Levo-Tetrahydroberberrubine Produces Anxiolytic-Like Effects in Mice through the 5-HT1A Receptor.
Levo-Tetrahydroberberrubine Produces Anxiolytic-Like Effects in Mice through the 5-HT1A Receptor.
复制标题
Levo-四氢小檗红素通过 5-HT1A 受体在小鼠中产生抗焦虑样作用。
DOI：
10.1371/journal.pone.0168964
复制
发表时间：
2017
期刊：
影响因子：
3.7
通讯作者：
Yang Z
中科院分区：
文献类型：
--
作者：
Mi G;Liu S;Zhang J;Liang H;Gao Y;Li N;Yu B;Yang H;Yang Z
四氢原小檗碱 (THPB) 是从中药延胡索中分离出来的异喹啉生物碱。在本研究中，我们进行了竞争性结合测定，以检查 l-THBr 与已知参与镇静、催眠和焦虑的神经递质受体的结合。我们的结果表明，l-THBr 不与 GABA 受体相互作用，但与多巴胺和血清素受体具有结合亲和力。此外，cAMP 和 [35S]GTPγS 测定用于确定 l-THBr 对多巴胺 (D1、D2) 或血清素 (5-HT) 受体的激动剂或拮抗剂特性。我们的结果表明，l-THBr 显示 D1 和 D2 拮抗剂以及 5-HT1A 激动剂特性。此外，l-THBr处理的啮齿动物在明/暗箱和高架十字迷宫测试中表现出抗焦虑样作用，并且l-THBr的抗焦虑作用可以被选择性5-HT1A受体拮抗剂WAY-100635降低。我们的结果表明，l-THBr 可能主要通过血清素受体产生有效的抗焦虑样作用。
Tetrahydroprotoberberines (THPBs) are isoquinoline alkaloids isolated from the Chinese herb Corydalis yanhusuo. In the present study, we performed competitive binding assays to examine the binding of l-THBr to neurotransmitter receptors known to be involved in sedation, hypnosis and anxiety. Our results show that l-THBr does not interact with GABAergic receptors but has binding affinities for dopamine and serotonin receptors. In addition, cAMP and [35S]GTPγS assays were used to determine the agonist or antagonist properties of l-THBr at dopamine (D1, D2) or serotonin (5-HT) receptors. Our results show that l-THBr displays D1 and D2 antagonist and 5-HT1A agonist properties. Moreover, l-THBr-treated rodents exhibit anxiolytic-like effects in the light/dark box and elevated plus-maze tests, and the anxiolytic effect of l-THBr can be reduced by WAY-100635, a selective 5-HT1A receptor antagonist. Our results suggest that l-THBr may produce potent anxiolytic-like effects mainly through serotonin receptors.