Otero D A, Conrad B, O'Brien J S
Department of Neuroscience, University of California, San Diego, La Jolla 92093-0634, USA.
Neurosci Lett. 1999 Jul 23;270(1):29-32. doi: 10.1016/s0304-3940(99)00461-9.
We used the partial sciatic nerve ligation (PSL) model of Seltzer to assess thermal hyperalgesia after administration of Prosaptide 14-mer, TX14(A). At a dose of 200 microg/kg in Wistar rats, subcutaneous delivery of TX14(A) reversed thermal hyperalgesia at 3 and 24 h. Values declined at 48 h and returned to baseline at 72 h. A dosing study of TX(14)A gave a dependent response with 100 microg/kg having a similar potency to the 200 microg/kg study with 50 and 10 microg/kg responding somewhat lower. When TX(14)A was administered every fourth day for 12 days at 100 microg/kg, 24 h post injection values returned to baseline each time. Our results suggest that Prosaptide may have potential for therapeutic use in neuropathic pain syndromes in humans.
我们使用塞尔策的部分坐骨神经结扎(PSL)模型来评估给予十四肽原(Prosaptide)14聚体TX14(A)后的热痛觉过敏。在Wistar大鼠中,以200微克/千克的剂量皮下注射TX14(A)后,在3小时和24小时时逆转了热痛觉过敏。在48小时时数值下降,在72小时时恢复到基线水平。一项关于TX(14)A的给药研究呈现出剂量依赖性反应,100微克/千克的效力与200微克/千克的研究相似,50微克/千克和10微克/千克的反应略低。当以100微克/千克的剂量每四天注射一次TX(14)A,持续12天时,每次注射后24小时的数值都会恢复到基线水平。我们的结果表明,十四肽原可能在人类神经性疼痛综合征的治疗中具有潜在用途。