PMID: 9160247May 1, 1997Paper

Met5-enkephalin-Arg6-Phe7, an endogenous neuropeptide, binds to multiple opioid and nonopioid sites in rat brain

Journal of Neuroscience Research
Sándor BenyheM Wollemann

Abstract

Receptor binding properties of the naturally occurring opioid heptapeptide MERF were studied in rat brain membrane preparations using tritium-labeled derivative of the peptide with 40 Ci/mmol specific radioactivity. Binding assays were performed in the presence of broad-spectrum peptidase inhibitors at 0 degree C. Under these conditions, the equilibrium binding was achieved in 30-40 min, and approximately 90% of the applied radioligand remained unchanged as determined by HPLC analysis. The apparent affinity (Kd value) of [3H]Met-enkephalin-Arg6-Phe7, calculated from saturation binding data, was 10.2 +/- 2.5 nM, and the maximal number (Bmax) of the heptapeptide binding sites was found to be 468 +/- 43 fmol/mg protein. About half the sites represent nonopioid sites because the Bmax was only 255 +/- 30 fmol/mg, when the nonspecific binding was measured with 1 microM naloxone. The rank order potencies of the examined compounds revealed that the opioid component of [3H]Met-enkephalin-Arg6-Phe7 recognition site are probably not mu and certainly not kappa 1 sites, whereas these sites are characterized by a kappa 2-like binding profile. Considering the discrepancies between rat and frog brain found in the affinity of some compounds, in...Continue Reading

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Citations

Aug 9, 2007·Brain Research Bulletin·Eniko IojaSándor Benyhe
Sep 24, 2004·Regulatory Peptides·Fanni TóthSándor Benyhe
May 12, 2004·Life Sciences·Mária Wollemann, Sándor Benyhe
Apr 12, 2016·Journal of Enzyme Inhibition and Medicinal Chemistry·Ludovica MontiEttore Novellino
Jun 2, 2015·Frontiers in Cellular Neuroscience·Daniil SarkisyanGeorgy Bakalkin
Oct 3, 2014·BioMed Research International·Katarzyna Popiolek-BarczykJoanna Mika
Aug 19, 2007·Neurochemistry International·Estera PáldyováSándor Benyhe
Jan 24, 2016·Chemical Biology & Drug Design·Annu MudgalSantosh Pasha
Jun 21, 2014·Comparative Biochemistry and Physiology. Part B, Biochemistry & Molecular Biology·Engin BojnikSandor Benyhe
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Nov 14, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Giulio PoliAzzurra Stefanucci
Oct 16, 2015·Anesthesia and Analgesia·Eszter SzlaviczEngin Bojnik
Mar 21, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ferenc ZádorMahmoud Al-Khrasani
Aug 8, 2020·The Journal of Pharmacology and Experimental Therapeutics·Takugi KanToshiyasu Suzuki
Aug 9, 2019·MedChemComm·Piotr F J LipińskiJoanna Sadlej
Apr 27, 2019·Frontiers in Pharmacology·Mihály BaloghMahmoud Al-Khrasani
Jan 2, 2021·Frontiers in Behavioral Neuroscience·Christopher Martínez-AguirreLuisa Rocha
Feb 1, 2002·European Journal of Pharmacology·Mariana SpeteaAndris Kreicbergs
May 22, 2002·European Journal of Pharmacology·Dauren BiyashevSándor Benyhe

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