Panchenko L F, Aliab'eva T N, Malinovskaia V V, Balashov A M
Biull Eksp Biol Med. 1987 Jul;104(7):87-9.
The preferential interactions of alpha-interferon (alpha-IFN) with delta and mu opiate receptors were studied. alpha-IFN (specific antiviral activity 2 X 10(3) U/mg protein) was shown to inhibit in the competitive manner 3H-naloxone and 3H-D-ala2, D-leu5-enkephalin (3H-DADL) specific binding to opiate receptor subpopulations. alpha-IFN was much more effective in decreasing 3H-DADL than 3H-naloxone binding in opiate receptors: K1 values averaged 160 +/- 30 and 1150 +/- 80 U/ml, respectively. IFN effective concentrations inhibiting 50% of 3H-naloxone opiate receptor binding in the absence or presence of 100 mmol/l NaCl were similar, and the "sodium shift" value was equal to 1. The independence of alpha-IFN activity of the presence of NA+ cations suggests the antagonist character of alpha-IFN interaction with opiate receptors. Thus, alpha-IFN employed appears to be an alpha-selective ligand displaying the in vitro properties of "pure" morphine antagonists.
研究了α-干扰素(α-IFN)与δ和μ阿片受体的优先相互作用。α-干扰素(比活性为2×10³U/mg蛋白质)以竞争性方式抑制³H-纳洛酮和³H-D-丙氨酸²、D-亮氨酸⁵-脑啡肽(³H-DADL)与阿片受体亚群的特异性结合。在阿片受体中,α-干扰素降低³H-DADL结合的效果比降低³H-纳洛酮结合的效果更显著:K1值分别平均为160±30和1150±80 U/ml。在不存在或存在100 mmol/l氯化钠的情况下,抑制50%³H-纳洛酮阿片受体结合的干扰素有效浓度相似,“钠移位”值等于1。α-干扰素活性不依赖于钠离子的存在,这表明α-干扰素与阿片受体相互作用具有拮抗剂特性。因此,所使用的α-干扰素似乎是一种α选择性配体,具有体外“纯”吗啡拮抗剂的特性。