RESUMO
FMRFamide is a molluscan peptide that has shown antiopiate activity in a number of mammalian test systems. The current study determined the antiopiate potency of FMRFamide and two conformationally constrained peptidomimetics of FMRFamide containing stereoisomers of (E)-2,3-methanomethionine. Morphine abstinence signs were observed after varying doses (0.25-25.0 microgram) of these substances were injected into the third ventricle of morphine-dependent rats. Both peptidomimetics were far more potent than FMRFamide itself. In addition, although both peptidomimetics bound with lower affinity than FMRFamide to rat spinal cord receptors for NPFF (the mammalian FMRFamide-like peptide), they were far more resistant than FMRFamide to enzymatic degradation by leucine aminopeptidase.
Assuntos
Leucil Aminopeptidase/metabolismo , Metionina/análogos & derivados , Antagonistas de Entorpecentes/farmacologia , Neuropeptídeos/farmacologia , Sequência de Aminoácidos , Animais , FMRFamida , Hidrólise , Masculino , Metionina/análise , Dados de Sequência Molecular , Neuropeptídeos/metabolismo , Oligopeptídeos/metabolismo , Ligação Proteica , Ratos , Ratos Sprague-Dawley , Receptores de Neuropeptídeos/metabolismo , Receptores Opioides/metabolismo , Estereoisomerismo , Síndrome de Abstinência a Substâncias/etiologiaRESUMO
A 40-year-old woman who ingested a 35% hydrogen peroxide solution presented to the emergency department with abdominal pain. Acute abdominal series showed gas in the portal vein system. The patient was admitted and treated conservatively. She was released after five days in the hospital with no major sequelae.
