Estudos psicofarmacológicos pré clínicos do 3-fenil-5-(4-metilfenil)-imidazolidin-2,4-diona (hpa-05) em camundongos

Detalhes bibliográficos
Ano de defesa: 2013
Autor(a) principal: Maia, Ana Karina Holanda Leite lattes
Orientador(a): Almeida, Reinaldo Nobrega de lattes
Banca de defesa: Não Informado pela instituição
Tipo de documento: Tese
Tipo de acesso: Acesso aberto
Idioma: por
Instituição de defesa: Universidade Federal da Paraí­ba
Programa de Pós-Graduação: Programa de Pós Graduação em Produtos Naturais e Sintéticos Bioativos
Departamento: Farmacologia
País: BR
Palavras-chave em Português:
Palavras-chave em Inglês:
Área do conhecimento CNPq:
Link de acesso: https://repositorio.ufpb.br/jspui/handle/tede/6803
Resumo: Heterocyclic compounds are found in many drugs with several therapeutic purposes, particularly in hydantoin derivatives. These derivatives, such as imidazolidine pharmaceuticals are employed as: anticonvulsants, cicatrizants, muscle relaxants, antimicrobials and antitumorals. Previous studies, using behavioral methodologies, have demonstrated that HPA-05 (3-phenyl-5-(4-methylphenyl) imidazolidine-2,4-dione) presented depressant actions on the CNS (Central Nervous System) with indications such as antinociceptives. These results have guided this work to a better study of the therapeutic activity of HPA-05 in pain relief. The dose of 200 mg/Kg of HPA-05, through i.p., does not involve the participation of K+ATP receptors in its mechanisms of action, neither GABAA receptors, it is not exerted by the cholinergic pathway and also does not involve the glutamatergic pathway, since the treatment with the substance under study does not reduce the duration of paw licking at any phases in the formalin test. The pretreatment of the animals with L-arginine was capable of reversing the antinociceptive effect of HPA-05 in the first phase of the formalin test, which involves the dopamine D2 receptors in the second phase and the interaction of caffeine with HPA-05, showing a reversion of the antinociceptive effect of HPA-05 in the first phase of the formalin test. The results with HPA-05 were effective in inhibiting the latency of convulsions induced by pentylenetetrazol and by auricular electroshock, what indicates to show profile of anticonvulsant drugs in these tests. In the Elevated Plus Maze test, it has not been observed any behavioral modification indicating a possible anxiolytic effect. In the peritonitis induced by carrageenan, there was a reduction in the levels of leukocytes and neutrophils in the intraperitoneal cavity of the treated animals, demonstrating the anti-inflammatory activity of HPA-05. The results shown in this study have evidenced a promising effect of HPA-05 as an analgesic, anti-inflammatory and anticonvulsant agent.
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spelling 2015-05-14T12:59:57Z2018-07-21T00:25:08Z2014-09-112018-07-21T00:25:08Z2013-09-13MAIA, Ana Karina Holanda Leite. Preclinical Psychopharmacological studies of 3-phenyl-5-(4-methylphenyl) imidazolidine-2,4-dione (HPA-05) in mice. 2013. 112 f. Tese (Doutorado em Farmacologia) - Universidade Federal da Paraí­ba, João Pessoa, 2013.https://repositorio.ufpb.br/jspui/handle/tede/6803Heterocyclic compounds are found in many drugs with several therapeutic purposes, particularly in hydantoin derivatives. These derivatives, such as imidazolidine pharmaceuticals are employed as: anticonvulsants, cicatrizants, muscle relaxants, antimicrobials and antitumorals. Previous studies, using behavioral methodologies, have demonstrated that HPA-05 (3-phenyl-5-(4-methylphenyl) imidazolidine-2,4-dione) presented depressant actions on the CNS (Central Nervous System) with indications such as antinociceptives. These results have guided this work to a better study of the therapeutic activity of HPA-05 in pain relief. The dose of 200 mg/Kg of HPA-05, through i.p., does not involve the participation of K+ATP receptors in its mechanisms of action, neither GABAA receptors, it is not exerted by the cholinergic pathway and also does not involve the glutamatergic pathway, since the treatment with the substance under study does not reduce the duration of paw licking at any phases in the formalin test. The pretreatment of the animals with L-arginine was capable of reversing the antinociceptive effect of HPA-05 in the first phase of the formalin test, which involves the dopamine D2 receptors in the second phase and the interaction of caffeine with HPA-05, showing a reversion of the antinociceptive effect of HPA-05 in the first phase of the formalin test. The results with HPA-05 were effective in inhibiting the latency of convulsions induced by pentylenetetrazol and by auricular electroshock, what indicates to show profile of anticonvulsant drugs in these tests. In the Elevated Plus Maze test, it has not been observed any behavioral modification indicating a possible anxiolytic effect. In the peritonitis induced by carrageenan, there was a reduction in the levels of leukocytes and neutrophils in the intraperitoneal cavity of the treated animals, demonstrating the anti-inflammatory activity of HPA-05. The results shown in this study have evidenced a promising effect of HPA-05 as an analgesic, anti-inflammatory and anticonvulsant agent.Os compostos heterocíclicos são encontrados em muitos medicamentos com finalidades terapêuticas diversas, tendo destaque os derivados da hidantoína. Estes derivados, tais como os fármacos imidazolidínicos, são empregados como anticonvulsivantes, cicatrizantes, miorrelaxantes, antimicrobianos e antitumorais. Estudos anteriores, realizados por SALGADO, 2011, utilizando metodologias comportamentais, demonstraram que a HPA-05 (3-fenil-5-(4-metilfenil)-imidazolidin - 2,4 - diona) apresenta ações depressoras sobre o SNC (Sistema Nervoso Central) com indicações antinociceptivas. Estes resultados revelaram a necessidade de aprofundar o trabalho no sentido de que a atividade terapêutica para o alívio da dor da HPA - 05 fosse melhor estudada, além de complementar o estudo psicofarmacológico da mesma. A dose de 200 mg/Kg da HPA-05, via i.p., não envolve a participação dos receptores K+ATP no seu mecanismo de ação, nem receptores GABAA, não é exercida pela via colinérgica e também não envolve a via glutamatérgica, visto que o tratamento com a substância em estudo não reduz o tempo de lambida da pata em nenhuma das fases no teste da formalina. O pré-tratamento dos animais com L-arginina foi capaz de reverter o efeito antinociceptivo da HPA - 05 na primeira fase do teste da formalina, o qual envolve os receptores D2 da dopamina na segunda fase e a interação da cafeína com a HPA 05, mostrando uma reversão do efeito antinociceptivo da HPA - 05, na primeira fase do teste da formalina. Os resultados com a HPA-05 se mostraram efetivos em inibir a latência das convulsões induzidas pelo pentilenotetrazol e pelo eletrochoque auricular, o que indica apresentar perfil de drogas anticonvulsivantes. No teste do Labirinto em Cruz Elevado, não foi observado nenhuma modificação comportamental indicativa de um possível efeito ansiolítico. Na peritonite induzida pela carragenina, houve redução na quantidade de leucócitos e neutrófilos na cavidade intraperitoneal dos animais tratados, revelando a atividade anti-inflamatória da HPA - 05. Os resultados apresentados neste estudo evidenciaram um efeito promissor da HPA - 05 como substância analgésica, anti-inflamatória e anticonvulsivante.Made available in DSpace on 2015-05-14T12:59:57Z (GMT). No. of bitstreams: 1 arquivototal.pdf: 2175947 bytes, checksum: 976f66e936aee47ebff24e70dd90795d (MD5) Previous issue date: 2013-09-13Made available in DSpace on 2018-07-21T00:25:08Z (GMT). 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dc.title.por.fl_str_mv Estudos psicofarmacológicos pré clínicos do 3-fenil-5-(4-metilfenil)-imidazolidin-2,4-diona (hpa-05) em camundongos
dc.title.alternative.eng.fl_str_mv Preclinical Psychopharmacological studies of 3-phenyl-5-(4-methylphenyl) imidazolidine-2,4-dione (HPA-05) in mice
title Estudos psicofarmacológicos pré clínicos do 3-fenil-5-(4-metilfenil)-imidazolidin-2,4-diona (hpa-05) em camundongos
spellingShingle Estudos psicofarmacológicos pré clínicos do 3-fenil-5-(4-metilfenil)-imidazolidin-2,4-diona (hpa-05) em camundongos
Maia, Ana Karina Holanda Leite
Imidazolidínicos
Psicofármacos
Anticonvulsivante
Antinociceptivo
Anti-inflamatório
Imidazolidines
Psychopharmaceuticals
Anticonvulsant
Antinociceptive
Anti-inflammatory
CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
title_short Estudos psicofarmacológicos pré clínicos do 3-fenil-5-(4-metilfenil)-imidazolidin-2,4-diona (hpa-05) em camundongos
title_full Estudos psicofarmacológicos pré clínicos do 3-fenil-5-(4-metilfenil)-imidazolidin-2,4-diona (hpa-05) em camundongos
title_fullStr Estudos psicofarmacológicos pré clínicos do 3-fenil-5-(4-metilfenil)-imidazolidin-2,4-diona (hpa-05) em camundongos
title_full_unstemmed Estudos psicofarmacológicos pré clínicos do 3-fenil-5-(4-metilfenil)-imidazolidin-2,4-diona (hpa-05) em camundongos
title_sort Estudos psicofarmacológicos pré clínicos do 3-fenil-5-(4-metilfenil)-imidazolidin-2,4-diona (hpa-05) em camundongos
author Maia, Ana Karina Holanda Leite
author_facet Maia, Ana Karina Holanda Leite
author_role author
dc.contributor.advisor1.fl_str_mv Almeida, Reinaldo Nobrega de
dc.contributor.advisor1ID.fl_str_mv CPF:08693463420
dc.contributor.advisor1Lattes.fl_str_mv http://lattes.cnpq.br/5034028656386134
dc.contributor.advisor-co1.fl_str_mv Morais, Liana Clébia Soares Lima de
dc.contributor.advisor-co1ID.fl_str_mv CPF:71429433434
dc.contributor.advisor-co1Lattes.fl_str_mv http://lattes.cnpq.br/1764937418865472
dc.contributor.authorID.fl_str_mv CPF:03339501432
dc.contributor.authorLattes.fl_str_mv http://lattes.cnpq.br/4898646458744452
dc.contributor.author.fl_str_mv Maia, Ana Karina Holanda Leite
contributor_str_mv Almeida, Reinaldo Nobrega de
Morais, Liana Clébia Soares Lima de
dc.subject.por.fl_str_mv Imidazolidínicos
Psicofármacos
Anticonvulsivante
Antinociceptivo
Anti-inflamatório
topic Imidazolidínicos
Psicofármacos
Anticonvulsivante
Antinociceptivo
Anti-inflamatório
Imidazolidines
Psychopharmaceuticals
Anticonvulsant
Antinociceptive
Anti-inflammatory
CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
dc.subject.eng.fl_str_mv Imidazolidines
Psychopharmaceuticals
Anticonvulsant
Antinociceptive
Anti-inflammatory
dc.subject.cnpq.fl_str_mv CNPQ::CIENCIAS BIOLOGICAS::FARMACOLOGIA
description Heterocyclic compounds are found in many drugs with several therapeutic purposes, particularly in hydantoin derivatives. These derivatives, such as imidazolidine pharmaceuticals are employed as: anticonvulsants, cicatrizants, muscle relaxants, antimicrobials and antitumorals. Previous studies, using behavioral methodologies, have demonstrated that HPA-05 (3-phenyl-5-(4-methylphenyl) imidazolidine-2,4-dione) presented depressant actions on the CNS (Central Nervous System) with indications such as antinociceptives. These results have guided this work to a better study of the therapeutic activity of HPA-05 in pain relief. The dose of 200 mg/Kg of HPA-05, through i.p., does not involve the participation of K+ATP receptors in its mechanisms of action, neither GABAA receptors, it is not exerted by the cholinergic pathway and also does not involve the glutamatergic pathway, since the treatment with the substance under study does not reduce the duration of paw licking at any phases in the formalin test. The pretreatment of the animals with L-arginine was capable of reversing the antinociceptive effect of HPA-05 in the first phase of the formalin test, which involves the dopamine D2 receptors in the second phase and the interaction of caffeine with HPA-05, showing a reversion of the antinociceptive effect of HPA-05 in the first phase of the formalin test. The results with HPA-05 were effective in inhibiting the latency of convulsions induced by pentylenetetrazol and by auricular electroshock, what indicates to show profile of anticonvulsant drugs in these tests. In the Elevated Plus Maze test, it has not been observed any behavioral modification indicating a possible anxiolytic effect. In the peritonitis induced by carrageenan, there was a reduction in the levels of leukocytes and neutrophils in the intraperitoneal cavity of the treated animals, demonstrating the anti-inflammatory activity of HPA-05. The results shown in this study have evidenced a promising effect of HPA-05 as an analgesic, anti-inflammatory and anticonvulsant agent.
publishDate 2013
dc.date.issued.fl_str_mv 2013-09-13
dc.date.available.fl_str_mv 2014-09-11
2018-07-21T00:25:08Z
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2018-07-21T00:25:08Z
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dc.identifier.citation.fl_str_mv MAIA, Ana Karina Holanda Leite. Preclinical Psychopharmacological studies of 3-phenyl-5-(4-methylphenyl) imidazolidine-2,4-dione (HPA-05) in mice. 2013. 112 f. Tese (Doutorado em Farmacologia) - Universidade Federal da Paraí­ba, João Pessoa, 2013.
dc.identifier.uri.fl_str_mv https://repositorio.ufpb.br/jspui/handle/tede/6803
identifier_str_mv MAIA, Ana Karina Holanda Leite. Preclinical Psychopharmacological studies of 3-phenyl-5-(4-methylphenyl) imidazolidine-2,4-dione (HPA-05) in mice. 2013. 112 f. Tese (Doutorado em Farmacologia) - Universidade Federal da Paraí­ba, João Pessoa, 2013.
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