Enhanced antiopiate activity and enzyme resistance in peptidomimetics of FMRFamide containing (E)-2,3-methanomethionine. Academic Article

abstract

• 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.

authors

• Burgess, Kevin

published proceedings

• Peptides

author list (cited authors)

• Malin, D. H., Lake, J. R., Payza, K., Corriere, L. S., Benson, T. M., Garber, T. L., ... Smith, D. A.

citation count

• 26

complete list of authors

• Malin, DH||Lake, JR||Payza, K||Corriere, LS||Benson, TM||Garber, TL||Waller, ML||Luu, TA||Kelley, RS||Smith, DA

publication date

• July 1993

publisher

• Elsevier  Publisher

published in

• Peptides  Journal

keywords

• Amino Acid Sequence
• Animals
• Fmrfamide
• Hydrolysis
• Leucyl Aminopeptidase
• Male
• Methionine
• Molecular Sequence Data
• Narcotic Antagonists
• Neuropeptides
• Oligopeptides
• Protein Binding
• Rats
• Rats, Sprague-Dawley
• Receptors, Neuropeptide
• Receptors, Opioid
• Stereoisomerism
• Substance Withdrawal Syndrome

PubMed Central ID

• 8234017

Digital Object Identifier (DOI)

• 10.1016/0196-9781(93)90105-p

start page

• 731

end page

• 734

volume

• 14

issue

• 4

URL

• http://dx.doi.org/10.1016/0196-9781(93)90105-p