title: Interaction of synthetic peptide octarphin with rat myocardium membranes.
abstract: A selective agonist of non-opioid β-endorphin receptor synthetic peptide octarphin (TPLVTLFK, specific activity 28 Ci/mmol) was prepared. The [3H]octarphin binding to rat myocardium membranes before and after experimental myocardial infarction (EMI) was studied. It was found that [3H]octarphin with high affinity and specificity binds to non-opioid β-endorphin receptor of rat myocardium membranes before EMI: K(d1) value of the [3H]octarphin specific binding to membranes was 1.8 ± 0.2 nM. In 3 h after EMI a sharp lowering in affinity of the binding is observed (K(d2) = 13.3 ± 0.4 nM), and in 48 h its almost complete restoration (K(d4) = 2.2 ± 0.3 nM). The results indicate participation of non-opioid β-endorphin receptor in the regulation of myocardial activity.
authors.affiliation: Branch of Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, pr. Nauki 6, 142290 Pushchino, Moscow Region, Russia.
authors.forename: Y N
authors.initials: YN
authors.lastname: Nekrasova
authors.forename: Y A
authors.initials: YA
authors.lastname: Zolotarev
authors.forename: E V
authors.initials: EV
authors.lastname: Navolotskaya
mesh_terms: D000818:Animals; D002462:Cell Membrane / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D007700:Kinetics; D008297:Male; D009203:Myocardial Infarction / Q000378:metabolism*; D009206:Myocardium / Q000737:chemistry / Q000378:metabolism*; D009842:Oligopeptides / Q000737:chemistry / Q000378:metabolism*; D011485:Protein Binding; D051381:Rats; D017207:Rats, Sprague-Dawley; D011957:Receptors, Opioid / Q000819:agonists / Q000737:chemistry / Q000378:metabolism
chemical_list: D009842:Oligopeptides; D011957:Receptors, Opioid; C555005:octarphin