[Mediated participation of the opioid system in regulation of pain sensitivity by peptide fragments MP1 and MP2].
The naloxone-dependent modulating effect of synthetic analogs of myelopeptides, MP1 and MP2, on pain sensitivity in mice was determined at doses 10(-13) and 10(-8) g/animal. Binding of the peptides to opioid receptors of mouse brain membranes was studied by the radioligand assay. For MP1, the displacement of [3H]DAGO (selective mu-agonist) by IC50 = 7.3 x 10(-5) M and [3H]DSLET (selective delta-agonist) with IC50 = 7.0 x 10(-5) M. The data obtained suggest that the hypoalgesic effect of the peptides cannot be due to their direct interaction with opioid receptors. However, the naloxone dependence provides a possibility of mediated involvement of the opioidergic system in the realization of this effect.
Maliukova
I V
IV
Zakharova
L A
LA
Metaksa
E E
EE
D000595:Amino Acid Sequence; D000700:Analgesics / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D004745:Enkephalins / Q000378:metabolism / Q000494:pharmacology; D051379:Mice; D008810:Mice, Inbred C57BL; D008808:Mice, Inbred CBA; D008969:Molecular Sequence Data; D009842:Oligopeptides; D017288:Pain Threshold / Q000187:drug effects*; D010455:Peptides / Q000378:metabolism / Q000494:pharmacology*; D011869:Radioligand Assay; D017465:Receptors, Opioid, delta / Q000187:drug effects* / Q000378:metabolism; D017450:Receptors, Opioid, mu / Q000187:drug effects* / Q000378:metabolism
D000700:Analgesics; D004745:Enkephalins; D009842:Oligopeptides; D010455:Peptides; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu; D020875:Enkephalin, Ala(2)-MePhe(4)-Gly(5)-; C048617:myelopeptides; D004743:Enkephalin, Leucine; C034318:enkephalin, Ser(2), Leu(5), Thr(6)-
Oposredovannoe uchastie opioidnoĭ sistemy v reguliatsii bolevoĭ chuvstvitel'nosti peptidnymi fragmentami MP1 i MP2.