Barron B A, Murrin L C, Hexum T D
Eur J Pharmacol. 1986 Mar 18;122(2):269-73. doi: 10.1016/0014-2999(86)90112-3.
The presence of muscarinic binding sites in the bovine adrenal medulla was investigated using [3H]QNB and the bovine adrenal medulla. Scatchard analysis combined with computer analysis yielded data consistent with a two binding site configuration. KDs of 0.15 and 14 nM and Bmax s of 29 and 210 fmol/mg protein, respectively, were observed. Displacement of [3H]QNB by various cholinergic agents is, in order of decreasing potency: QNB, dexetimide, atropine, scopolamine, imipramine, desipramine, oxotremorine, pilocarpine, acetylcholine, methacholine and carbachol. These results demonstrate the presence of more than one muscarine binding site in the bovine adrenal gland.
利用[3H]QNB和牛肾上腺髓质研究了牛肾上腺髓质中毒蕈碱结合位点的存在情况。Scatchard分析结合计算机分析得出的数据与双结合位点构型一致。分别观察到解离常数(KD)为0.15和14 nM,最大结合量(Bmax)为29和210 fmol/mg蛋白质。各种胆碱能药物对[3H]QNB的置换能力由强到弱依次为:QNB、右旋苯乙呱酯、阿托品、东莨菪碱、丙咪嗪、地昔帕明、氧化震颤素、毛果芸香碱、乙酰胆碱、醋甲胆碱和卡巴胆碱。这些结果表明牛肾上腺中存在不止一个毒蕈碱结合位点。