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Eur J Med Chem ; 62: 122-9, 2013 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-23353749

RESUMO

The synthesis and the effect of a novel MIF-1 analogue on nociception during acute pain in rat model are reported. The synthesis of this enantiopure trifluoromethyl group containing tripeptide was performed through a peptide coupling reaction between the HCl. Leu-Gly-NH2 and the (S)-α-Tfm-proline. The analgesic effect of the CF3-(MIF-1) 2 has been evaluated in vivo on rat model by paw pressure (PP) and hot plate (HP) tests and compared to the native peptide MIF-1. Highest analgesic effect was observed with CF3-(MIF-1) 2 only in PP test. In order to study the mechanisms of nociception induced by the studied peptides, the involvement of the opioid and the nitric oxideergic systems was investigated. The results are in favor of a participation of both system since pretreatment, 20 min before injection of the CF3-(MIF-1) 2, with the non-competitive antagonist of opiate receptors naloxone, the nitric oxide synthase (NOS) inhibitor l-N(G)-nitroarginine ester (l-NAME) or the nitric oxide (NO) donor l-arginine (l-Arg) significantly decreased the pain perception in PP and HP tests.


Assuntos
Dor Aguda/tratamento farmacológico , Hormônio Inibidor da Liberação de MSH/farmacologia , Antagonistas de Entorpecentes/farmacologia , Nociceptividade/efeitos dos fármacos , Oligopeptídeos/química , Animais , Modelos Animais de Doenças , Hormônio Inibidor da Liberação de MSH/análogos & derivados , Hormônio Inibidor da Liberação de MSH/síntese química , Masculino , Conformação Molecular , Estrutura Molecular , Antagonistas de Entorpecentes/síntese química , Antagonistas de Entorpecentes/química , Ratos , Ratos Wistar
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