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世界最新医学信息文摘 2015年第14期 165-165页

作者：李宗明李秀凤河南省漯河医学高等专科学校神经生物学实验室河南省漯河医学高等专科学校

damgo是一种人工合成的μ-阿片受体激动剂,被用于缓解或治疗疼痛,能产生与吗啡相同的镇痛作用,同时又减少对吗啡的耐受性和成瘾性。对急性痛有很强的镇痛作用,但对持久的慢性疼痛的作用尚不清楚。关节腔内注射单碘醋酸钠,可以诱发关节... 详细信息

damgo是一种人工合成的μ-阿片受体激动剂,被用于缓解或治疗疼痛,能产生与吗啡相同的镇痛作用,同时又减少对吗啡的耐受性和成瘾性。对急性痛有很强的镇痛作用,但对持久的慢性疼痛的作用尚不清楚。关节腔内注射单碘醋酸钠,可以诱发关节产生慢性疼痛。本研究的目的是观察damgo对单碘醋酸钠引起骨关节炎模型及诱发疼痛的影响。研究结果表明10-11-10-9摩尔damgo注射入膝关节,可显著地降低外周传入神经纤维放电的频率。这表明damgo可以缓解关节炎性疼痛,治疗关节炎症状。

关键词： damgo 骨关节炎传入神经放电

damgo长期作用对μ—CHO基因表达的影响

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中国药理学会通讯 2000年第2期17卷 31-31页

作者：陆久怡叶菜英等中国医学科学院基础医学研究所药理室，北京100005

MODULATION OF A δ-AND C-FIBER EVOKED RESPONSES OF NOCICEPTIVE NEURONS IN THE SUPERFICIAL AND THE DEEPER DORSAL HORN OF THE MEDULLA:ROLE OF OPIOID RECEPTORS(μ, δ_1, δ_2)

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Journal of Pharmaceutical Analysis 1995年第2期9卷 202-203页

作者：王小民

The present study was designed to investigate the effects of intravenously administered agonists and antagonists at μ(damgo, naloxone,)δ1 (DPDPE,BNTX)andδ2(DELT, NTB)opioid receptors on the Aδ-and C-fiber evoked responses of nociceptive neurons in the superficial and the deeper dorsal horn of the rat *** single unit recording were made from 70 nociceptive neurons(28 NS,42 WDR) in the superficial dorsal horn and 37 nociceptive neurons(4 NS,33 WDR)in the deeper dorsal *** these neurons had an ipsilateral orofacial mechanoreceptive field and majority of these neurons had no spontaneous activity. The latencies for the C fiber evoked responses ranged from 34～105 msec whereas for Aδfiber-evoked responses it ranged from 3～22msec. A clear separation was observed between early and late responses of evoked by Cand Aδ-*** of DPDPE,DELT and damgo produced inhibitory effects on the Aδ-and C-fiber evoked responses of nociceptive neurons in the superficial and thedeeper dorsal *** comparison,the inhibition was more pronounced on the C-fiber evoked response than on the Aδ-fiber evoked response,and damgo produced a stronger inhibitory action than both DELT and DPDPE. Additionally,DPDPE produced facilitation, or inhibition followed by facilitation on the Aδ-and C-response and the effect had longer latency and longer time *** also induced completely oppsite effects on the Aδ-and C-fiber evoked *** the facilitation was observed,the effect was not dose-dependent. Application of BNTX (0.4～1mg/kg),a δ1 receptor antagonist,produced antagonism of DPDPE in 88%(7/8) neurons. Application of the doses (0.7～1mg/kg) of BTB,δ2-receptor antagonist,resulted in antagonism of both DELT and DPDPE. The inhibition of DELT on Aδ-response was antagonized by doses (0.3～1mg/kg)of NTB in 100% (14/14)neurons while the antagonism on C-response was in 79%(11/14) *** effect produced by DPDPE was antagonized by the doses (0.7～1mg/kg) of NTB

关键词： pain trigeminal dorsal horn opioid receptor DPDPE DELT damgo NTB BNTX naloxone

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μ-opioid presynaptic inhibition of GABA release in rat ventrolateral orbital cortex neurons

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μ-opioid presynaptic inhibition of GABA release in rat vent...

共表达人μ阿片受体与Gq蛋白的稳定细胞株的建立及功能鉴定

中国神经科学学会第四次会员代表大会暨第七届全国学术会议

作者： Chao-Ling QU~1,Fu-Quan HUO~1,Fen-Sheng HUANG~1,Yun-Qing LI~2,Jing-Shi TANG~1 1 Department of Physiology and Pathophysiology,Xi''an Jiaotong University School of Medicine,Key Laboratory of Environment and Genes Related to Diseases,Ministry of Education,Xi''an 710061 2 Department of Anatomy and K.K.Leung Brain Research Centre,The Fourth Military Medical University,Xi''an 710032

＜正＞Previous studies have indicated that the ventrolateral orbital cortex（VLO） is involved in modulation of nociception as part of an endogenous analgesic system consisting of the spinal cord-nucleus submedius（Sm）-VLO-periaqueductal gray（PAG）-spinal cord *** of morphine into the VLO depresses the rat tail-flick reflex and suggests that the GABAergic modulation may be involved in the VLO morphine-induced *** provide electrophysiological evidence for the GABAergic modulation mechanism,the present study examined whether the presynapticμ-opioid activation inhibited release of the GAB A neurotransmitter in rat VLO *** TTX,a voltage-dependent Na+ channel blocker and kynurentic acid,a non-selective excitatory amino acid receptor antagonist,pharmacologically separated spontaneous GABAergic miniature inhibitory postsynaptic currents（mIPSCs） were recorded using the whole-cell patch clamp *** results showed that damgo,a specificμ-opioid receptor agonist,inhibited mlPSCs frequency in a dose-dependent manner without affecting mIPSC amplitude in the same VLO *** presynaptic opioid effect was blocked by CTOP,a specificμ-opioid receptor *** alone application did not affect the mIPSC amplitude or *** results provide support for the hypotheses that GABAergic modulation is involved in the opioidinduced antinociception,i.e.,theμ-opioid receptor activation presynaptically inhibits the inhibitory effect of GABAergic neurons on the projection neurons leading to activation of the VLO-PAG brainstem descending inhibitory system and depression of the nociceptive inputs at the spinal cord level.

关键词： ventrolateral orbital cortex mIPSCs damgo CTOP whole-cell patch clamp

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实验技术与管理 2023年第5期40卷 24-30页

作者：石晶晶张毅陈学军朱思庆王陈李丽琴国民核生化灾害防护国家重点实验室北京102205

建立共表达人μ阿片受体(humanμ-opiatereceptor,hMOR,OPRM)与Gq蛋白的CHO-Flp In稳定细胞模型,并鉴定其药理学功能,可为体外高通量筛选靶向OPRM的药物奠定基础。该研究首先构建重组表达质粒OPRM-pcDNA5/FRT,并进行鉴定;然后通过脂质... 详细信息

建立共表达人μ阿片受体(humanμ-opiatereceptor,hMOR,OPRM)与Gq蛋白的CHO-Flp In稳定细胞模型,并鉴定其药理学功能,可为体外高通量筛选靶向OPRM的药物奠定基础。该研究首先构建重组表达质粒OPRM-pcDNA5/FRT,并进行鉴定;然后通过脂质体转染法将OPRM-pcDNA5/FRT、GqG66Di5-pIRES/puro3和FLP重组酶质粒POG44共转染CHO-Flp In细胞,经抗性加压和有限稀释法挑取耐药单克隆,采用FLIPR钙信号检测方法筛选阳性克隆株;最后,通过RT-q PCR对细胞中的OPRM和GqG66Di5m RNA表达水平进行检测,并选用OPRM激动剂damgo和抑制剂Naloxone对稳定细胞株的药理学功能进行鉴定。结果显示:经酶切确定了重组质粒的正确构建;通过重组质粒转染、抗生素加压筛选以及钙信号测定获得22个具有活性的克隆细胞株,其中15号细胞株的荧光信号值最高,命名为Gq-OPRM1-CHO;与对照组相比,Gq-OPRM1-CHO细胞组中OPRM与GqG66Di5基因m RNA水平分别升高约400倍和120倍;在Gq-OPRM1-CHO细胞中,FLIPR钙信号检测激动剂damgo的EC_(50)为0.02±0.002μmol/L,抑制剂Naloxone的IC_(50)为0.04±0.003μmol/L。该研究成功建立了OPRM与GqG66Di5蛋白稳定共表达的细胞模型Gq-OPRM1-CHO,该细胞株具有对OPRM激动剂和拮抗剂特异性反应的药理学功能。

关键词： μ阿片受体 G蛋白耦联受体钙离子实时荧光检测分析系统 damgo

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基底外侧杏仁核—外侧下丘脑通路对类鸦片诱导的脂肪摄入的作用

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燕山大学学报 2008年第1期32卷 49-52页

作者：马慧燕山大学心理健康服务中心河北秦皇岛066004

研究了大鼠脑横核(Acb)内注入μ-类鸦片受体激活剂damgo诱导的脂肪摄入增加与基底外侧杏仁核(BLA)—外侧下丘脑(LH)通路激活的关系。通过立体定位技术将微型不锈钢套管植入大鼠脑的Acb、BLA和LH,通过注射GABA_A受体激活剂muscimol的方... 详细信息

研究了大鼠脑横核(Acb)内注入μ-类鸦片受体激活剂damgo诱导的脂肪摄入增加与基底外侧杏仁核(BLA)—外侧下丘脑(LH)通路激活的关系。通过立体定位技术将微型不锈钢套管植入大鼠脑的Acb、BLA和LH,通过注射GABA_A受体激活剂muscimol的方法暂时失活试验脑区的神经元活性,然后观察失活一侧BLA或对侧LH以及同时失活上述两区对于Acb内注入damgo诱导的脂肪摄入增加的影响。单纯Acb内注入damgo的大鼠(2组)较生理盐水对照组大鼠(1组)2h脂肪摄入量显著增加[(19.10±1.07)g vs.(8.12±0.80) g,F=1080.74,pdamgo诱导的脂肪摄入增加无影响,但同时失活上述两区则完全阻断这种摄入增加,提示Acb内注入damgo所诱导的脂肪摄入增加依赖于BLA-LH通路内复杂、严格的交互作用。

关键词：脂肪摄入横核基底外侧杏仁核外侧下丘脑 damgo muscimol

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