[Binding of beta-endorphin and its fragments to the non-opiod receptor of murine peritoneal macrophages].
The tritium-labeled selective agonist of the nonopioid beta-endorphin receptor the decapeptide immunorphin ([3H]SLTCLVKGFY) with a specific activity of 24 Ci/mmol was prepared. It was shown that [3H]immunorphin binds with a high affinity to the non-opioid beta-endorphin receptor of mouse peritoneal macrophages (Kd 2.4 +/- 0.1 nM). The specific binding of [3H]immunorphin to macrophages was inhibited by unlabeled beta-endorphin (Ki of the [3H]immunorphin-receptor complex 2.9 +/- 0.2 nM) and was not inhibited by unlabeled naloxone, alpha-endorphin, gamma-endorphin, and [Met5]enkephalin (Ki > 10 microM). Thirty fragments of beta-endorphin were synthesized, and their ability to inhibit the specific binding of [3H]immunorphin to macrophages was studied. It was found that the shortest peptide having practically the same inhibitory activity as beta-endorphin is its fragment 12-19 (Ki 3.1 +/- 0.3 nM).
Kovalitskaia
Iu A
IuA
Sadovnikov
V B
VB
Kolobov
A A
AA
Zolotarev
Iu A
IuA
Iurovskií
V V
VV
Lipkin
V M
VM
Navolotskaia
E V
EV
D000818:Animals; D006801:Humans; D017737:Macrophages, Peritoneal / Q000378:metabolism*; D051379:Mice; D008807:Mice, Inbred BALB C; D009270:Naloxone / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000494:pharmacology; D018377:Neurotransmitter Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology*; D011485:Protein Binding; D011957:Receptors, Opioid / Q000819:agonists* / Q000378:metabolism; D001615:beta-Endorphin / Q000138:chemical synthesis / Q000494:pharmacology*
D009292:Narcotic Antagonists; D018377:Neurotransmitter Agents; D009842:Oligopeptides; D011957:Receptors, Opioid; D009270:Naloxone; D001615:beta-Endorphin