阿片受体激动剂不同调节mu-opioid受体和贩卖蛋白质在体内。

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帕特尔MB, Patel CN, Rajashekara V, Yoburn BC

阿片受体激动剂不同调节mu-opioid受体和贩卖蛋白质在体内。

摩尔杂志。2002年12月,62 (6):1464 - 70。

PubMed ID

12435815 (在PubMed

]

文摘

慢性阿片受体激动剂治疗产生宽容和在某些情况下阿片受体内化和下调。吗啡和埃托啡诱导;然而,只有埃托啡产生mu-opioid受体(muOR)下调。体外研究表明dynamin-2 (DYN-2)和g蛋白受体kinase-2 (GRK-2)在这些流程。因此,我们研究了埃托啡和吗啡对监管GRK-2和DYN-2鼠标脊髓。小鼠治疗7天与埃托啡(注入200 microg /公斤/天)或吗啡(40毫克/公斤/天灌注+一个25毫克植入颗粒)。控制与安慰剂颗粒植入。在植入后第七天老鼠检测电脑。[D-Ala (2), N-Me-Phe (4), g (5) ol)脑啡肽(DAMGO)镇痛。在其他老鼠,脊髓被[(3)H] DAMGO绑定研究或GRK-2 DYN-2蛋白质和mRNA丰度测定。埃托啡和吗啡产生显著公差(ED(50)转变= 7.6 - 7.3倍,吗啡和埃托啡,分别)。 Etorphine decreased spinal muOR density by approximately 30%, whereas morphine did not change muOR density. Etorphine increased ( approximately 70%) DYN-2 protein abundance and decreased its mRNA (31%), whereas it had no effect on GRK-2 protein and mRNA abundance. Morphine had no effect on either DYN-2 or GRK-2 protein or mRNA abundance. These data raise the possibility that unequal receptor regulation by etorphine and morphine might be due to differential regulation of trafficking proteins. Overall, receptor down-regulation associated with chronic etorphine treatment may accelerate dynamin-related activity. Finally, the decrease in DYN-2 mRNA may be related to stabilization of DYN-2 protein abundance, which might inhibit transcription.

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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