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• W2288925112 abstract "O receptor de potencial transiente vaniloide 1 (TRPV1) e um canal ionico permeavel a cations ativado por uma serie de estimulos nocivos, como calor, acidificacao e agentes irritantes como a capsaicina. Este receptor e responsavel pela deteccao e transmissao da dor aguda e cronica. Devido a isso, substâncias que modulem a atividade deste receptor apresentam um potencial clinico para o tratamento da dor. Assim, este trabalho objetiva a possivel interacao do flavonoide eriodictiol com o receptor TRPV1. Inicialmente, observamos que o eriodictiol foi capaz de deslocar o radioligante [3H]-resiniferatoxina, em ensaio de uniao especifica, do receptor TRPV1 com uma concentracao inibitoria 50% (IC50) de 46.9 (20.70 - 118.9) nM. Ao mesmo tempo, o eriodictiol tambem inibiu o influxo de calcio estimulado por capsaicina com IC50 de 44,4 (15,6 125,1) nM, sugerindo que este aja como um antagonista do receptor. Alem disso, tambem observamos que o eriodictiol induz antinocicepcao no teste da capsaicina intraplantar com efeito maximo de 49,010.5 e 63,94.0 % de inibicao maxima para o tratamento oral e intratecal, respectivamente, e com uma dose efetiva 50% (DE50) de 2,4 (1,0 5,5) mg/kg 2,2 (1,6 2,9) nmol/site, respectivamente. Alem disso, nao observamos alteracoes na atividade locomotora ou temperatura corporal dos animais. A administracao oral de eriodictiol tambem foi capaz de prevenir a nocicepcao induzida por capsaicina intratecal (71,75,7 % de inibicao). Ao mesmo tempo, o eriodictiol tambem aboliu a hiperalgesia termica e reduziu a alodinia mecânica (62,49,2 %) induzidas por adjuvante completo de Freund. Da mesma forma, o eriodictiol tambem preveniu totalmente a diminuicao de tiois nao proteicos e formacao de 3-nitrotirosina (3-NT) espinhais induzidas por capsaicina, ao passo que apresentou atividade antioxidante direta no texto de neutralizacao do radical ABTS. Em conclusao, nossos resultados mostram que o eriodictiol age como um antagonista do receptor TRPV1, com atividade antioxidante, induzindo antinocicepcao sem os efeitos colaterais e limitacoes esperados para antagonistas do receptor TRPV1.%%%%The transient receptor potential vanilloid 1 (TRPV1) is a calcium permeable channel responsible for the transduction and modulation of acute and chronic pain signaling, being a potential target for treatment of different pain disorders. In spite of that, AMG517, a TRPV1 antagonist, presents several clinical limitations, such as the development of severe hypertermia. The aim of this study was to investigate the possible interaction of the flavonoid eriodictyol with the TRPV1 receptor and its putative antinociceptive and hyperthermic effect. Eriodictyol was able to displace the [3H]-resiniferatoxin binding (IC50 = 47 (21 - 119) nM) and to inhibit the calcium influx mediated by capsaicin (IC50 = 44 (16 125) nM), suggesting that eriodictyol acts as a TRPV1 antagonist. Moreover, eriodictyol induces antinociception in the intraplantar capsaicin test, with maximal effect of 4910 and 644% of inhibition for oral (ED50 = 2 (1-5) mg/kg) and…" @default.
• W2288925112 created "2016-06-24" @default.
• W2288925112 creator A5015596805 @default.
• W2288925112 date "2010-08-13" @default.
• W2288925112 modified "2023-09-24" @default.
• W2288925112 title "Eriodictiol: um flavonóide antagonista do receptor trpv1 com atividade antioxidante" @default.
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