N‐Salicyloyltryptamine, a new anticonvulsant drug, acts on voltage‐dependent Na+, Ca2+, and K+ ion channels

Araújo, Demétrius Antônio Machado de; Mafra, Roberta Amaral; Rodrigues, Andreia Laura Prates; Miguel-Silva, Válter; Beirão, Paulo Sérgio Lacerda; Almeida, Reinaldo Nóbrega de; Quintans‐Júnior, Lucindo José; Souza, M. F. V.; Cruz, Jáder Santos

doi:10.1038/sj.bjp.0705471

Cited by 16 publications

(12 citation statements)

References 35 publications

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“…ethosuximide). 23 Furthermore, Araújo et al 24 have demonstrated that NST promotes the blockade of sodium channels from GH3 cells, corroborating with the results of this work. However, the alteration produced by NST on the time constant of repolarization could also indicate a possible involvement of voltage-gated potassium channels, as was verified by Pisciotta and Prestipino 25 when fenitoine was used.…”

Section: Discussionsupporting

confidence: 89%

Anticonvulsant property of N-salicyloyltryptamine: evidence of enhance of central GABAergic neurotransmission

Quintans‐Júnior

Silva

Quintans

et al. 2009

J. epilepsy clin. neurophysiol.

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AIM: In the present study we verified the anticonvulsant properties of the new tryptamine analogue, N-salicyloyltryptamine (NST), in rodents. METHODS AND RESULTS: In the evaluation of the anticonvulsant activity, NST protected the animals from the incidence of seizures induced by pentylenetetrazole (PTZ) and picrotoxin (PIC), in doses of 100 and 200 mg/kg. NST (100 and 200 mg/kg, i.p.) significantly eliminated the extensor reflex of maximal electric-induced seizure tests in 40% of the experimental animals. However, in the PTZ model FLU (10 mg/kg, i.p.), an antagonist of the benzodiazepine (BZD) site in the GABA A-BZD receptor complex, inhibited the prolongation of seizure latency induced by NST. CONCLUSION: Our results demonstrated an anticonvulsant activity of the new analogue that could be, at least in part, associated to the involvement of the GABAergic mechanism.

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Section: Discussionsupporting

confidence: 89%

Anticonvulsant property of N-salicyloyltryptamine: evidence of enhance of central GABAergic neurotransmission

Quintans‐Júnior

Silva

Quintans

et al. 2009

J. epilepsy clin. neurophysiol.

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“…Throughout this review we showed the complex pharmacological profile of eugenol in blocking different ion channels. Interesting to note is the fact that other anticonvulsant substances seems to exert its effects via multiple mechanisms Araujo et al (2003). From a functional viewpoint, the simultaneous action of eugenol over distinct ion channels may prevent the ability of neuronal cells to trigger action potentials and therefore makes it very attractive as an anticonvulsant agent.…”

Section: Constituents Of Essential Oils That Acts In the Central And mentioning

confidence: 99%

Essential oils components as a new path to understand ion channel molecular pharmacology

2011

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“…Because they are easily cultivated in the laboratory, our patch clamp experiments performed to measure calcium currents were carried out on those neuroendocrine cells. This investigation was done using barium as the charge carrier through the L-type calcium channel (Araújo et al, 2003). AqEx reduced in 30 % this inward current without changing the peak of the current-voltage curve.…”

Section: Discussionmentioning

confidence: 99%

Aqueous leaf extract of Averrhoa carambola L. (Oxalidaceae) reduces both the inotropic effect of BAY K 8644 on the guinea pig atrium and the calcium current on GH3cells

Vasconcelos¹,

Gondim

Cruz³

et al. 2008

Rev. bras. farmacogn.

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RESUMO: "Extrato aquoso das folhas de Averrhoa carambola L. (Oxalidaceae) reduz tanto o efeito inotrópico do BAY K 8644 em átrio de cobaia, quanto a corrente de cálcio em células GH 3 ". Em estudo prévio mostrou-se que o extrato aquoso das folhas de Averrhoa carambola (ExAq) reduziu o inotropismo atrial da cobaia. Por isso, este trabalho avaliou se o ExAq interfere com o infl uxo de cálcio através da membrana celular. A investigação foi conduzida em átrio esquerdo de cobaia, montado em cuba (5 mL, Tyrode, 27 ± 0,1 °C, 95 % O 2 , 5 % CO 2 ), estirado para uma tensão de repouso de 10 mN e submetido a uma estimulação de 2 Hz (0,5 ms, 400 V). O efeito do ExAq sobre a entrada de cálcio nas células foi avaliado em átrio de cobaia e em células GH 3 , estas submetidas a 'patch clamp' na confi guração 'whole cell'. No átrio, o ExAq (1500 μg /mL) deslocou para direita a curva concentração-efeito do (±) BAY K 8644 (agonista dos canais de cálcio tipo-L), aumentando a CE 50 (concentração capaz de produzir 50 % do efeito máximo) de 7,8 ± 0,38 para 115,1 ± 0,44 nM (N = 3, p < 0,05). Em células GH 3 , este extrato (500 μg /mL) reduziu de 282 para 190 pA (30 %) a corrente de cálcio, sem contudo alterar a voltagem de pico da curva desta corrente. Estes resultados mostram que, pelo menos em parte, o efeito inotrópico negativo do ExAq em átrio de cobaia se deve a uma diminuição do infl uxo de cálcio pelos canais tipo-L.Unitermos: Averrhoa carambola, extrato aquoso, corrente de cálcio tipo-L, átrio de cobaia, células GH 3 . ABSTRACT:It was previously showed that aqueous leaf extract (AqEx) of Averrhoa carambola depresses the guinea pig atrial inotropism. Therefore, experiments were carried out on guinea pig left atrium and on pituitary GH 3 cells in order to evaluate the effect of AqEx on the cellular calcium infl ux. The atrium was mounted in an organ chamber (5 mL, Tyrode, 27 ± 0.1 °C, 95 % O 2 , 5 % CO 2 ), stretched to 10 mN, and paced at 2 Hz (0.5 ms, 400 V) and GH 3 cells were submitted to a whole cell voltage clamp confi guration. In the atrium, the AqEx (1500 μg/mL) shifted to the right the concentration-effect curve of the positive inotropic effect produced by (±) BAY K 8644, an L-type calcium channel agonist. The AqEx increased EC 50 (concentration required to promote 50% of the maximum effect) of the inotropic effect of BAY K 8644 from 7.8 ± 0.38 to 115.1 ± 0.44 nM (N = 3; p < 0.05). In GH 3 cells assayed with 500 μg/mL of AqEx, the L-type calcium inward current declined 30 % (from 282 to 190 pA). Nevertheless, the extract did not change the voltage correspondent to the peak current. These data suggest that, at least in part, the negative inotropic effect of AqEx on the guinea pig atrium is due to a reduction of the L-type calcium current.

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N‐Salicyloyltryptamine, a new anticonvulsant drug, acts on voltage‐dependent Na⁺, Ca²⁺, and K⁺ ion channels

Cited by 16 publications

References 35 publications

Anticonvulsant property of N-salicyloyltryptamine: evidence of enhance of central GABAergic neurotransmission

Anticonvulsant property of N-salicyloyltryptamine: evidence of enhance of central GABAergic neurotransmission

Essential oils components as a new path to understand ion channel molecular pharmacology

Aqueous leaf extract of Averrhoa carambola L. (Oxalidaceae) reduces both the inotropic effect of BAY K 8644 on the guinea pig atrium and the calcium current on GH3cells

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