Paradoxical relationship between RAVE (relative activity versus endocytosis) values of several opioid receptor agonists and their liability to cause dependence
文献类型：期刊论文
| 作者 | Wang, Yu-hua1,2,3; Sun, Jian-feng2; Tao, Yi-min2; Xu, Xue-jun2; Chi, Zhi-qiang2 ; Liu, Jing-gen2
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| 刊名 | ACTA PHARMACOLOGICA SINICA
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| 出版日期 | 2010-04 |
| 卷号 | 31期号:4页码:393-398 |
| 关键词 | RAVE mu-opioid receptor cyclic AMP endocytosis physical dependence psychological dependence |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2010.19 |
| 文献子类 | Article |
| 英文摘要 | Aim: To examine the relationship between the RAVE (relative activity versus endocytosis) values of opiate agonists and their dependence liability by studying several potent analgesics with special profiles in the development of physical and psychological dependence. Methods: The effects of (-)-cis-(3R, 4S, 2'R) ohmefentanyl (F9202), (+)-cis-(3R, 4S, 2'S) ohmefentanyl (F9204), dihydroetorphine (DHE) and morphine on [S-35] GTP gamma S binding, forskolin-stimulated cAMP accumulation, and receptor internalization were studied in CHO cells stably expressing HA-tagged mu-opioid receptors (CHO-HA-MOR). cAMP overshoot in response to the withdrawal of these compound treatments was also tested. Results: All four agonists exhibited the same rank order of activity in stimulation of [S-35]GTP gamma S binding, inhibition of adenylyl cyclase (AC) and induction of receptor internalization: DHE>F9204>F9202> morphine. Based on these findings and the previous in vivo analgesic data obtained from our and other laboratories, the RAVE values of the four agonists were calculated. The rank order of RAVE values was morphine>F9202>F9204>DHE. For the induction of cAMP overshoot, the rank order was F9202 >= morphine>F9204 >= DHE. Conclusion: Taken in combination with previous findings of these compounds' liability to develop dependence, the present study suggests that the agonist with the highest RAVE value seems to have a relatively greater liability to develop psychological dependence relative to the agonist with the lowest RAVE value. However, the RAVE values of these agonists are not correlated with their probability of developing physical dependence or inducing cAMP overshoot, a cellular hallmark of dependence. |
| WOS关键词 | MORPHINE-TOLERANCE ; OHMEFENTANYL STEREOISOMERS ; PLACE PREFERENCE ; OPIATE DRUGS ; CYCLIC-AMP ; G-PROTEIN ; IN-VIVO ; MICE ; INTERNALIZATION ; DIHYDROETORPHINE |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:3893562 |
| WOS记录号 | WOS:000276834300002 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278924]  |
| 专题 | 药理学第二研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Liu, Jing-gen |
| 作者单位 | 1.China Pharmaceut Univ, Sch Pharm, Nanjing 210009, Peoples R China; 2.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Shanghai 201203, Peoples R China; 3.Nanjing Univ Chinese Med, Sch Pharm, Nanjing 210046, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Yu-hua,Sun, Jian-feng,Tao, Yi-min,et al. Paradoxical relationship between RAVE (relative activity versus endocytosis) values of several opioid receptor agonists and their liability to cause dependence[J]. ACTA PHARMACOLOGICA SINICA,2010,31(4):393-398. |
| APA | Wang, Yu-hua,Sun, Jian-feng,Tao, Yi-min,Xu, Xue-jun,Chi, Zhi-qiang,&Liu, Jing-gen.(2010).Paradoxical relationship between RAVE (relative activity versus endocytosis) values of several opioid receptor agonists and their liability to cause dependence.ACTA PHARMACOLOGICA SINICA,31(4),393-398. |
| MLA | Wang, Yu-hua,et al."Paradoxical relationship between RAVE (relative activity versus endocytosis) values of several opioid receptor agonists and their liability to cause dependence".ACTA PHARMACOLOGICA SINICA 31.4(2010):393-398. |
入库方式： OAI收割
来源：上海药物研究所
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