Eckelman W C, Grissom M, Conklin J, Rzeszotarski W J, Gibson R E, Francis B E, Jagoda E M, Eng R, Reba R C
J Pharm Sci. 1984 Apr;73(4):529-34. doi: 10.1002/jps.2600730424.
Among ligands that bind to the alpha- and beta-adrenoceptors and to the muscarinic acetylcholine receptor (m-AChR), those that bind to the latter have the best properties for external detection of receptor sites by gamma-camera imaging. To develop the optimal radiotracer, nonradioactive analogues of 3-quinuclidinyl benzilate (I) were tested in in vivo displacement studies with (-)-[3H]I to determine their ability to compete with (-)-[3H]I for the muscarinic acetylcholine receptor. There is a linear correlation between the ability to compete with (-)-[3H]I for the m-AChR and the affinity constant of the analogue as determined by in vitro assay, suggesting that the test is a valid indicator of in vivo distribution. One radioiodinated analogue, 3-quinuclidinyl p- iodobenzilate , bound to m-AChR in the heart and brain of rats.
在与α-和β-肾上腺素能受体以及毒蕈碱型乙酰胆碱受体（m-AChR）结合的配体中，那些与后者结合的配体在通过γ相机成像对受体位点进行外部检测方面具有最佳特性。为了开发最佳放射性示踪剂，在与（-）-[³H]碘的体内置换研究中测试了3-奎宁环基苯甲酸酯（I）的非放射性类似物，以确定它们与（-）-[³H]碘竞争毒蕈碱型乙酰胆碱受体的能力。与（-）-[³H]碘竞争m-AChR的能力与通过体外测定确定的类似物的亲和常数之间存在线性相关性，这表明该测试是体内分布的有效指标。一种放射性碘化类似物，3-奎宁环基对碘苯甲酸酯，在大鼠的心脏和大脑中与m-AChR结合。
