title: [Octarphin--Nonopioid Peptide of the Opioid Origin].
abstract: The data on the properties and mechanism of action of the peptide octarphin (TPLVTLFK, the fragment 12-19 of β-endorphin)--a selective agonist of nonopioid (insensitive to the action of the opioid antagonist naloxone) β-endorphin receptor found on n immune cells (peritoneal macrophages, T and B lymphocytes of spleen and blood), endocrine (adrenal cortex, hypothalamus), cardiovascular (cardiomyocytes) systems are analyzed and systematized. Binding to the receptor octarphin increases increases the mitogen-induced pro- liferation of human and mouse T and B lymphocytes in vitro, activates murine peritoneal macrophages in vitro and in vivo, stimulates growth of human T-lymphoblast cell lines Jurkat and MT-4, inhibits adenylate cyclase activity of rat adrenal cortex membranes and suppresses the secretion of glucocorticoids from the adrenal gland into the blood. It was shown that in a concentration range of 1-1000 nM the peptide increases the activity of inducible NO-synthase (iNOS), and the content of NO and cGMP in lipopolysaccharide-activated murine peritoneal macrophages. Taking into account that NO acts as a primary activator of soluble guanylate cyclase (sGC), it can be assumed that the activating effect of octarphin on macrophages is realized in the following way: increase in th iNOS expression --> increase in the NO production --> increase in the sGC activity --> increase in intracellular levels of cGMP.
authors.forename: E V
authors.initials: EV
authors.lastname: Navolotskaya
mesh_terms: D000818:Animals; D006801:Humans; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D009569:Nitric Oxide / Q000378:metabolism; D009842:Oligopeptides / Q000378:metabolism* / Q000494:pharmacology*; D011485:Protein Binding; D011957:Receptors, Opioid / Q000819:agonists*; D001615:beta-Endorphin / Q000378:metabolism*
chemical_list: D009842:Oligopeptides; D011957:Receptors, Opioid; C555005:octarphin; D009569:Nitric Oxide; D001615:beta-Endorphin