体内调节mu-opioid受体密度远系繁殖和基因表达在CXBK和瑞士韦伯斯特老鼠。

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Duttaroy, Yoburn BC

体内调节mu-opioid受体密度远系繁殖和基因表达在CXBK和瑞士韦伯斯特老鼠。

Synapse。2000年8月,37 (2):118 - 24。

PubMed ID

10881033 (在PubMed

]

文摘

体内慢性治疗阿片受体激动剂埃托啡会使mu-opioid受体密度,产生耐受性,并在鼠标调节基因表达。停止治疗后,有增加mu-opioid受体信使rna水平与复苏mu-opioid受体有关。然而,埃托啡对信使rna治疗期间的规定的影响目前不清楚。在这项研究中,etorphine-induced mu-opioid受体密度的变化,信使rna,阿片类药物镇痛效力确定在两个鼠标菌株在大脑基底mu-opioid受体密度不同。CXBK远系繁殖老鼠(mu-opioid受体缺陷)和瑞士韦伯斯特小鼠植入与安慰剂南卡罗来纳州丸(控制)或埃托啡微型泵(250 microg /公斤/天)1 - 7天,mu-opioid受体密度或mRNA水平在整个大脑进行评估或老鼠检测埃托啡镇痛治疗后7天。控制CXBK老鼠,mu-receptor密度大约是40%不到的瑞士韦伯斯特,尽管mRNA丰富两株相似。埃托啡的效力是4倍大控制相比,瑞士韦伯斯特CXBK老鼠。埃托啡治疗下降(约25 - 40%)mu-receptor密度同样在这两个菌株在治疗。埃托啡镇痛公差的大小是8番鼠标菌株。埃托啡产生两相的影响受体信使rna在菌株水平下降(25%),3天,增加了7天(30 - 40%)。 mRNA levels remained elevated (55%) 16 h following the end of the 7 day etorphine treatment. Taken together, these data suggest that in vivo etorphine treatment that produces mu-opioid receptor downregulation and tolerance, can regulate mu-opioid receptor mRNA abundance. Receptor downregulation may initially induce decreases in mRNA levels since downregulation preceded a decrease in gene expression. Prolonged (>3 days) receptor downregulation may be responsible for increasing message levels and may be important in recovery of receptors following treatment. In addition, the magnitude of changes in receptor density, mRNA, and tolerance were similar in both CXBK and Swiss Webster mice, indicating that the mechanisms required for receptor regulation and its functional consequences are independent of basal mu-opioid receptor density.

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药物靶点

药物	目标	类	生物	药理作用	行动
埃托啡	Mu-type阿片受体	蛋白质	人类	是的	受体激动剂	细节