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Papers of the Week


January 27, 2023


Fundam Clin Pharmacol


http://www.ncbi.nlm.nih.gov/pubmed/36579760?dopt=Abstract

LQM10, a guanylhydrazone derivative, reduces nociceptive and inflammatory responses in mice.

Authors

Noé J P, de Souza Ferro J N, da Silva Rodrigues É E, da Silva-Júnior E F, Alexandre-Moreira M S, de Araújo-Junior J X, Barreto E
Fundam Clin Pharmacol. 2022 Dec 29.
PMID: 36579760.

Abstract

In the present study, we examined the antinociceptive and anti-inflammatory activities of a guanylhydrazone derivative, (E)-(3,5-di-tert-butyl-4-hydroxybenzylidene)-2-guanylhydrazone hydrochloride (LQM10), in mice. The antinociceptive effect was determined by assessing behavioural responses in different pain models, while anti-inflammatory activity was examined in carrageenan-induced pleurisy. Intraperitoneal LQM10 administration reduced the acetic acid-induced nociceptive behaviour, a phenomenon which was unaltered by pretreatment with yohimbine, atropine, naloxone, or glibenclamide. In the formalin assay, LQM10 reduced nociceptive behaviour only in the second phase, indicating an inhibitory effect on inflammatory pain. LQM10 did not alter the pain latency in the hot plate assay and did not impact the locomotor activity of mice in the rotarod assay. In the carrageenan-induced pleurisy assay, LQM10 treatment inhibited critical events involved in inflammatory responses, namely, leucocyte recruitment, plasma leakage, and increased inflammatory mediators (tumour necrosis factor [TNF]-α and interleukin [IL]-1β) in the pleural exudate. Overall, these results indicate that LQM10 exhibits antinociceptive effects associated with peripheral mechanisms and anti-inflammatory activity mediated via a reduction in leucocyte migration and proinflammatory mediators, rendering this compound a promising candidate for treating pain and inflammatory process.