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(S)-(+)-mecamylamine (TC-5214): a neuronal nicotinic receptor modulator enters phase III trials as an adjunct treatment for Major Depressive Disorder (MDD).

作者信息

Lindsley Craig W

出版信息

ACS Chem Neurosci. 2010 Aug 18;1(8):530-1. doi: 10.1021/cn100070s.

DOI:10.1021/cn100070s
PMID:22778844
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3368682/
Abstract
摘要

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(S)-(+)-mecamylamine (TC-5214): a neuronal nicotinic receptor modulator enters phase III trials as an adjunct treatment for Major Depressive Disorder (MDD).(S)-(+)-美加明(TC-5214):一种神经元烟碱受体调节剂作为重度抑郁症(MDD)的辅助治疗进入III期试验。
ACS Chem Neurosci. 2010 Aug 18;1(8):530-1. doi: 10.1021/cn100070s.
2
Efficacy and tolerability of flexibly-dosed adjunct TC-5214 (dexmecamylamine) in patients with major depressive disorder and inadequate response to prior antidepressant.在对先前的抗抑郁药反应不足的重性抑郁障碍患者中,灵活剂量辅助 TC-5214(地美卡胺)的疗效和耐受性。
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Two Phase III randomised double-blind studies of fixed-dose TC-5214 (dexmecamylamine) adjunct to ongoing antidepressant therapy in patients with major depressive disorder and an inadequate response to prior antidepressant therapy.两项III期随机双盲研究,针对重度抑郁症且对先前抗抑郁治疗反应不足的患者,在持续抗抑郁治疗基础上加用固定剂量的TC-5214(右旋美加明)。
World J Biol Psychiatry. 2015 Oct;16(7):483-501. doi: 10.3109/15622975.2014.989261. Epub 2015 Jan 20.
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Safety and tolerability of dexmecamylamine (TC-5214) adjunct to ongoing antidepressant therapy in patients with major depressive disorder and an inadequate response to antidepressant therapy: results of a long-term study.右旋美加明(TC-5214)辅助治疗对重度抑郁症且对抗抑郁治疗反应不足的患者进行持续抗抑郁治疗的安全性和耐受性:一项长期研究的结果
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Nicotinic antagonist augmentation of selective serotonin reuptake inhibitor-refractory major depressive disorder: a preliminary study.烟碱拮抗剂增强选择性5-羟色胺再摄取抑制剂难治性重度抑郁症:一项初步研究。
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Nicotine, but not mecamylamine, enhances antidepressant-like effects of citalopram and reboxetine in the mouse forced swim and tail suspension tests.在小鼠强迫游泳和悬尾试验中,尼古丁而非美加明增强了西酞普兰和瑞波西汀的抗抑郁样作用。
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Similar activity of mecamylamine stereoisomers in vitro and in vivo.美加明立体异构体在体外和体内的相似活性。
Eur J Pharmacol. 2013 Nov 15;720(1-3):264-75. doi: 10.1016/j.ejphar.2013.10.018. Epub 2013 Oct 23.
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Mecamylamine (Targacept).美加明(Targacept公司生产)。
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Nicotinic acetylcholine receptors as targets for antidepressants.作为抗抑郁药靶点的烟碱型乙酰胆碱受体
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Towards new mechanisms: an update on therapeutics for treatment-resistant major depressive disorder.迈向新机制:治疗难治性重度抑郁症治疗方法的最新进展。
Mol Psychiatry. 2015 Oct;20(10):1142-50. doi: 10.1038/mp.2015.92. Epub 2015 Jul 7.
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Molecular interactions between mecamylamine enantiomers and the transmembrane domain of the human α4β2 nicotinic receptor.(-)-美加明对映异构体与人α4β2 型烟碱型乙酰胆碱受体跨膜结构域的分子相互作用。
Biochemistry. 2014 Feb 11;53(5):908-18. doi: 10.1021/bi400969x. Epub 2014 Jan 30.
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Similar activity of mecamylamine stereoisomers in vitro and in vivo.美加明立体异构体在体外和体内的相似活性。
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Citalopram versus other anti-depressive agents for depression.西酞普兰与其他抗抑郁药治疗抑郁症的比较。
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Translating laboratory discovery to the clinic: from nicotine and mecamylamine to Tourette's, depression, and beyond.将实验室发现转化为临床应用:从尼古丁和美加仑胺到妥瑞氏症、抑郁症等。
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Functional brain imaging of nicotinic effects on higher cognitive processes.尼古丁对高级认知过程影响的功能性脑成像。
Biochem Pharmacol. 2011 Oct 15;82(8):943-51. doi: 10.1016/j.bcp.2011.06.008. Epub 2011 Jun 13.

本文引用的文献

1
The top prescription drugs of 2009 in the US: CNS therapeutics rank among highest grossing.2009年美国的顶级处方药:中枢神经系统治疗药物跻身创收最高的药物之列。
ACS Chem Neurosci. 2010 Jun 16;1(6):407-8. doi: 10.1021/cn1000556.
2
TC-5214 (S-(+)-mecamylamine): a neuronal nicotinic receptor modulator with antidepressant activity.TC-5214(S-(+)-美加明):一种具有抗抑郁活性的神经元烟碱受体调节剂。
CNS Neurosci Ther. 2008 Winter;14(4):266-77. doi: 10.1111/j.1755-5949.2008.00054.x.
3
The economic burden of depression in the United States: how did it change between 1990 and 2000?美国抑郁症的经济负担:1990年至2000年间有何变化?
J Clin Psychiatry. 2003 Dec;64(12):1465-75. doi: 10.4088/jcp.v64n1211.