氯卡塞林:值得进一步深入研究吗?最新研究成果。

IF 2.7 4区 医学 Q3 NEUROSCIENCES
Marianna Mazza, Georgios D Kotzalidis, Giuseppe Marano, Domenico De Berardis, Giovanni Martinotti, Enrico Romagnoli, Giuseppe Biondi-Zoccai, Antonio Abbate, Gabriele Sani
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引用次数: 0

摘要

Lorcaserin 是一种 3-苯并氮杂卓,能与下丘脑中的 5-HT2C 血清素受体结合,从而介导饥饿感和/或饱腹感的产生;还能与腹侧被盖区中的 5-HT2C 血清素受体结合,而腹侧被盖区是间叶和中皮层多巴胺能投射的起源部位,能介导愉悦感和奖赏感的产生。这种药物最初被开发用于治疗肥胖症,并显示出疗效,随后被试用于对抗药物使用(主要是可卡因、大麻、阿片类药物和尼古丁)和渴求,但显示出不一致的效果。自 2020 年起,美国食品和药物管理局以发现长期使用该药物会增加某些类型癌症的发病率为由,主动从美国市场撤出了该药物。正在进行的研究表明,如果能证明洛卡西林没有致癌作用,那么它可能对肥胖症以外的各种疾病和病症具有治疗潜力。由于 5-HT2C 受体参与多种生理功能(情绪、进食、生殖行为、与冲动有关的神经元过程以及调节与奖赏有关的机制),这种药物有可能治疗不同的中枢神经系统疾病,如抑郁症和精神分裂症。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Lorcaserin: Worthy of Further Insights? Results from Recent Research.

Lorcaserin is a 3-benzazepine that binds 5-HT2C serotonin receptors in the hypothalamus, where it mediates lack of hunger and/or satiety, and in the ventral tegmental area, the site of origin of the mesolimbic and mesocortical dopaminergic projections, which mediate pleasure and reward. The drug has been first developed for the treatment of obesity, where it has shown efficacy, and subsequently trialed to counter substance use (mostly cocaine, cannabis, opioids, and nicotine) and craving, but showed inconsistent effects. Since 2020, the US Food and Drug Administration obtained that the drug was voluntarily withdrawn from the US market on the grounds that its long-term use was found to be associated with a greater incidence of some types of cancer. Provided it can show to be free from cancerogenic effects, ongoing research suggests that lorcaserin may have therapeutic potential for a variety of disorders and conditions beyond obesity. Since 5-HT2C receptors are involved in many diversified physiological functions (mood, feeding, reproductive behavior, neuronal processes related to impulsiveness, and modulating reward-related mechanisms) this drug has the potential to treat different central nervous system conditions, such as depression and schizophrenia.

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来源期刊
CiteScore
5.10
自引率
3.30%
发文量
158
审稿时长
6-12 weeks
期刊介绍: Aims & Scope CNS & Neurological Disorders - Drug Targets aims to cover all the latest and outstanding developments on the medicinal chemistry, pharmacology, molecular biology, genomics and biochemistry of contemporary molecular targets involved in neurological and central nervous system (CNS) disorders e.g. disease specific proteins, receptors, enzymes, genes. CNS & Neurological Disorders - Drug Targets publishes guest edited thematic issues written by leaders in the field covering a range of current topics of CNS & neurological drug targets. The journal also accepts for publication original research articles, letters, reviews and drug clinical trial studies. As the discovery, identification, characterization and validation of novel human drug targets for neurological and CNS drug discovery continues to grow; this journal is essential reading for all pharmaceutical scientists involved in drug discovery and development.
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