Abstract
The synthetic peptide octarphin (TPLVTLFK, fragment 12–19 of β-endorphin), a selective agonist of the nonopioid β-endorphin receptor, was labeled with tritium yielding specific activity of 28 Ci/mmol. The binding of [3H]octarphin to rat adrenal cortex membranes was studied under normal conditions as well as after cold and heat shocks. It was found that under normal conditions [3H]octarphin specifically binds to the membranes with high affinity: K d1 = 36.3 ± 2.5 nM, Bmax1 = 41.0 ± 3.8 pmol/mg protein. The specific binding of [3H]octarphin to the membranes was inhibited by unlabeled β-endorphin (K i = 33.9 ± 3.6 nM) and the agonist of the non-opioid receptor decapeptide immunorphin (K i = 36.8 ± 3.3 nM). Unlabeled naloxone, [Leu5]- and [Met5]enkephalins, α- and γ-endorphins, and corticotropin were inactive (K i > 1 μM). Both cold and heat shocks decreased the binding affinity: K d2 = 55.6 ± 4.2 nM and K d3 = 122.7 ± 5.6 nM, respectively. In both cases, the maximal binding capacity of the receptor did not change. Thus, even a short-term thermal shock significantly affects the sensitivity of the non-opioid β-endorphin receptor of adrenal cortex membranes.
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Original Russian Text © Y. N. Nekrasova, Y. A. Zolotarev, E. V. Navolotskaya, 2012, published in Biokhimiya, 2012, Vol. 77, No. 12, pp. 1693–1698.
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Nekrasova, Y.N., Zolotarev, Y.A. & Navolotskaya, E.V. Interaction of the synthetic peptide octarphin with rat adrenal cortex membranes. Biochemistry Moscow 77, 1377–1381 (2012). https://doi.org/10.1134/S000629791212005X
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DOI: https://doi.org/10.1134/S000629791212005X