肌肉松弛剂盐酸依哌立松是一种强效的 P2X7 受体拮抗剂

IF 1.5 4区医学 Q4 CHEMISTRY, MEDICINAL

Chemical & pharmaceutical bulletin Pub Date : 2024-01-01 DOI:10.1248/cpb.c24-00032

Makoto Okada, Takashi Nose

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引用次数: 0

摘要

盐酸依哌立松于 1983 年在日本上市，一直用于改善肌肉张力和治疗痉挛性瘫痪（原产国：卫材株式会社）。然而，其生化作用机制尚不清楚。SB Drug Discovery 采用荧光法评估嘌呤能 P2X（P2X）受体的拮抗作用。在这项研究中，我们发现其靶蛋白是 P2X7 受体。此外，P2X 受体亚型的选择性也很高。这一发现证明了（艾培松-P2X7-疼痛联系）、P2X7 作为药物靶点的有效性以及盐酸艾培松药物重新定位的可能性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Eperisone Hydrochloride, a Muscle Relaxant, Is a Potent P2X7 Receptor Antagonist.

Eperisone Hydrochloride was launched in Japan in 1983 and has been used to improve muscle tone and treat spastic paralysis (Originator: Eisai Co., Ltd.). However, its biochemical mechanism of action is unknown. SB Drug Discovery was used to evaluate purinergic P2X (P2X) receptor antagonism using fluorescence. In this study, we discovered that its target protein is the P2X7 receptor. Also, P2X receptor subtype selectivity was high. This finding demonstrates the (Eperisone-P2X7-pain linkage), the validity of P2X7 as a drug target, and the possibility of drug repositioning of Eperisone Hydrochloride.

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来源期刊

Chemical & pharmaceutical bulletin 医学-化学综合

CiteScore

3.20

自引率

5.90%

发文量

132

审稿时长

1.7 months

期刊介绍： The CPB covers various chemical topics in the pharmaceutical and health sciences fields dealing with biologically active compounds, natural products, and medicines, while BPB deals with a wide range of biological topics in the pharmaceutical and health sciences fields including scientific research from basic to clinical studies. For details of their respective scopes, please refer to the submission topic categories below. Topics: Organic chemistry In silico science Inorganic chemistry Pharmacognosy Health statistics Forensic science Biochemistry Pharmacology Pharmaceutical care and science Medicinal chemistry Analytical chemistry Physical pharmacy Natural product chemistry Toxicology Environmental science Molecular and cellular biology Biopharmacy and pharmacokinetics Pharmaceutical education Chemical biology Physical chemistry Pharmaceutical engineering Epidemiology Hygiene Regulatory science Immunology and microbiology Clinical pharmacy Miscellaneous.