• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

大麻素受体激动剂 WIN55,212-2 在急性和炎症性疼痛动物模型中于楔状核的镇痛作用。

Analgesic effects of cannabinoid receptor agonist WIN55,212-2 in the nucleus cuneiformis in animal models of acute and inflammatory pain in rats.

机构信息

Neuroscience Research Center, Shahid Beheshti University of Medical Sciences, P.O. Box 19615-1178, Tehran, Iran.

出版信息

Brain Res. 2011 Oct 28;1420:19-28. doi: 10.1016/j.brainres.2011.08.028. Epub 2011 Aug 17.

DOI:10.1016/j.brainres.2011.08.028
PMID:21911208
Abstract

Nucleus cuneiformis (NCF) along with periaqueductal gray (PAG) and rostral ventromedial medulla (RVM) is a part of descending system for pain modulation. Cannabinoids have analgesic effects on the PAG and RVM. This study investigates the possible role of cannabinoids in pain modulation in the NCF. Cannabinoid agonist, WIN55,212-2 (5, 10 and 20μg/0.3μl DMSO per side), and selective cannabinoid CB1 receptor antagonist, AM251(1, 5 and 10μg/0.3μl DMSO per side), were microinjected alone or in succession. As models of acute and inflammatory pain, tail-flick and formalin test were utilized to examine the effects of these drugs on pain modulation in 5min time blocks for 60min. Results of tail-flick and formalin tests demonstrated a dose-dependent analgesic effects for WIN55,212-2, with the most significant response at the dose of 20μg/side. The analgesic responses were more effective during the first 45-min period of the tail-flick test (P<0.001) and during the late phase (P<0.001) of formalin test, compared to the early phase (P<0.05). These analgesic effects were blocked in the presence of AM251 (1μg/0.3μl DMSO per side) in both tests. Administration of AM251 alone did not have any effect on nociceptive responses in either test. The cannabinoid-mediated analgesia demonstrated in this study suggests the presence of a cannabinoid-sensitive nociceptive modulatory system in the NCF.

摘要

楔内核对疼痛调制的下行系统与导水管周围灰质(PAG)和延髓头端腹内侧区(RVM)一起构成。大麻素对 PAG 和 RVM 具有镇痛作用。本研究旨在探讨大麻素在 NCF 疼痛调制中的可能作用。大麻素激动剂 WIN55,212-2(5、10 和 20μg/0.3μl DMSO 每侧)和选择性大麻素 CB1 受体拮抗剂 AM251(1、5 和 10μg/0.3μl DMSO 每侧)单独或连续注射。作为急性和炎症性疼痛模型,利用尾部闪烁和福尔马林试验来检查这些药物对疼痛调制的影响,时间为 60 分钟,每隔 5 分钟记录一次。尾部闪烁和福尔马林试验的结果表明 WIN55,212-2 具有剂量依赖性的镇痛作用,在 20μg/侧的剂量下效果最显著。在尾部闪烁试验的前 45 分钟(P<0.001)和福尔马林试验的晚期(P<0.001),与早期(P<0.05)相比,镇痛反应更有效。在两种试验中,AM251(1μg/0.3μl DMSO 每侧)的存在阻断了这些镇痛作用。单独给予 AM251 在两种试验中均未对伤害性反应产生任何影响。本研究中观察到的大麻素介导的镇痛作用表明,楔内核对伤害性感觉调制系统存在大麻素敏感性。

相似文献

1
Analgesic effects of cannabinoid receptor agonist WIN55,212-2 in the nucleus cuneiformis in animal models of acute and inflammatory pain in rats.大麻素受体激动剂 WIN55,212-2 在急性和炎症性疼痛动物模型中于楔状核的镇痛作用。
Brain Res. 2011 Oct 28;1420:19-28. doi: 10.1016/j.brainres.2011.08.028. Epub 2011 Aug 17.
2
Periaqueductal grey CB1 cannabinoid and metabotropic glutamate subtype 5 receptors modulate changes in rostral ventromedial medulla neuronal activities induced by subcutaneous formalin in the rat.导水管周围灰质的CB1大麻素受体和代谢型谷氨酸5型受体调节皮下注射福尔马林诱导的大鼠延髓头端腹内侧神经元活动的变化。
Neuroscience. 2005;134(1):269-81. doi: 10.1016/j.neuroscience.2005.03.014.
3
CB cannabinoid receptor agonist mouse VD-hemopressin(α) produced supraspinal analgesic activity in the preclinical models of pain.CB大麻素受体激动剂小鼠VD-血管加压素(α)在临床前疼痛模型中产生了脊髓上镇痛活性。
Brain Res. 2018 Feb 1;1680:155-164. doi: 10.1016/j.brainres.2017.12.013. Epub 2017 Dec 21.
4
Blockade of D1/D2 dopamine receptors within the nucleus accumbens attenuated the antinociceptive effect of cannabinoid receptor agonist in the basolateral amygdala.伏隔核内 D1/D2 多巴胺受体阻断减弱了外侧杏仁核大麻素受体激动剂的镇痛作用。
Brain Res. 2012 Aug 30;1471:23-32. doi: 10.1016/j.brainres.2012.06.023. Epub 2012 Jul 2.
5
CB1 receptor activation in the basolateral amygdala produces antinociception in animal models of acute and tonic nociception.在急性和持续性伤害感受的动物模型中,基底外侧杏仁核中的CB1受体激活可产生抗伤害感受作用。
Clin Exp Pharmacol Physiol. 2007 May-Jun;34(5-6):439-49. doi: 10.1111/j.1440-1681.2007.04592.x.
6
Antinociception and modulation of rostral ventromedial medulla neuronal activity by local microinfusion of a cannabinoid receptor agonist.通过局部微量注射大麻素受体激动剂对延髓头端腹内侧神经元活动的镇痛及调节作用
Neuroscience. 2004;124(3):685-93. doi: 10.1016/j.neuroscience.2003.10.001.
7
CB1 receptor mediated analgesia from the Nucleus Reticularis Gigantocellularis pars alpha is activated in an animal model of neuropathic pain.在神经性疼痛动物模型中,源自巨细胞网状核α部的CB1受体介导的镇痛作用被激活。
Brain Res. 2001 Jul 20;908(1):67-74. doi: 10.1016/s0006-8993(01)02605-1.
8
Changes in cannabinoid receptor subtype 1 activity and interaction with metabotropic glutamate subtype 5 receptors in the periaqueductal gray-rostral ventromedial medulla pathway in a rodent neuropathic pain model.在啮齿动物神经病理性疼痛模型中,大麻素受体 1 亚型活性的变化及其与periaqueductal gray-rostral ventromedial medulla 通路中代谢型谷氨酸受体 5 亚型的相互作用。
CNS Neurol Disord Drug Targets. 2012 Mar;11(2):148-61. doi: 10.2174/187152712800269731.
9
Elevation of endocannabinoid levels in the ventrolateral periaqueductal grey through inhibition of fatty acid amide hydrolase affects descending nociceptive pathways via both cannabinoid receptor type 1 and transient receptor potential vanilloid type-1 receptors.通过抑制脂肪酸酰胺水解酶提高腹外侧导水管周围灰质中的内源性大麻素水平,会通过1型大麻素受体和瞬时受体电位香草酸亚型1受体影响下行伤害性感受通路。
J Pharmacol Exp Ther. 2006 Mar;316(3):969-82. doi: 10.1124/jpet.105.093286. Epub 2005 Nov 11.
10
Cannabinoid receptor-mediated inhibition of the rat tail-flick reflex after microinjection into the rostral ventromedial medulla.向大鼠延髓头端腹内侧微量注射后,大麻素受体介导的大鼠甩尾反射抑制作用。
Neurosci Lett. 1998 Feb 6;242(1):33-6. doi: 10.1016/s0304-3940(98)00044-5.

引用本文的文献

1
The Development of Cannabinoids as Therapeutic Agents in the United States.大麻素类药物在美国作为治疗药物的发展。
Pharmacol Rev. 2024 Aug 15;76(5):915-955. doi: 10.1124/pharmrev.123.001121.
2
Convergence of monosynaptic inputs from neurons in the brainstem and forebrain on parabrachial neurons that project to the paraventricular nucleus of the thalamus.来自脑干和前脑的神经元的单突触传入在投射到丘脑室旁核的臂旁核神经元上汇聚。
Brain Struct Funct. 2022 Sep;227(7):2409-2437. doi: 10.1007/s00429-022-02534-6. Epub 2022 Jul 15.
3
Effects of GABAA receptors in nucleus cuneiformis on the cannabinoid antinociception using the formalin test.
使用福马林测试研究楔状核中 GABA 受体对大麻素类药物镇痛作用的影响。
Psychopharmacology (Berl). 2021 Jun;238(6):1657-1669. doi: 10.1007/s00213-021-05800-3. Epub 2021 Mar 13.
4
The prefrontal cortical endocannabinoid system modulates fear-pain interactions in a subregion-specific manner.前额皮质内源性大麻素系统以亚区特异性方式调节恐惧-疼痛相互作用。
Br J Pharmacol. 2019 May;176(10):1492-1505. doi: 10.1111/bph.14376. Epub 2018 Jul 14.