analgesics / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D002073:Butanes / Q000494:pharmacology* / Q000627:therapeutic use; D002908:Chronic Disease; D006930:Hyperalgesia / Q000188:drug therapy; D008297:Male; D008565:Membrane Proteins / Q000819:agonists*; D051379:Mice; D008807:Mice, Inbred BALB C; D009281:Naphthalenes / Q000494:pharmacology* / Q000627:therapeutic use; D010146:Pain / Q000188:drug therapy*; D010147:Pain Measurement; D017288:Pain Threshold; D010812:Physical Stimulation; D051381:Rats; D017208:Rats, Wistar; D017481:Receptors, Somatostatin / Q000819:agonists*; D013450:Sulfones / Q000494:pharmacology* / Q000627:therapeutic use; D014110:Touch
D000700:Analgesics; D002073:Butanes; D008565:Membrane Proteins; D009281:Naphthalenes; D017481:Receptors, Somatostatin; D013450:Sulfones; C098681:somatostatin receptor subtype-4; C499293:(1'S, 2S)-4-amino-N-(1'-carbamoyl-2'-phenylethyl)-2-(4''-methyl-1''-naphthalenesulfonylamino)butanamide