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Discrimination between peptide and non-peptide opioid agonists on the transcription of opioid receptors in two cell lines

机译：两种细胞系中阿片受体与非肽类阿片激动剂之间的区别

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The aim of the present study was to characterize the effects of prolonged use of peptide mu- and delta -receptor agonists [D-Ala(2), N-me-phe, Gly(5)-ol]-enkephalin (DAMGO) and [D-Pen(2), D-Pen(5)]-enkephalin (DPDPE) and non-peptide agonists ohmefentanyl (OMF) and BW373U86 on the transcription of opioid receptors of cultured NG108-15 cell and SHSY5Y cells, respectively using the method of reverse transcription-polymerase chain reaction (RT-PCR). It was found that (1) The abundance of mu- and delta- receptor mRNA decreased significantly up to 48h after the administration of DAMGO and DPDPE, respectively; whereas the inhibitory effect of OMF and BW373U86 lasted only for 24h; (2) DAMGO and DPDPE produced a significant decrease of the mRNA coding for mu -redeptor and 6-receptor at concentrations as low as 10(-8) mol/L and 10(-6) mol/L, respectively, whereas OMF and BW373U86 were effective at concentrations one order of magnitude higher, respectively. These results suggested that (1) Long-term administration of either peptide or non-peptide opioid agonist to cultured cell line produced a significant decrease of the gene expression of opioid receptor at transcription level. (2) The effect of peptide agonists was stronger and lasted longer than that of corresponding nonpeptide agonists. (C) 2001 Elsevier Science Inc. All rights reserved. [References: 20]
机译：本研究的目的是表征长时间使用肽mu和delta受体激动剂[D-Ala（2），N-me-phe，Gly（5）-ol]-脑啡肽（DAMGO）和[D-Pen（2），D-Pen（5）]-脑啡肽（DPDPE）和非肽激动剂ohmefentanyl（OMF）和BW373U86对培养的NG108-15细胞和SHSY5Y细胞阿片受体的转录分别逆转录聚合酶链反应（RT-PCR）的方法。结果发现：（1）分别在DAMGO和DPDPE给药后48h时，mu和delta受体mRNA的丰度明显下降;而OMF和BW373U86的抑制作用仅持续24小时。 （2）在低至10（-8）mol / L和10（-6）mol / L的浓度下，DAMGO和DPDPE产生的编码mu受体和6受体的mRNA显着降低，而OMF和BW373U86在浓度分别高一个数量级时有效。这些结果表明（1）对培养的细胞系长期施用肽或非肽阿片样物质激动剂在转录水平上使阿片样物质受体的基因表达显着降低。 （2）肽激动剂的作用比相应的非肽激动剂的作用更强且持续时间更长。 （C）2001 Elsevier Science Inc.保留所有权利。 [参考：20]

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