Enhanced antiopiate activity in peptidomimetics of FMRFamide containing Z-2,3-methanomethionine Academic Article uri icon

abstract

  • 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.

citation count

  • 24

publication date

  • January 1993