Enhanced antiopiate activity in peptidomimetics of FMRFamide containing Z-2,3-methanomethionine.
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FMRFa is a molluscan peptide that has shown antiopiate activity in a number of mammalian test systems. The current study determined the antiopiate potency of FMRFa and two conformationally constrained peptidomimetics of FMRFa containing stereoisomers of Z-2,3-methanomethionine. Morphine abstinence signs were observed after varying doses (0.25-25.0 micrograms) of these substances were injected into the third ventricle of morphine-dependent rats. Although both peptidomimetics were far more potent than FMRFa itself, they bound with lower affinity than FMRFa to rat spinal cord receptors for the mammalian FMRFa-like peptide, NPFF.
author list (cited authors)
Malin, D. H., Payza, K., Lake, J. R., Corriere, L. S., Benson, T. M., Smith, D. A., ... Burgess, K.
complete list of authors
Malin, DH||Payza, K||Lake, JR||Corriere, LS||Benson, TM||Smith, DA||Kelley, RS||Ho, KK||Burgess, K