人参茎叶皂甙对吗啡耐受性的影响

本文研究了人参茎叶皂甙对吗啡耐受性产生的影响。实验结果表明，人参茎叶皂甙５０ｍｇ／ｋｇ灌胃给药能够明显对抗吗啡引起的小鼠自主活动增强现象，并抑制吗啡镇痛（小鼠对夹尾压痛）的耐受作用。长期应用吗啡对小鼠体重增长抑制的作用逐渐减弱。人参茎叶皂甙能够加强吗啡抑制体重增长的作用。上述结果提示。

β-arrestin与吗啡耐受性

吗啡耐受的形成可归因于受体的脱敏、内化和受体下游信号的调控。许多研究表明β-arrestin在阿片受体的脱敏、内化和吗啡耐受形成过程中起关键作用。敲除小鼠控制阿片受体内化的蛋白β-arrestin2基因后。吗啡的镇痛作用明显增强而耐受减弱。最近研究还发现8阿片受体(DOR)的激动可以导致β-arrestin1向核内转移,同时促进依赖β-arrestin1的p27和c-fos的转录,表明β-arrestin具有将受体信号传人细胞核内的信使作用。本综述简要概括了近年来关于β-arrestin与吗啡耐受的研究进展。

胍丁胺的镇痛作用及拮抗吗啡的耐受性和物质依赖性

目的探讨胍丁胺对阿片类药物的耐受和物质依赖的拮抗作用。方法利用行为药理学实验观察胍丁胺对上述作用的影响,使用受体阻滞剂,测定cAMP浓度的改变、一氧化氮合酶(NOS)活性。结果胍丁胺具有镇痛作用;增强吗啡的镇痛作用;及拮抗吗啡的耐受性和物质依赖性作用;咪唑克生可阻断其作用。胍丁胺能阻止cAMP的上调和戒断时的超射,并抑制NOS的活性。结论胍丁胺可抑制吗啡的戒断症状,其可能的机制是通过激活咪唑啉受体抑制cAMP的上调和戒断时的超射及抑制NOS的活性。

Regulatory mechanisms and therapeutic potential of microglial inhibitors in neuropathic pain and morphine tolerance

Microglia are important cells involved in the regulation of neuropathic pain(NPP)and morphine tolerance.Information on their plasticity and polarity has been elucidated after determining their physiological structure,but there is still much to learn about the role of this type of cell in NPP and morphine tolerance.Microglia mediate multiple functions in health and disease by controlling damage in the central nervous system(CNS)and endogenous immune responses to disease.Microglial activation can result in altered opioid system activity,and NPP is characterized by resistance to morphine.Here we investigate the regulatory mechanisms of microglia and review the potential of microglial inhibitors for modulating NPP and morphine tolerance.Targeted inhibition of glial activation is a clinically promising approach to the treatment of NPP and the prevention of morphine tolerance.Finally,we suggest directions for future research on microglial inhibitors.