Adenosine A_1 receptor agonist N~6-cyclohexyl-adenosine induced phosphorylation of delta opioid receptor and desensitization of its signaIing
文献类型：期刊论文
| 作者 | Cheng Yun; Tao Yimin; Sun Jianfeng; Wang Yuhua; Xu Xuejun; Chen Jie; Chi Zhiqiang ; Liu Jinggen
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| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2010 |
| 卷号 | 31期号:7页码:784 |
| 关键词 | adenosine A_1 receptor N~6-cycloh xyladenosine delta opioid receptor cAMP Akt |
| ISSN号 | 1671-4083 |
| 英文摘要 | Aim: To define the effect of adenosine A_1 receptor (AR) on delta opioid receptor (DOR)-mediated signal transduction. Methods: CHO cells stably expressing HA-tagged A_1R and DOR-CFP fusion protein were used. The localization of receptors was observed using confocal microscope. DOR-mediated inhibition of adenylyl cyclase was measured using cyclic AMP assay. Western blots were employed to detect the phosphorylation of Akt and the DOR. The effect of AR agonist N~6-cyclohexyladenosine (CHA) on DOR down-regulation-was assessed using radioligand binding assay. Results: CHA 1 μmol/L time-dependently attenuated DOR agonist D-Pen~(2.5)enkephalin (DPDPE)-induced inhibition of intracellular cAMP accumulation with a t~1/2=2.56 (2.09-3.31) h. Pretreatment with 1 μmol/L CHA for 24 h caused a right shift of the dose-response curve of DPDPE-mediated inhibition of cAMP accumulation, with a significant increase in EC_50 but no change in E_max. Pretreatmentwith 1 μmol/L CHA for 1 h also induced a significant attenuation of DPDPE-stimulated phosphorylation of Akt. Moreover, CHA time-dependently phosphorylated DOR (Ser363), and this effect was inhibited by A_1R antagonist 1,3-Dipropyl-8-cyclopentylxanthine (DPCPX) but not by DOR antagonist naloxone. However, CHA failed to produce the down-regulation of DOR, as neither receptor affinity (K_d) nor receptor density (B_max) of DOR showed significant change after chronic CHA exposure. Conclusion: Activation ofAR by its agonist caused heterologous desensitization ofDOR-mediated inhibition of intracellular cAMP accumulation and phosphorylation of Akt Activation of A_1R by its agonist also induced heterologous phosphorylation but not downregulation of DOR. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/304925]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Cheng Yun,Tao Yimin,Sun Jianfeng,et al. Adenosine A_1 receptor agonist N~6-cyclohexyl-adenosine induced phosphorylation of delta opioid receptor and desensitization of its signaIing[J]. ACTA PHARMACOLOGICA SINICA,2010,31(7):784. |
| APA | Cheng Yun.,Tao Yimin.,Sun Jianfeng.,Wang Yuhua.,Xu Xuejun.,...&Liu Jinggen.(2010).Adenosine A_1 receptor agonist N~6-cyclohexyl-adenosine induced phosphorylation of delta opioid receptor and desensitization of its signaIing.ACTA PHARMACOLOGICA SINICA,31(7),784. |
| MLA | Cheng Yun,et al."Adenosine A_1 receptor agonist N~6-cyclohexyl-adenosine induced phosphorylation of delta opioid receptor and desensitization of its signaIing".ACTA PHARMACOLOGICA SINICA 31.7(2010):784. |
入库方式： OAI收割
来源：上海药物研究所
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