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 flu...

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Bibliographic Details
Published inChemical & pharmaceutical bulletin Vol. 72; no. 3; pp. 345 - 348
Main Authors Okada, Makoto, Nose, Takashi
Format Journal Article
LanguageEnglish
Published Japan The Pharmaceutical Society of Japan 30.03.2024
Japan Science and Technology Agency
Subjects
Chemical Biology
drug repositioning
Eperisone
mechanism of action
Muscle relaxants
P2X7
Paralysis
Purine P2X receptors
Receptors
Therapeutic targets
Chemical Biology
mechanism of action
Eperisone
P2X7
drug repositioning
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Summary: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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.c24-00032