Navolotskaia E V, Vanina V I, Zargarova T A, Goncharenko E N, Kudriashova N Iu, Akhalaia M Ia, Sadovnikov V B, Semushkina S G, Kolobov A A, Kampe-Nemm E A, Iurovskiĭ V V, Lipkin V M
Bioorg Khim. 2004 Jul-Aug;30(4):350-5.
The effect of immunocortin, an ACTH-like decapeptide VKKPGSSVKV corresponding to the 11-20 sequence of the variable part of the human IgG1 heavy chain on the content of 11-hydroxycorticosteroids (CS) in rat adrenal glands and blood serum in vivo was studied. An intramuscular injection of immunocortin at a dose of 10 microg/kg was found in an hour to induce a twofold decrease in CS content in the adrenal glands and a 1.8-fold increase in the blood serum CS content. At the same time, an immunocortin dose of 100 microg/kg exerted practically no effect on the CS content and its dose of 1000 microg/kg increased the CS content both in adrenal glands and in blood serum by 1.6 and 2.2 times, respectively. Four hours after the injection of any of the three doses of immunocortin, the CS content in adrenal glands did not differ from the control value, and after 24 h the content decreased threefold. Immunocortin was shown to be bound by the ACTH receptors in the membranes of the rat adrenal cortex with a high affinity and specificity (inhibiting the specific binding of 125I-labeled ACTH-(11-24) peptide with Ki of 1.2 nM).
研究了免疫皮质素（一种与人类IgG1重链可变部分11 - 20序列相对应的ACTH样十肽VKKPGSSVKV）对大鼠肾上腺和血清中11 - 羟基皮质类固醇（CS）含量的体内影响。发现以10微克/千克的剂量肌肉注射免疫皮质素1小时后，肾上腺中CS含量降低两倍，血清中CS含量增加1.8倍。同时，100微克/千克的免疫皮质素剂量对CS含量几乎没有影响，而1000微克/千克的剂量使肾上腺和血清中的CS含量分别增加1.6倍和2.2倍。注射三种剂量的免疫皮质素中的任何一种4小时后，肾上腺中的CS含量与对照值无差异，24小时后含量降低三倍。结果表明，免疫皮质素与大鼠肾上腺皮质膜中的ACTH受体具有高亲和力和特异性结合（抑制125I标记的ACTH - (11 - 24)肽的特异性结合，Ki为1.2纳摩尔）。
