Effects of (-)-stepholidine on NMDA receptors: comparison with haloperidol and clozapine
文献类型：期刊论文
| 作者 | Gu, Wei-hua; Yang, Shen; Shi, Wei-xing; Zhen, Xue-chu; Jin, Guo-zhang
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| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2007-07 |
| 卷号 | 28期号:7页码:953-958 |
| 关键词 | (-)-stepholidine haloperidol clozapine NMDA receptor calcium imaging neuroleptics |
| ISSN号 | 1671-4083 |
| DOI | 10.1111/j.1745-7254.2007.00581.x |
| 文献子类 | Article |
| 英文摘要 | Aim: To examine whether (-)-stepholidine (SPD) has a direct effect on the N-methyl-D-aspartic acid receptors (NMDAR) containing the NMDA receptor subunits NR2A or NR2B and to compare its effect with those of haloperidol (Hal) and clozapine (Cloz). Methods: NMDAR was transiently expressed in human embryonic kidney 293 (HEK293) cells. Changes in intracellular calcium concentration ([Ca2+](i)) induced by NMDAR activation were monitored with Fura-2 ratio imaging techniques. Results: SPD had no significant effects on either subunit of NMDAR at a concentration of less than 100 mu mol/L. Hal selectively inhibited NMDAR containing the NR2B subunit, whereas Cloz inhibited both subunits of NMDAR Although both Hal and Cloz inhibited NR1a/NR2B receptor-mediated Ca2+ influx, their effects were different. Hal was more potent and had a faster peak effect than Cloz. Conclusion: Both Hal and Cloz inhibit NMDAR-mediated function, Whereas SPD produced only a little inhibition at a high concentration. Based on our other studies, the modulation of SPD on NMDAR function may be via D-1 receptor action underlying an indirect mechanism. |
| WOS关键词 | D-ASPARTATE RECEPTORS ; ANTIPSYCHOTIC-DRUGS ; PREFRONTAL CORTEX ; CLINICAL-RESPONSE ; CORTICAL-NEURONS ; L-STEPHOLIDINE ; DOPAMINE D1 ; SCHIZOPHRENIA ; GLUTAMATE ; MODULATION |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:3088167 |
| WOS记录号 | WOS:000247661400005 |
| 出版者 | BLACKWELL PUBLISHING |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273205]  |
| 专题 | 院士及顾问专家 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 | Jin, Guo-zhang |
| 作者单位 | 1.Yale Univ, Sch Med, Dept Psychiat, Neuropsychopharmacol Res Unit, New Haven, CT 06511 USA 2.Chinese Acad Sci, Grad Sch, Shanghai Inst Mat Med, Dept Pharmacol,State Key Lab Drug Res,Shanghai In, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Gu, Wei-hua,Yang, Shen,Shi, Wei-xing,et al. Effects of (-)-stepholidine on NMDA receptors: comparison with haloperidol and clozapine[J]. ACTA PHARMACOLOGICA SINICA,2007,28(7):953-958. |
| APA | Gu, Wei-hua,Yang, Shen,Shi, Wei-xing,Zhen, Xue-chu,&Jin, Guo-zhang.(2007).Effects of (-)-stepholidine on NMDA receptors: comparison with haloperidol and clozapine.ACTA PHARMACOLOGICA SINICA,28(7),953-958. |
| MLA | Gu, Wei-hua,et al."Effects of (-)-stepholidine on NMDA receptors: comparison with haloperidol and clozapine".ACTA PHARMACOLOGICA SINICA 28.7(2007):953-958. |
入库方式： OAI收割
来源：上海药物研究所
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