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组胺H₄受体拮抗剂:耳鸣治疗的新方法?

Histamine H₄ Receptor Antagonists: A New Approach for Tinnitus Treatment?

作者信息

Hagenow Jens, Stark Holger

机构信息

Heinrich Heine University, Institute of Pharmaceutical and Medicinal Chemistry, Universitaetsstr. 1, 40225 Duesseldorf, Germany.

出版信息

Recent Pat CNS Drug Discov. 2015;10(1):6-9. doi: 10.2174/1574889810666150424161907.

Abstract

Tinnitus, a disorder with disruptive sound perception in the head without an external source, affects around 15 % of the worldwide adult population. Since there is no approved drug for the treatment for this symptom, novel strategies need to be developed to provide relief for the patient. A patent from the small French start-up company Sensorion suggests the use of histamine H4 receptor (H4R) inhibitors as potential treatment. Since histamine and its receptor subtypes are strongly involved in neuronal and inflammatory processes in vestibular areas, targeting the H4R could be a novel way to gain a treatment for tinnitus. Although mRNA and protein levels of H4R have been demonstrated on isolated spiral ganglion neurons from mice, the methods of receptor detection as well as the species relevance of the data are under discussion and require considerable further verification, especially on a disease with a high medical need like tinnitus.

摘要

耳鸣是一种在头部无外部声源情况下产生干扰性声音感知的病症,影响着全球约15%的成年人口。由于目前尚无获批用于治疗该症状的药物,因此需要开发新的策略来为患者缓解症状。法国小型初创公司Sensorion的一项专利表明,使用组胺H4受体(H4R)抑制剂可能是一种治疗方法。由于组胺及其受体亚型在前庭区域的神经元和炎症过程中起着重要作用,靶向H4R可能是一种治疗耳鸣的新途径。虽然已经在从小鼠分离出的螺旋神经节神经元上证实了H4R的mRNA和蛋白质水平,但受体检测方法以及数据的物种相关性仍在讨论中,需要进一步大量验证,特别是对于像耳鸣这样有高度医疗需求的疾病。

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