化学神经科学经典:天奈普汀

IF 4.1 3区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY ACS Chemical Neuroscience Pub Date : 2024-11-06 Epub Date: 2024-10-09 DOI:10.1021/acschemneuro.4c00519
Yu Nishio, Craig W Lindsley, Aaron M Bender
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引用次数: 0

摘要

替奈普汀(1)是一种不同寻常的抗抑郁药,因为它的作用机制似乎与血清素受体或单胺转运体的任何活性无关。事实上,噻奈普汀已被证明是μ阿片受体(MOR)的中度强效激动剂,其次是δ阿片受体(DOR)。此外,噻奈普汀的功效可能与它对谷氨酸介导的神经可塑性途径的作用有关。无论哪种神经递质系统对所观察到的疗效负有主要责任,MOR 激动剂的活性在滥用责任方面都存在问题。越来越多的病例报告表明,噻奈普汀确实被用于娱乐,其剂量远远超出了治疗相关剂量或安全剂量。本综述旨在讨论噻奈普汀的药物化学和药理学,并总结噻奈普汀作为一种安全有效的抗抑郁剂的历史用途与其新出现的滥用潜力之间的惊人差异。
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Classics in Chemical Neuroscience: Tianeptine.

Tianeptine (1) is an unusual antidepressant in that its mechanism of action appears to be independent from any activity at serotonin receptors or monoamine transporters. In fact, tianeptine has been shown to be a moderately potent agonist for the mu opioid receptor (MOR) and to a lesser extent the delta opioid receptor (DOR). Additionally, tianeptine's efficacy may be related to its action on glutamate-mediated pathways of neuroplasticity. Regardless of which neurotransmitter system is primarily responsible for the observed efficacy, the MOR agonist activity is problematic with respect to abuse liability. Increasing numbers of case reports have demonstrated that tianeptine is indeed being used recreationally at doses far beyond what are considered therapeutically relevant or safe, and scheduling reclassifications or outright bans on tianeptine products are ongoing around the world. It is the aim of this review to discuss the medicinal chemistry and pharmacology of tianeptine and to summarize this intriguing discrepancy between tianeptine's historical use as a safe and effective antidepressant and its emerging potential for abuse.

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来源期刊
ACS Chemical Neuroscience
ACS Chemical Neuroscience BIOCHEMISTRY & MOLECULAR BIOLOGY-CHEMISTRY, MEDICINAL
CiteScore
9.20
自引率
4.00%
发文量
323
审稿时长
1 months
期刊介绍: ACS Chemical Neuroscience publishes high-quality research articles and reviews that showcase chemical, quantitative biological, biophysical and bioengineering approaches to the understanding of the nervous system and to the development of new treatments for neurological disorders. Research in the journal focuses on aspects of chemical neurobiology and bio-neurochemistry such as the following: Neurotransmitters and receptors Neuropharmaceuticals and therapeutics Neural development—Plasticity, and degeneration Chemical, physical, and computational methods in neuroscience Neuronal diseases—basis, detection, and treatment Mechanism of aging, learning, memory and behavior Pain and sensory processing Neurotoxins Neuroscience-inspired bioengineering Development of methods in chemical neurobiology Neuroimaging agents and technologies Animal models for central nervous system diseases Behavioral research
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