Antinociceptive profile of salvinorin A, a structurally unique kappa opioid receptor agonist
Antinociceptive profile of salvinorin A, a structurally unique kappa opioid receptor agonist
复制标题
DOI：
10.1016/j.pbb.2005.12.011
复制
发表时间：
2006-01-01
影响因子：
3.6
通讯作者：
Nieto, MJ
中科院分区：
文献类型：
--
作者：
McCurdy, CR;Sufka, KJ;Nieto, MJ
Salvinorin A 是一种结构独特的非氮 kappa 阿片受体 (KOP) 激动剂。鉴于 KOP 在镇痛过程中的作用，我们着手确定 Salvinorin A 在热和化学伤害感受测定中是否具有抗伤害活性。采用甩尾测定法研究 1) Salvinorin A（0.5、1.0、2.0 和 4.0 mg/kg）在热伤害性测定中的剂量反应和时程（10、20 和 30 分钟）效应，以及 2) KOP 拮抗剂 NorBNI (10.0 mg/kg) 预防 Salvinorin A 镇痛的能力。热板测定被用作第二种热伤害性测量来测试 Salvinorin A 的剂量反应效应。醋酸腹部收缩试验用于研究化学伤害试验中 Salvinorin A 的剂量反应和时程（超过 30 分钟）效应。总之，这些研究表明，salvinorin A 产生剂量依赖性的镇痛作用，在注射后 10 分钟达到峰值，但很快恢复到基线。此外，用 KOP 拮抗剂去甲托菲明 (norBNI) 进行预处理可逆转 Salvinorin A 诱导的镇痛作用。这些发现表明 Salvinorin A 产生 KOP 介导的镇痛作用，且作用持续时间短。 (C) 2005 Elsevier Inc. 保留所有权利。
Salvinorin A, is a structurally unique, non-nitrogenous, kappa opioid receptor (KOP) agonist. Given the role of KOPs in analgesic processes, we set out to determine whether salvinorin A has antinociceptive activity in thermal and chemo-nociceptive assays. The tail-flick assay was employed to investigate 1) salvinorin A's (0.5, 1.0, 2.0, and 4.0 mg/kg) dose-response and time-course (10, 20, and 30 min) effects in a thermal nociceptive assay, and 2) the ability for the KOP antagonist norBNI (10.0 mg/kg) to prevent salvinorin A antinociception. The hotplate assay was utilized as a second thermal nociceptive measure to test salvinorin A's dose-response effects. The acetic acid abdominal constriction assay was used to study salvinorin A's dose-response and time-course (over 30 min) effects in a chemo-nociceptive assay. Together, these studies revealed that salvinorin A produces a dose-dependent antinociception that peaked at 10 min post-injection but rapidly returned to baseline. Additionally, pretreatment with the KOP antagonist norbinaltorphimine (norBNI) reversed salvinorin A-induced antinociception. These findings demonstrate that salvinorin A produces a KOP mediated antinociceptive effect with a short duration of action. (C) 2005 Elsevier Inc. All rights reserved.