Adem A, Nordberg A, Slanina P
Life Sci. 1986 Apr 14;38(15):1359-68. doi: 10.1016/0024-3205(86)90468-6.
Human blood lymphocytes from normal blood donors exhibited specific binding of the muscarinic antagonist 3H-quinuclidinyl benzilate (3H-QNB). The 3H-QNB binding to intact viable lymphocytes as well as to lysed lymphocyte membranes "P2" was saturable and displaceable by both muscarinic agonists and antagonists. For the lysed lymphocyte membranes "P2" a single binding site with a Bmax of 109 pmol/g protein and a Kd of 15 nM was obtained. Intact viable lymphocytes also showed one binding site with a Kd of 24 nM and a Bmax of 1556 pmol/g protein. The higher Bmax value might be explained in terms of uptake of the ligand when using intact cells or through loss of binding sites when using lysed lymphocyte membranes "P2". IC50 values were lower by a factor of 10(2) for atropine and scopolamine and by 10(4) for pirenzepine when lysed lymphocyte membranes "P2" were used instead of intact viable lymphocytes.
来自正常献血者的人血淋巴细胞表现出对毒蕈碱拮抗剂3H-喹核醇基苯甲酸酯(3H-QNB)的特异性结合。3H-QNB与完整活淋巴细胞以及裂解的淋巴细胞膜“P2”的结合是可饱和的,并且可被毒蕈碱激动剂和拮抗剂置换。对于裂解的淋巴细胞膜“P2”,获得了一个单一结合位点,其Bmax为109 pmol/g蛋白质,Kd为15 nM。完整活淋巴细胞也显示出一个结合位点,其Kd为24 nM,Bmax为1556 pmol/g蛋白质。当使用完整细胞时,较高的Bmax值可能用配体摄取来解释,或者当使用裂解的淋巴细胞膜“P2”时,用结合位点的丧失来解释。当使用裂解的淋巴细胞膜“P2”而不是完整活淋巴细胞时,阿托品和东莨菪碱的IC50值低10(2)倍,哌仑西平的IC50值低10(4)倍。