Bioassay-Guided Evaluation of Antinociceptive Effect of<i>N</i>-Salicyloyltryptamine: A Behavioral and Electrophysiological Approach

Quintans‐Júnior, Lucindo J.; Silva, Davi A.; Siqueira, Jullyana S.; Araújo, Adriano A. S.; Barreto, Rosana S.S.; Bonjardim, Leonardo Rigoldi; DeSantana, Josimari Melo; Júnior, Waldeci De Lucca; Souza, M. F. V.; Gutierrez, Stanley Juan Chaves; Barbosa-Filho, José Maria; Filho, Valter Joviniano de Santana; Araújo, Demétrius Antônio Machado de; Almeida, Reinaldo Nóbrega de

doi:10.1155/2010/230745

Cited by 5 publications

(2 citation statements)

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“…The major finding of this study was that this tryptamine analogue induced marked vasorelaxation by activating the NO/sGC pathway and reducing Ca 2+ influx. The actions of STP have been investigated in some biological systems and have revealed the involvement of ionic channels [ 16 , 17 , 19 ]. However, there have been no studies reporting the effect of STP on the cardiovascular system.…”

Section: Discussionmentioning

confidence: 99%

“…In general, benzyl or phenethyl substituted tryptamines have significant effects on neuronal and gastrointestinal system [ 13 , 14 ]. A benzyltryptamine analogue, N -salicyloyltryptamine (STP), reduced the generation of action potentials in neuronal cells and strongly influencing neuronal excitability through its action on ion channels [ 15 , 16 , 17 ]. In guinea pig ileum, STP is a smooth muscle relaxant [ 18 ].…”

Section: Introductionmentioning

confidence: 99%

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N-Salicyloyltryptamine, an N-Benzoyltryptamine Analogue, Induces Vasorelaxation through Activation of the NO/sGC Pathway and Reduction of Calcium Influx

et al. 2018

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Benzoyltryptamine analogues act as neuroprotective and spasmolytic agents on smooth muscles. In this study, we investigated the ability of N-salicyloyltryptamine (STP) to produce vasorelaxation and determined its underlying mechanisms of action. Isolated rat mesenteric arteries with and without functional endothelium were studied in an isometric contraction system in the presence or absence of pharmacological inhibitors. Amperometric experiments were used to measure the nitric oxide (NO) levels in CD31+ cells using flow cytometry. GH3 cells were used to measure Ca2+ currents using the whole cell patch clamp technique. STP caused endothelium-dependent and -independent relaxation in mesenteric rings. The endothelial-dependent relaxations in response to STP were markedly reduced by L-NAME (endothelial NO synthase—eNOS—inhibitor), jHydroxocobalamin (NO scavenger, 30 µM) and ODQ (soluble Guanylyl Cyclase—sGC—inhibitor, 10 µM), but were not affected by the inhibition of the formation of vasoactive prostanoids. These results were reinforced by the increased NO levels observed in the amperometric experiments with freshly dispersed CD31+ cells. The endothelium-independent effect appeared to involve the inhibition of voltage-gated Ca2+ channels, due to the inhibition of the concentration-response Ca2+ curves in depolarizing solution, the increased relaxation in rings that were pre-incubated with high extracellular KCl (80 mM), and the inhibition of macroscopic Ca2+ currents. The present findings show that the activation of the NO/sGC/cGMP pathway and the inhibition of gated-voltage Ca2+ channels are the mechanisms underlying the effect of STP on mesenteric arteries.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

N-Salicyloyltryptamine, an N-Benzoyltryptamine Analogue, Induces Vasorelaxation through Activation of the NO/sGC Pathway and Reduction of Calcium Influx

et al. 2018

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Citronellol, a monoterpene alcohol, reduces nociceptive and inflammatory activities in rodents

et al. 2012

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We describe the antinociceptive and anti-inflammatory properties of citronellol (CT) in rodents. CT, a monoterpene alcohol, is a naturally occurring monoterpene compound prevalent in essential oils of various aromatic plant species, such as Cymbopogon citratus. In mice, when evaluated against acetic-acid-induced abdominal writhing, CT (25, 50 and 100 mg/kg, i.p.) reduced (P < 0.001) the amount of writhing compared to the control group. In the formalin test, CT also significantly inhibited both the early (neurogenic pain) and the late (inflammatory pain) phases of formalin-induced licking (P < 0.001). When assessed in a thermal model of pain, CT (100 mg/kg, i.p.) caused a significant increase (P < 0.05) in the latency response on the hot-plate test. Such results were unlikely to be caused by motor abnormality. The anti-inflammatory activity of CT was investigated through carrageenan-induced pleurisy in mice. Pretreatment with CT was able to inhibit both neutrophil infiltration and the increase in TNF-α level in the exudates from carrageenan-induced pleurisy. In in vitro experiments, CT (1 and 100 μg/ml) also decreased nitric oxide production by LPS-stimulated macrophage. Together, these results indicate that CT is effective as an analgesic compound in various pain models, with its action probably mediated by the inhibition of peripheral mediators as well as central inhibitory mechanisms that could be related to its strong antioxidant effect observed in vitro.

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Antinociceptive effect of semi-purified petroleum ether partition of Muntingia calabura leaves

Zakaria

Sani

Kadir

et al. 2016

Revista Brasileira de Farmacognosia

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Bioassay-Guided Evaluation of Antinociceptive Effect ofN-Salicyloyltryptamine: A Behavioral and Electrophysiological Approach

Cited by 5 publications

References 21 publications

N-Salicyloyltryptamine, an N-Benzoyltryptamine Analogue, Induces Vasorelaxation through Activation of the NO/sGC Pathway and Reduction of Calcium Influx

N-Salicyloyltryptamine, an N-Benzoyltryptamine Analogue, Induces Vasorelaxation through Activation of the NO/sGC Pathway and Reduction of Calcium Influx

Citronellol, a monoterpene alcohol, reduces nociceptive and inflammatory activities in rodents

Antinociceptive effect of semi-purified petroleum ether partition of Muntingia calabura leaves

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