EFFECTS OF H4415 ON PAIN SENSITIVITY IN RAT

被引:0
作者
Marza, Aurelia [1 ]
Caratasu, Catalin Cezar [1 ]
Ciobica, Andrei [1 ]
Bild, Veronica [1 ,2 ]
Vasincu, Alexandru [1 ]
Rusu, Razvan-Nicolae [1 ]
Tamba, Bogdan Ionel [1 ,3 ]
Bild, Walther [1 ,2 ]
机构
[1] Grigore T Popa Univ Med & Pharm, Iasi, Romania
[2] Romanian Acad, Ctr Biomed Res, Iasi Branch, Iasi, Romania
[3] Grigore T Popa Univ Med & Pharm, Adv Ctr Res & Dev Expt Med, Prof Ostin C Mungiu CEMEX, Iasi, Romania
关键词
pain; TRPV channel blockers; thermal stimulation; ION-CHANNEL TRPA1; RECEPTOR; COLD; ACTIVATION; NEURONS; SENSITIZATION;
D O I
10.31925/farmacia.2024.3.4
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
H4415, also known chemically as HC -030031, is a xanthine derivative that acts as an experimental antagonist of the TRPA1 (transient receptor potential ankyrin 1) channels, known to be involved in the transmission of pain signals, particularly in response to inflammatory stimuli. H4415 inhibits the entry of calcium ions into cells, inhibiting a crucial step in the pain signalling pathway. The compound has been studied for its potential in treating both inflammatory and neuropathic pain. This study aims to explore the efficacy of H4415 in reducing pain sensation by blocking TRPA1 channels. Various pain induction experiments such as tail flick, hot plate, cold plate, and pressure algesimetry tests were used, comparing the pain response at various doses of H4415 (0.4 mg/kg, 0.8 mg/kg, 1.2 mg/kg), dissolved in 5% glucose solution to controls. The results suggest that H4415 significantly alleviates pain across all tests, with notable decreases in pain response, mainly at lower doses. Statistical analysis of the results supports the compound's potential as a pain reliever, showing a marked increase in pain thresholds and a reduction in pain sensitivity, results that underscore the importance of TRPA1 channels in pain perception and position H4415 as a promising candidate for treating both inflammatory and neuropathic pain conditions.
引用
收藏
页码:506 / 512
页数:7
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