Characterization of [3H]morphine binding to interleukin-1-activated thymocytes.
Characterization of [3H]morphine binding to interleukin-1-activated thymocytes.
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发表时间：
1992-11
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通讯作者：
S. Roy;B. Ge;H. Loh;N. Lee
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作者：
S. Roy;B. Ge;H. Loh;N. Lee
我们以前曾报道，白介素1诱导的胸腺细胞增殖伴随着这些细胞上出现[~3H]吗啡结合部位。在本研究中，我们对这些结合位点进行了表征。它们与大脑中经典的阿片受体在几个方面不同，包括：1)缺乏立体选择性；2)相对低亲和力(Kd=50 nM)和高容量(Bmax=3pmol/mg蛋白质)；3)结合被钙、镁、锰和氯离子强烈抑制；4)结合被蛋白酶K或E和磷脂酶A2抑制，但不被胸腺细胞膜的胰酶处理所抑制。主要在T细胞的CD4+亚群上发现的结合部位也显示出对阿片生物碱的偏好而不是多肽。这些[~3H]吗啡结合部位可能在体内对白细胞介素1诱导的胸腺细胞增殖起负反馈作用。
We have previously reported that interleukin-1-induced proliferation of thymocytes is accompanied by the appearance of [3H]morphine binding sites on these cells. In the present study, we have characterized these binding sites. They differ from classical opioid receptors in the brain in several ways, including: 1) lack of stereoselectivity; 2) relatively low affinity (Kd = 50 nM) and high capacity (Bmax = 3 pmol/mg of protein); 3) binding is strongly inhibited by Ca++, Mg++, Mn++ and Cl- ions and 4) binding is inhibited by proteinase K or E and by phospholipase A2 but not trypsin treatment of thymocyte membranes. The binding sites, which were found largely on the CD4+ subset of T-cells, also showed a preference for opioid alkaloids over peptides. These [3H]morphine binding sites may mediate a negative feedback effect on interleukin-1-induced proliferation of thymocytes in vivo.