Estudos psicofarmacológicos pré clínicos do 3-fenil-5-(4-metilfenil)-imidazolidin-2,4-diona (hpa-05) em camundongos
| Ano de defesa: | 2013 |
|---|---|
| Autor(a) principal: | |
| Orientador(a): | |
| Banca de defesa: | |
| 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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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 |
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CPF:08693463420 |
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http://lattes.cnpq.br/5034028656386134 |
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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 |
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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. |
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2013 |
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2013-09-13 |
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2014-09-11 2018-07-21T00:25:08Z |
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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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https://repositorio.ufpb.br/jspui/handle/tede/6803 |
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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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