Effects of ohmefentanyl stereoisomers on phosphorylation of cAMP-response element binding protein in cultured rat hippocampal neurons
文献类型：期刊论文
| 作者 | Gao, C; Chen, LW; Tao, YM; Chen, J ; Xu, XJ; Chi, ZQ
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2003-12 |
| 卷号 | 24期号:12页码:1253-1258 |
| 关键词 | ohmefentanyl stereoisomers cAMP-response element binding protein mu opioid receptor cyclic AMP hippocampal neurons phosphorylation |
| ISSN号 | 1671-4083 |
| 文献子类 | Article |
| 英文摘要 | AIM: To define the effects and signal pathways of ohmefentanyl stereoisomers [(-)-cis-(3R,4S,2'R) OMF (F9202), (+)-cis-(3R,4S,2'S) OMF (F9204), and (-)-cis-(3S,4S,2'R) OMF (F9203)] on the phosphorylation of cAMP-response element binding protein (CREB) in cultured rat hippocampal neurons. METHODS: The effects of the three OMF stereoisomers and morphine (Mor) on cAMP accumulation and CREB phosphorylation were monitored by radioimmunoassay and Western blot analysis, respectively. RESULTS: The three OMF stereoisomers and Mor could all partially inhibit forskolin-stimulated (25 mumol/L, 15 min) cAMP accumulation in a dose-dependent manner and this effect could be reversed by naloxone. F9202, F9204, and Mor could significantly increase CREB phosphorylation from 2.88 to 3.59 folds over control levels after 30-min exposure. This effect was reversed by naloxone, but F9203 failed to increase CREB phosphorylation. KN-62 and staurosporine significantly blocked the opioids-induced CREB phosphorylation, while H-89 and PD 98059 had no effect on the actions. CONCLUSION: Mor, F9202, and F9204, which could induce psychological dependence affected via the p-opioid receptor, stimulated intracellular signal pathways involving Ca2+/calmodulin-dependent protein kinases (CCDPK) and protein kinase C (PKC) pathways, which in turn initiated CREB phosphorylation. F9203, which could not induce dependence, had no effect on CREB phosphorylation in hippocampal neurons. The increased CREB phosphorylation in hippocampal neurons may play a role in opioids dependence. |
| WOS关键词 | CREB PHOSPHORYLATION ; ANALGESIC ACTIVITY ; OPIOID RECEPTORS ; MICE ; ADDICTION |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:1270661 |
| WOS记录号 | WOS:000187218600013 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/274151]  |
| 专题 | 院士及顾问专家 |
| 通讯作者 | Chi, ZQ |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Shanghai 200031, Peoples R China 2.Xuzhou Med Coll, Res Ctr Biochem & Mol Biol, Xuzhou 221002, Jiangsu, Peoples R China |
| 推荐引用方式 GB/T 7714 | Gao, C,Chen, LW,Tao, YM,et al. Effects of ohmefentanyl stereoisomers on phosphorylation of cAMP-response element binding protein in cultured rat hippocampal neurons[J]. ACTA PHARMACOLOGICA SINICA,2003,24(12):1253-1258. |
| APA | Gao, C,Chen, LW,Tao, YM,Chen, J,Xu, XJ,&Chi, ZQ.(2003).Effects of ohmefentanyl stereoisomers on phosphorylation of cAMP-response element binding protein in cultured rat hippocampal neurons.ACTA PHARMACOLOGICA SINICA,24(12),1253-1258. |
| MLA | Gao, C,et al."Effects of ohmefentanyl stereoisomers on phosphorylation of cAMP-response element binding protein in cultured rat hippocampal neurons".ACTA PHARMACOLOGICA SINICA 24.12(2003):1253-1258. |
入库方式： OAI收割
来源：上海药物研究所
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