Sándor Katalin, Elekes Krisztián, Szabó Arpád, Pintér Erika, Engström Mia, Wurster Siegfried, Szolcsányi János, Helyes Zsuzsanna
Department of Pharmacology and Pharmacotherapy, Faculty of Medicine, University of Pécs, Pécs-7624 Szigeti str. 12, Hungary.
Eur J Pharmacol. 2006 Jun 6;539(1-2):71-5. doi: 10.1016/j.ejphar.2006.03.082. Epub 2006 Apr 18.
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.
从辣椒素敏感传入神经释放的生长抑素发挥全身抗伤害感受作用，推测是通过生长抑素受体亚型4（sst4）实现的。在本研究中，检测了一种新型生长抑素sst4受体选择性拟肽化合物J-2156（腹腔注射1-100微克/千克）的抗伤害感受作用。J-2156抑制了福尔马林试验第二阶段小鼠的伤害防御行为。用J-2156治疗21天的大鼠，佐剂诱发的慢性炎性机械性异常性疼痛减轻。坐骨神经结扎诱导的神经性机械性痛觉过敏在术后第7天被J-2156抑制。使用这种高选择性激动剂获得的结果表明，生长抑素sst4受体是镇痛治疗新视角的一个有前景的靶点。
