Peptide E and other proenkephalin-derived peptides are potent kappa opiate receptor agonists.
Various proenkephalin-derived peptides such as peptide E and the bovine adrenal medulla peptides BAM-12P and BAM-22P are potent competitors on mu and kappa binding sites in guinea pig brain sections. Moreover, they are all potent agonists in the rabbit vas deferens, a specific kappa opiate receptor bioassay. As described before, dynorphin and some of its fragments are also potent kappa agonists. Our results suggest that not only prodynorphin-derived peptides could act as endogenous kappa ligands but also some proenkephalin-derived peptides such as peptide E.
D000313:Adrenal Medulla; D000818:Animals; D001681:Biological Assay; D001921:Brain / Q000378:metabolism*; D004744:Enkephalin, Methionine / Q000031:analogs & derivatives / Q000494:pharmacology; D004745:Enkephalins / Q000494:pharmacology*; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D007700:Kinetics; D008297:Male; D051379:Mice; D009119:Muscle Contraction / Q000187:drug effects; D010455:Peptides / Q000494:pharmacology*; D011498:Protein Precursors / Q000494:pharmacology; D011957:Receptors, Opioid / Q000187:drug effects / Q000378:metabolism*; D017473:Receptors, Opioid, kappa; D013329:Structure-Activity Relationship; D014649:Vas Deferens / Q000187:drug effects
D004745:Enkephalins; D010455:Peptides; D011498:Protein Precursors; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; D004744:Enkephalin, Methionine; C026771:BAM 12P; C028837:BAM 22P; C039933:peptide E (adrenal medulla)