Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl) pyrazolo[1,5-a][1,3,5]triazine

Autores
Estrada, Martín Hermógenes; Insuasty, Henry; Cuca, Luis Enrique; Marder, Nora Mariel; Fierro, Angélica; Guerrero, Mario Francisco
Año de publicación
2014
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
This work evaluates the central nervous effects in ICR strain mice of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo[1,5-a][1,3,5]triazine (MH4b1), a compound obtained by an efficient one-step reaction of S,S-diethyl 4-methylbenzoylimidodithiocarbonate with 5-amino-3-methyl-1H-pyrazole, in order to assess its neuro-pharmacological profile. The tests applied were: maximal electroshock seizure (MES), pentylenetetrazole (PTZ) seizures, forced swimming, plus maze, marble burying, sleeping time, rota-rod and catalepsy. In addition, MH4b1 binding to the benzodiazepine site of the GABA-A receptor and MH4b1 inhibition of monoamine oxidase (MAO) subtypes A and B were evaluated. MH4b1 showed anticonvulsant effects in a dose dependent manner (30-300 mg/kg, p.o.) against MES and inhibition of MAO-B (IC50: 24.5 µM) without activity at the benzodiazepine site. These data suggest that MH4b1 has anticonvulsant properties related to MAO-B inhibition.
Este trabalho avalia o efeito do 2-etiltio-7-metil-4-(4-metilfenil)pirazol[1,5-a][1,3,5]triazina (MH4b1) no sistema nervoso central de camundongos ICR. O MH4b1 foi obtido por a reação de 4-metilbenzoilimidoditiocarbonato de S,S-dietil e 5-amino-3-metil-1H-pirazol em uma única etapa. O perfil neurofarmacológico foi realizado por testes de convulsão induzida por eletrochoque (MES) e pentilenotetrazol (PTZ) e por testes de nado forçado, labirinto em cruz, esconder as esferas, sono barbitúrico, rota-rod e catalepsia. Também foi avaliada a união do MH4b1 ao o local de ligação de benzodiazepínicos do receptor GABA-A e a capacidade inibitória do MH4b1 sobre a monoaminoxidase (MAO) A e B. O MH4b1 mostrou efeito anticonvulsivante dependente da dose (30-300 mg) no teste do MES e apresentou atividade inibitória da MAO-B (CI50: 24.5 µM) sem interagir com o local de ligação de benzodiazepínicos do receptor. Os resultados sugerem que o MH4b1 tem atividade anticonvulsivante relacionada com a inibição da MAO-B.
Fil: Estrada, Martín Hermógenes. Universidad Nacional de Colombia; Colombia
Fil: Insuasty, Henry. Universidad de Nariño; Colombia
Fil: Cuca, Luis Enrique. Universidad Nacional de Colombia; Colombia
Fil: Marder, Nora Mariel. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Fisicoquímica Biológicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina
Fil: Fierro, Angélica. Universidad de Santiago de Chile; Chile
Fil: Guerrero, Mario Francisco. Universidad Nacional de Colombia; Colombia
Materia
Anticonvulsant.
Electroshock
Drug screening
Pyrazolo-triazine
Monoamine oxidase inhibition
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/11630
Acceder
id CONICETDig_08d0d748faf7d515c61832926de46e22
oai_identifier_str oai:ri.conicet.gov.ar:11336/11630
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl) pyrazolo[1,5-a][1,3,5]triazineEstrada, Martín HermógenesInsuasty, HenryCuca, Luis EnriqueMarder, Nora MarielFierro, AngélicaGuerrero, Mario FranciscoAnticonvulsant.ElectroshockDrug screeningPyrazolo-triazineMonoamine oxidase inhibitionhttps://purl.org/becyt/ford/1.6https://purl.org/becyt/ford/1This work evaluates the central nervous effects in ICR strain mice of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo[1,5-a][1,3,5]triazine (MH4b1), a compound obtained by an efficient one-step reaction of S,S-diethyl 4-methylbenzoylimidodithiocarbonate with 5-amino-3-methyl-1H-pyrazole, in order to assess its neuro-pharmacological profile. The tests applied were: maximal electroshock seizure (MES), pentylenetetrazole (PTZ) seizures, forced swimming, plus maze, marble burying, sleeping time, rota-rod and catalepsy. In addition, MH4b1 binding to the benzodiazepine site of the GABA-A receptor and MH4b1 inhibition of monoamine oxidase (MAO) subtypes A and B were evaluated. MH4b1 showed anticonvulsant effects in a dose dependent manner (30-300 mg/kg, p.o.) against MES and inhibition of MAO-B (IC50: 24.5 µM) without activity at the benzodiazepine site. These data suggest that MH4b1 has anticonvulsant properties related to MAO-B inhibition.Este trabalho avalia o efeito do 2-etiltio-7-metil-4-(4-metilfenil)pirazol[1,5-a][1,3,5]triazina (MH4b1) no sistema nervoso central de camundongos ICR. O MH4b1 foi obtido por a reação de 4-metilbenzoilimidoditiocarbonato de S,S-dietil e 5-amino-3-metil-1H-pirazol em uma única etapa. O perfil neurofarmacológico foi realizado por testes de convulsão induzida por eletrochoque (MES) e pentilenotetrazol (PTZ) e por testes de nado forçado, labirinto em cruz, esconder as esferas, sono barbitúrico, rota-rod e catalepsia. Também foi avaliada a união do MH4b1 ao o local de ligação de benzodiazepínicos do receptor GABA-A e a capacidade inibitória do MH4b1 sobre a monoaminoxidase (MAO) A e B. O MH4b1 mostrou efeito anticonvulsivante dependente da dose (30-300 mg) no teste do MES e apresentou atividade inibitória da MAO-B (CI50: 24.5 µM) sem interagir com o local de ligação de benzodiazepínicos do receptor. Os resultados sugerem que o MH4b1 tem atividade anticonvulsivante relacionada com a inibição da MAO-B.Fil: Estrada, Martín Hermógenes. Universidad Nacional de Colombia; ColombiaFil: Insuasty, Henry. Universidad de Nariño; ColombiaFil: Cuca, Luis Enrique. Universidad Nacional de Colombia; ColombiaFil: Marder, Nora Mariel. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Fisicoquímica Biológicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; ArgentinaFil: Fierro, Angélica. Universidad de Santiago de Chile; ChileFil: Guerrero, Mario Francisco. Universidad Nacional de Colombia; ColombiaUniversidade de Sao Paulo2014-03info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/11630Estrada, Martín Hermógenes; Insuasty, Henry; Cuca, Luis Enrique; Marder, Nora Mariel; Fierro, Angélica; et al.; Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl) pyrazolo[1,5-a][1,3,5]triazine; Universidade de Sao Paulo; Brazilian Journal Of Pharmaceutical Sciences; 50; 1; 3-2014; 73-801984-82502175-9790enginfo:eu-repo/semantics/altIdentifier/url/http://ref.scielo.org/vgtz84info:eu-repo/semantics/altIdentifier/doi/10.1590/S1984-82502011000100007info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-10-15T14:44:30Zoai:ri.conicet.gov.ar:11336/11630instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-10-15 14:44:31.229CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl) pyrazolo[1,5-a][1,3,5]triazine
title Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl) pyrazolo[1,5-a][1,3,5]triazine
spellingShingle Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl) pyrazolo[1,5-a][1,3,5]triazine
Estrada, Martín Hermógenes
Anticonvulsant.
Electroshock
Drug screening
Pyrazolo-triazine
Monoamine oxidase inhibition
title_short Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl) pyrazolo[1,5-a][1,3,5]triazine
title_full Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl) pyrazolo[1,5-a][1,3,5]triazine
title_fullStr Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl) pyrazolo[1,5-a][1,3,5]triazine
title_full_unstemmed Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl) pyrazolo[1,5-a][1,3,5]triazine
title_sort Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl) pyrazolo[1,5-a][1,3,5]triazine
dc.creator.none.fl_str_mv Estrada, Martín Hermógenes
Insuasty, Henry
Cuca, Luis Enrique
Marder, Nora Mariel
Fierro, Angélica
Guerrero, Mario Francisco
author Estrada, Martín Hermógenes
author_facet Estrada, Martín Hermógenes
Insuasty, Henry
Cuca, Luis Enrique
Marder, Nora Mariel
Fierro, Angélica
Guerrero, Mario Francisco
author_role author
author2 Insuasty, Henry
Cuca, Luis Enrique
Marder, Nora Mariel
Fierro, Angélica
Guerrero, Mario Francisco
author2_role author
author
author
author
author
dc.subject.none.fl_str_mv Anticonvulsant.
Electroshock
Drug screening
Pyrazolo-triazine
Monoamine oxidase inhibition
topic Anticonvulsant.
Electroshock
Drug screening
Pyrazolo-triazine
Monoamine oxidase inhibition
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.6
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv This work evaluates the central nervous effects in ICR strain mice of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo[1,5-a][1,3,5]triazine (MH4b1), a compound obtained by an efficient one-step reaction of S,S-diethyl 4-methylbenzoylimidodithiocarbonate with 5-amino-3-methyl-1H-pyrazole, in order to assess its neuro-pharmacological profile. The tests applied were: maximal electroshock seizure (MES), pentylenetetrazole (PTZ) seizures, forced swimming, plus maze, marble burying, sleeping time, rota-rod and catalepsy. In addition, MH4b1 binding to the benzodiazepine site of the GABA-A receptor and MH4b1 inhibition of monoamine oxidase (MAO) subtypes A and B were evaluated. MH4b1 showed anticonvulsant effects in a dose dependent manner (30-300 mg/kg, p.o.) against MES and inhibition of MAO-B (IC50: 24.5 µM) without activity at the benzodiazepine site. These data suggest that MH4b1 has anticonvulsant properties related to MAO-B inhibition.
Este trabalho avalia o efeito do 2-etiltio-7-metil-4-(4-metilfenil)pirazol[1,5-a][1,3,5]triazina (MH4b1) no sistema nervoso central de camundongos ICR. O MH4b1 foi obtido por a reação de 4-metilbenzoilimidoditiocarbonato de S,S-dietil e 5-amino-3-metil-1H-pirazol em uma única etapa. O perfil neurofarmacológico foi realizado por testes de convulsão induzida por eletrochoque (MES) e pentilenotetrazol (PTZ) e por testes de nado forçado, labirinto em cruz, esconder as esferas, sono barbitúrico, rota-rod e catalepsia. Também foi avaliada a união do MH4b1 ao o local de ligação de benzodiazepínicos do receptor GABA-A e a capacidade inibitória do MH4b1 sobre a monoaminoxidase (MAO) A e B. O MH4b1 mostrou efeito anticonvulsivante dependente da dose (30-300 mg) no teste do MES e apresentou atividade inibitória da MAO-B (CI50: 24.5 µM) sem interagir com o local de ligação de benzodiazepínicos do receptor. Os resultados sugerem que o MH4b1 tem atividade anticonvulsivante relacionada com a inibição da MAO-B.
Fil: Estrada, Martín Hermógenes. Universidad Nacional de Colombia; Colombia
Fil: Insuasty, Henry. Universidad de Nariño; Colombia
Fil: Cuca, Luis Enrique. Universidad Nacional de Colombia; Colombia
Fil: Marder, Nora Mariel. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Química y Fisicoquímica Biológicas; Argentina. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica; Argentina
Fil: Fierro, Angélica. Universidad de Santiago de Chile; Chile
Fil: Guerrero, Mario Francisco. Universidad Nacional de Colombia; Colombia
description This work evaluates the central nervous effects in ICR strain mice of 2-ethylthio-7-methyl-4-(4-methylphenyl)pyrazolo[1,5-a][1,3,5]triazine (MH4b1), a compound obtained by an efficient one-step reaction of S,S-diethyl 4-methylbenzoylimidodithiocarbonate with 5-amino-3-methyl-1H-pyrazole, in order to assess its neuro-pharmacological profile. The tests applied were: maximal electroshock seizure (MES), pentylenetetrazole (PTZ) seizures, forced swimming, plus maze, marble burying, sleeping time, rota-rod and catalepsy. In addition, MH4b1 binding to the benzodiazepine site of the GABA-A receptor and MH4b1 inhibition of monoamine oxidase (MAO) subtypes A and B were evaluated. MH4b1 showed anticonvulsant effects in a dose dependent manner (30-300 mg/kg, p.o.) against MES and inhibition of MAO-B (IC50: 24.5 µM) without activity at the benzodiazepine site. These data suggest that MH4b1 has anticonvulsant properties related to MAO-B inhibition.
publishDate 2014
dc.date.none.fl_str_mv 2014-03
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/11630
Estrada, Martín Hermógenes; Insuasty, Henry; Cuca, Luis Enrique; Marder, Nora Mariel; Fierro, Angélica; et al.; Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl) pyrazolo[1,5-a][1,3,5]triazine; Universidade de Sao Paulo; Brazilian Journal Of Pharmaceutical Sciences; 50; 1; 3-2014; 73-80
1984-8250
2175-9790
url http://hdl.handle.net/11336/11630
identifier_str_mv Estrada, Martín Hermógenes; Insuasty, Henry; Cuca, Luis Enrique; Marder, Nora Mariel; Fierro, Angélica; et al.; Anticonvulsant profile of 2-ethylthio-7-methyl-4-(4-methylphenyl) pyrazolo[1,5-a][1,3,5]triazine; Universidade de Sao Paulo; Brazilian Journal Of Pharmaceutical Sciences; 50; 1; 3-2014; 73-80
1984-8250
2175-9790
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/http://ref.scielo.org/vgtz84
info:eu-repo/semantics/altIdentifier/doi/10.1590/S1984-82502011000100007
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Universidade de Sao Paulo
publisher.none.fl_str_mv Universidade de Sao Paulo
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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score 12.891075

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