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| Content Provider | Springer Nature Link |
|---|---|
| Author | Nekrasova, Yu. N. Navolotskaya, E. V. |
| Copyright Year | 2012 |
| Abstract | The peptide TPLVTLFK (coined by the authors “octarphin”), corresponding to the amino acid sequence of β-endorphin fragment 12–19, and its analogs (LPLVTLFK, TLLVTLFK, TPLVLLFK, TPLVTLLK, TPLVTLFL) were synthesized. The peptide octarphin was labeled with tritium (specific activity, 28 Ci/mol) and its binding to the rat brain cortex membranes and mouse peritoneal macrophages was studied. [$^{3}$H]Octarphin was found to bind to brain membranes and macrophages with high affinity (K $_{d}$ = 2.6 ±0.2 and 2.3 +0.2 nM, respectively) and specificity. The specific binding of [$^{3}$H]octarphin with rat brain membranes and mouse macrophages was inhibited by unlabeled β-endorphin (K $_{i}$ = 2.4 +0.2 and 2.7 +0.2 nM, respectively) and selective agonist of nonopioid β-endorphin receptor synthetic peptide immunorphin (SLTCLVKGFY) (K $_{i}$ = 2.9 +0.2 and 2.4 +0.2 nM, respectively) and was not inhibited by unlabeled naloxone, α-endorphin, γ-endorphin and [Met$^{5}$]enkephalin (K $_{i}$ > 10 mM). Inhibiting activity of unlabeled analogs of octarphin was more than 100 times lower than that of the unlabeled octarphin. Octarphin was shown to stimulate activity of mouse immunocompetent cells in vitro: at the concentration of 1 nM it enhanced the capacity of peritoneal macrophages to digest bacteria Salmonella typhimurium virulent strain 415 in vitro. Thus, octarphin is a selective agonist of nonopioid (insensitive to the opioid antagonist naloxone) β-endorphin receptor of rat brain cortex membranes and mouse peritoneal macrophages. |
| Starting Page | 82 |
| Ending Page | 91 |
| Page Count | 10 |
| File Format | |
| ISSN | 19907478 |
| Journal | Biochemistry (Moscow) Supplement Series A: Membrane and Cell Biology |
| Volume Number | 6 |
| Issue Number | 1 |
| e-ISSN | 19907494 |
| Language | English |
| Publisher | SP MAIK Nauka/Interperiodica |
| Publisher Date | 2012-02-25 |
| Publisher Place | Dordrecht |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | β-endorphin naloxone peptides receptors brain immune system Cell Biology |
| Content Type | Text |
| Resource Type | Article |
| Subject | Cell Biology Biochemistry Biophysics |
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