l-tetrahydropalamatine: a potential new medication for the treatment of cocaine addiction.

l-tetrahydropalamatine: a potential new medication for the treatment of cocaine addiction.
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DOI:
10.4155/fmc.11.166
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发表时间:
2012-02
影响因子:
4.2
通讯作者:
Mantsch JR
Mantsch JR
中科院分区:
医学3区
文献类型:
--
作者:
Wang JB;Mantsch JR

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左旋四氢巴马汀(L-THP)是含有千金藤属和Cordycum属植物的草药制剂的活性成分,在中国已被批准用于多种临床适应症,药物名称为罗通定。L-THP的药理学特征,包括多巴胺D1和D2受体的拮抗作用和对多巴胺D3、α肾上腺素能和5-羟色胺受体的作用,表明它可能具有治疗可卡因成瘾的效用。在这篇综述中,我们提供了一个概述的药理学特性的l-THP和证据支持其发展作为一种抗成瘾药物。临床前工作的结果表明,L-THP减弱可卡因的增强/奖励作用和恢复可卡因复吸的大鼠模型进行了总结,并描述了在人类成瘾者中证明疗效的研究结果。最后,概述了L-THP的安全性,并讨论了与FDA批准L-THP相关的挑战。
Levo-tetrahydropalmatine (l-THP) is an active constituent of herbal preparations containing plant species of the genera Stephania and Corydalis and has been approved and used in China for a number of clinical indications under the drug name Rotundine. The pharmacological profile of l-THP, which includes antagonism of dopamine D1 and D2 receptors and actions at dopamine D3, alpha adrenergic and serotonin receptors, suggests that it may have utility for treating cocaine addiction. In this review, we provide an overview of the pharmacological properties of l-THP and the evidence supporting its development as an anti-addiction medication. The results of preclinical work demonstrating that l-THP attenuates cocaine’s reinforcing/rewarding effects and reinstatement in rat models of cocaine relapse are summarized, and the outcomes of studies demonstrating efficacy in human addicts are described. Finally, an overview of the safety profile of l-THP is provided and challenges associated with FDA approval of l-THP are discussed.
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