Effects of ATPM-ET, a novel kappa agonist with partial mu activity, on morphine-induced physical dependence and behavior sensitization in mice
文献类型：期刊论文
| 作者 | Sun, Jian-feng1; Wang, Yu-hua2; Li, Fu-ying1; Lu, Gang1; Tao, Yi-min1; Cheng, Yun1; Chen, Jie1; Xu, Xue-jun1; Chi, Zhi-qiang1 ; Neumeyer, John L.3
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2010-12 |
| 卷号 | 31期号:12页码:1547-1552 |
| ISSN号 | 1671-4083 |
| 关键词 | behavioral sensitization mu opioid receptors morphine kappa opioid receptors physical dependence addiction |
| DOI | 10.1038/aps.2010.164 |
| 文献子类 | Article |
| 英文摘要 | Aim: To investigate the effects of ATPM-ET [(-)-3-N-Ethylaminothiazolo [ 5,4-b]-N-cyclopropylmethylmorphinan hydrochloride] on physical dependence and behavioral sensitization to morphine in mice. Methods: The pharmacological profile of ATPM-ET was characterized using competitive binding and GTP gamma S binding assays. We then examined the antinociceptive effects of ATPM-ET in the hot plate test. Morphine dependence assay and behavioral sensitization assay were used to determine the effect of ATPM-ET on physical dependence and behavior sensitization to morphine in mice. Results: The binding assay indicated that ATPM-ET ATPM-ET exhibited a high affinity to both kappa- and mu-opioid receptors with K-i values of 0.15 nmol/L and 4.7 nmol/L, respectively, indicating it was a full kappa-opioid receptor agonist and a partial mu-opioid receptor agonist. In the hot plate test, ATPM-ET produced a dose-dependent antinociceptive effect, with an ED50 value of 2.68 (2.34-3.07) mg/kg. Administration of ATPM-ET (1 and 2 mg/kg, sc) prior to naloxone (3.0 mg/kg, sc) injection significantly inhibited withdrawal jumping of mice. In addition, ATPM-ET (1 and 2 mg/kg, sc) also showed a trend toward decreasing morphine withdrawal-induced weight loss. ATPM-ET (1.5 and 3 mg/kg, sc) 15 min before the morphine challenge significantly inhibited the morphine-induced behavior sensitization (P<0.05). Conclusion: ATPM-ET may have potential as a therapeutic agent for the treatment of drug abuse. |
| WOS关键词 | OPIOID RECEPTOR AGONIST ; RHESUS-MONKEYS ; PHARMACOLOGICAL CHARACTERIZATION ; ANTINOCICEPTIVE TOLERANCE ; DRUG-ADDICTION ; COCAINE ; DECREASES ; RATS ; ANTAGONIST ; EXPRESSION |
| 资助项目 | Ministry of Science and Technology of China[2009CB522000] ; Ministry of Science and Technology of China[2009ZX09301-001] ; National Natural Science Foundation of China[30873050] ; Chinese Academy of Sciences[KSCX2-YW-R-253] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| WOS记录号 | WOS:000284936500004 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278697]  |
| 专题 | 药物化学研究室 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 药理学第二研究室 |
| 通讯作者 | Zhang, Ao |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Nanjing Univ Chinese Med, Sch Pharm, Nanjing 210046, Peoples R China; 3.Harvard Univ, Sch Med, McLean Hosp, Alcohol & Drug Abuse Res Ctr, Boston, MA 02478 USA |
| 推荐引用方式 GB/T 7714 | Sun, Jian-feng,Wang, Yu-hua,Li, Fu-ying,et al. Effects of ATPM-ET, a novel kappa agonist with partial mu activity, on morphine-induced physical dependence and behavior sensitization in mice[J]. ACTA PHARMACOLOGICA SINICA,2010,31(12):1547-1552. |
| APA | Sun, Jian-feng.,Wang, Yu-hua.,Li, Fu-ying.,Lu, Gang.,Tao, Yi-min.,...&Liu, Jing-gen.(2010).Effects of ATPM-ET, a novel kappa agonist with partial mu activity, on morphine-induced physical dependence and behavior sensitization in mice.ACTA PHARMACOLOGICA SINICA,31(12),1547-1552. |
| MLA | Sun, Jian-feng,et al."Effects of ATPM-ET, a novel kappa agonist with partial mu activity, on morphine-induced physical dependence and behavior sensitization in mice".ACTA PHARMACOLOGICA SINICA 31.12(2010):1547-1552. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。