Elucidation and Characteristics of Non-opioid β-Endorphin Receptors in Rat Adrenal Cortex.

Autor: Navolotskaya, E. V., Kovalitskaya, Yu. A., Zolotarev, Yu. A., Kudryashova, N. Yu., Goncharenko, E. N., Kolobov, A. A., Kampe-Nemm, E. A., Malkova, N. V., Yurovsky, V. V., Lipkin, V. M.
Předmět:
Zdroj: Biochemistry (00062979); Aug2004, Vol. 69 Issue 8, p870-875, 6p
Abstrakt: β-Endorphin-like decapeptide immunorphin (SLTCLVKGFY), a selective agonist of non-opioid β-endorphin receptor, was labeled with tritium to specific activity of 24 Ci/mmol. It was used for the detection and characterization of nonopioid β-endorphin receptors on rat adrenal cortex membranes (Kd1 = 39.6 ± 2.0 nM, Bmax1 = 40.7 ± 2.3 pmol/mg protein; Kd2 = 0.25 ± 0.01 μM, Bmax2 = 187.8 ± 9.4 pmol/mg protein). β-Endorphin was found to inhibit the [3H]immunorphin specific binding to membranes (Ki = 70.0 ± 9.2 nM); naloxone, [Met5]enkephalin, and α- and γ-endorphins tested in parallel were inactive. Immunorphin at concentrations of 10–9-10–6 M was found to inhibit the adenylate cyclase activity in adrenocortical membranes, while intramuscular injection of immunorphin at doses of 10-100 μg/kg was found to reduce the secretion of 11-oxycorticosteroids from the adrenals to the bloodstream. [ABSTRACT FROM AUTHOR]
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