Literature DB >> 14645142

N-salicyloyltryptamine, a new anticonvulsant drug, acts on voltage-dependent Na+, Ca2+, and K+ ion channels.

Démetrius Antonio Machado Araújo1, Roberta Amaral Mafra, Andréia Laura Prates Rodrigues, Válter Miguel-Silva, Paulo Sérgio Lacerda Beirão, Reinaldo Nóbrega de Almeida, Lucindo Quintans, Maria Fátima Vanderlei de Souza, Jader Santos Cruz.   

Abstract

1. The aim of this work was to study the effects of N-salicyloyltryptamine (STP), a novel anticonvulsant agent, on voltage-gated ion channels in GH3 cells. 2. In this study, we show that STP at 17 microM inhibited up to 59.2+/-10.4% of the Ito and 73.1+/-8.56% of the IKD K+ currents in GH3 cells. Moreover, the inhibitory activity of the drug STP on K+ currents was dose-dependent (IC50=34.6+/-8.14 microM for Ito) and partially reversible after washing off. 3. Repeated stimulation at 1 Hz (STP at 17 microM) led to the total disappearance of Ito current, and an enhancement of IKD. 4. In the cell-attached configuration, application of STP to the bath increased the open probability of large-conductance Ca2+-activated K+ channels. 5. STP at 17 microM inhibited the L-type Ca2+ current by 54.9+/-7.50% without any significant changes in the voltage dependence. 6. STP at 170 microM inhibited the TTX-sensitive Na+ current by 22.1+/-2.41%. At a lower concentration (17 microM), no effect on INa was observed. 7. The pharmacological profile described here might contribute to the neuroprotective effect exerted by this compound in experimental 'in vivo' models.

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Year:  2003        PMID: 14645142      PMCID: PMC1574129          DOI: 10.1038/sj.bjp.0705471

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  36 in total

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Authors:  V K Gribkoff; J E Starrett; S I Dworetzky
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Review 2.  High-conductance calcium-activated potassium channels; structure, pharmacology, and function.

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3.  Two distinct calcium-activated potassium currents in a rat anterior pituitary cell line.

Authors:  A K Ritchie
Journal:  J Physiol       Date:  1987-04       Impact factor: 5.182

4.  Inactivating 'ball' peptide from Shaker B blocks Ca(2+)-activated but not ATP-dependent K+ channels of rat skeletal muscle.

Authors:  P S Beirão; N W Davies; P R Stanfield
Journal:  J Physiol       Date:  1994-01-15       Impact factor: 5.182

5.  Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches.

Authors:  O P Hamill; A Marty; E Neher; B Sakmann; F J Sigworth
Journal:  Pflugers Arch       Date:  1981-08       Impact factor: 3.657

6.  Properties of single calcium-activated potassium channels in cultured rat muscle.

Authors:  J N Barrett; K L Magleby; B S Pallotta
Journal:  J Physiol       Date:  1982-10       Impact factor: 5.182

Review 7.  Calcium-activated potassium channels in adrenal chromaffin cells.

Authors:  C J Lingle; C R Solaro; M Prakriya; J P Ding
Journal:  Ion Channels       Date:  1996

8.  Intrinsic voltage dependence and Ca2+ regulation of mslo large conductance Ca-activated K+ channels.

Authors:  J Cui; D H Cox; R W Aldrich
Journal:  J Gen Physiol       Date:  1997-05       Impact factor: 4.086

9.  The new anticonvulsant retigabine (D-23129) acts as an opener of K+ channels in neuronal cells.

Authors:  C Rundfeldt
Journal:  Eur J Pharmacol       Date:  1997-10-08       Impact factor: 4.432

10.  The inactivating K+ current in GH3 pituitary cells and its modification by chemical reagents.

Authors:  G S Oxford; P K Wagoner
Journal:  J Physiol       Date:  1989-03       Impact factor: 5.182

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  4 in total

1.  Screening an In-House Isoquinoline Alkaloids Library for New Blockers of Voltage-Gated Na+ Channels Using Voltage Sensor Fluorescent Probes: Hits and Biases.

Authors:  Quentin Coquerel; Claire Legendre; Jacinthe Frangieh; Stephan De Waard; Jérôme Montnach; Leos Cmarko; Joseph Khoury; Charifat Said Hassane; Dimitri Bréard; Benjamin Siegler; Ziad Fajloun; Harold De Pomyers; Kamel Mabrouk; Norbert Weiss; Daniel Henrion; Pascal Richomme; César Mattei; Michel De Waard; Anne-Marie Le Ray; Christian Legros
Journal:  Molecules       Date:  2022-06-28       Impact factor: 4.927

2.  Bioassay-guided evaluation of antinociceptive effect of N-salicyloyltryptamine: a behavioral and electrophysiological approach.

Authors:  Lucindo J Quintans; Davi A Silva; Jullyana S Siqueira; Adriano A S Araújo; Rosana S S Barreto; Leonardo R Bonjardim; Josimari M Desantana; Waldeci De Lucca; Maria F V Souza; Stanley J C Gutierrez; José Maria Barbosa-Filho; Valter J Santana-Filho; Demétrius A M Araújo; Reinaldo N Almeida
Journal:  J Biomed Biotechnol       Date:  2010-10-05

3.  Replacement of Asymmetric Synaptic Profiles in the Molecular Layer of Dentate Gyrus Following Cycloheximide in the Pilocarpine Model in Rats.

Authors:  Simone Bittencourt; Luciene Covolan; Clement Hamani; Beatriz M Longo; Flávio P Faria; Edna Freymuller; Ole P Ottersen; Luiz E Mello
Journal:  Front Psychiatry       Date:  2015-11-17       Impact factor: 4.157

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

Authors:  Robson Cavalcante Veras; Darizy Flávia Silva; Lorena Soares Bezerra; Valéria Lopes de Assis; Walma Pereira de Vasconcelos; Maria do Carmo Alustau; José George Ferreira de Albuquerque; Fabíola Fialho Furtado; Islania Giselia de Albuquerque Araújo; Fátima de Lourdes Assunção Araújo de Azevedo; Thais Porto Ribeiro; José Maria Barbosa-Filho; Stanley Juan Chavez Gutierrez; Isac Almeida Medeiros
Journal:  Molecules       Date:  2018-01-28       Impact factor: 4.411

  4 in total

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