合成肽章鱼肽（TPLVTLFK）通过非阿片类β-内啡肽受体抑制下丘脑-垂体-肾上腺轴的活性。

Synthetic peptide octarphin (TPLVTLFK) inhibits the activity of the hypothalamus-pituitary-adrenal axis through nonopioid β-endorphin receptor.

作者信息

Nekrasova Yuliia N, Zolotarev Yury A, Navolotskaya Elena V

机构信息

Branch of Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry of the Russian Academy of Sciences, Science Avenue, 6, Pushchino, Moscow Region 142290, Russia.

Institute of Molecular Genetics of the Russian Academy of Sciences, Kurchatov Square, 2, Moscow 123182, Russia.

出版信息

Regul Pept. 2013 May 10;183:23-6. doi: 10.1016/j.regpep.2013.03.002. Epub 2013 Mar 13.

DOI:10.1016/j.regpep.2013.03.002

PMID:23499809

Abstract

The synthetic peptide octarphin (TPLVTLFK) corresponding to the sequence 12-19 of β-endorphin, a selective agonist of nonopioid β-endorphin receptor, was labeled with tritium to specific activity of 29 Ci/mmol. The analysis of [(3)H]octarphin binding to rat pituitary and adrenal cortex membranes revealed the existence of one type of binding sites (receptors): Kd 5.9 and 35.6 nM, respectively. Octarphin at concentrations of 1-1000 nМ was shown to inhibit the adenylate cyclase activity of rat adrenocortical membranes, while its intramuscular injection at doses of 10-100 μg/kg was found to reduce the secretion of corticosterone from the adrenals to the bloodstream. Thus, the nonopioid receptor of β-endorphin may be involved in the regulation of the activity of the pituitary and adrenal glands.

摘要

与β-内啡肽第12 - 19位序列对应的合成肽octarphin（TPLVTLFK），即非阿片类β-内啡肽受体的选择性激动剂，用氚标记至比活度为29 Ci/mmol。对[(3)H]octarphin与大鼠垂体和肾上腺皮质膜结合的分析揭示存在一种结合位点（受体）：解离常数（Kd）分别为5.9和35.6 nM。结果表明，浓度为1 - 1000 nM的octarphin可抑制大鼠肾上腺皮质膜的腺苷酸环化酶活性，而肌肉注射剂量为10 - 100 μg/kg的octarphin可减少肾上腺皮质酮向血液中的分泌。因此，β-内啡肽的非阿片类受体可能参与垂体和肾上腺活动的调节。