Novel κ-opioid receptor agonist MB-1C-OH produces potent analgesia with less depression and sedation
文献类型：期刊论文
| 作者 | Zhang Lesha3; Wang Jun3; Chen Jianchun2; Tao Yimin3; Wang Yuhua1; Xu Xuejun3; Chen Jie3; Xu Yungen1; Xi Tao1; Hu Xiaowu2 |
| 刊名 | Acta Pharmacologica Sinica
 |
| 出版日期 | 2015 |
| 卷号 | 36期号:5页码:565 |
| 关键词 | κ-opioid receptor MB-1C-OH (-)U50 488H Nor-BNI morphine pain acetic acid-induced writhing formalin test depression sedation |
| ISSN号 | 1671-4083 |
| 英文摘要 | Aim: To characterize the pharmacological profiles of a novel κ-opioid receptor agonist MB-1C-OH. Methods: ~3Hdiprenorphine binding and ~(35)SGTPγS binding assays were performed to determine the agonistic properties of MB-1C-OH. Hot plate, tail flick, acetic acid-induced writhing, and formalin tests were conducted in mice to evaluate the antinociceptive actions. Forced swimming and rotarod tests of mice were used to assess the sedation and depression actions. Results: In ~3Hdiprenorphine binding assay, MB-1C-OH did not bind to μ- and δ-opioid receptors at the concentration of 100 μmol/L,but showed a high affinity for κ-opioid receptor (K_1=35 nmol/L). In ~(35)SGTPγS binding assay, the compound had an E_(max) of 98% and an EC_(50) of 16.7 nmol/L for κ-opioid receptor. Subcutaneous injection of MB-1C-OH had no effects in both hot plate and tail flick tests, but produced potent antinociception in the acetic acid-induced writhing test (ED_(50)=0.39 mg/kg), which was antagonized by pretreatment with a selective κ-opioid receptor antagonist Nor-BNI. In the formalin test, subcutaneous injection of MB-1C-OH did not affect the flinching behavior in the first phase, but significantly inhibited that in the second phase (ED_(50)=0.87 mg/kg). In addition, the sedation or depression actions of MB-1C-OH were about 3-fold weaker than those of the classical k agonist (-)U50,488H. Conclusion: MB-1C-OH is a novel κ-opioid receptor agonist that produces potent antinociception causing less sedation and depression. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/294272]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.中国药科大学 2.第二军医大学 3.中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Zhang Lesha,Wang Jun,Chen Jianchun,et al. Novel κ-opioid receptor agonist MB-1C-OH produces potent analgesia with less depression and sedation[J]. Acta Pharmacologica Sinica,2015,36(5):565. |
| APA | Zhang Lesha.,Wang Jun.,Chen Jianchun.,Tao Yimin.,Wang Yuhua.,...&Liu Jinggen.(2015).Novel κ-opioid receptor agonist MB-1C-OH produces potent analgesia with less depression and sedation.Acta Pharmacologica Sinica,36(5),565. |
| MLA | Zhang Lesha,et al."Novel κ-opioid receptor agonist MB-1C-OH produces potent analgesia with less depression and sedation".Acta Pharmacologica Sinica 36.5(2015):565. |
入库方式： OAI收割
来源：上海药物研究所
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