Muscarinic receptor binding in rat brain using the agonist, [3H]cis methyldioxolane.
Muscarinic receptor binding in rat brain using the agonist, [3H]cis methyldioxolane.
复制标题
使用激动剂[3H]顺式甲基二氧戊环在大鼠脑中结合毒蕈碱受体。
DOI：
10.1016/0024-3205(80)90117-4
复制
发表时间：
1980
期刊：
影响因子：
6.1
通讯作者：
H. Yamamura
中科院分区：
文献类型：
--
作者：
F. Ehlert;Y. Dumont;W. Roeske;H. Yamamura
使用毒蕈碱激动剂[3 H]顺式甲基二氧戊环（[3 H]CD）在大鼠前脑制备物中测定毒蕈碱受体结合。使用0.5-64 nM [3 H]CD浓度的平衡结合研究结果表明，[3 H]CD结合在该浓度范围内未饱和，尽管结合等温线向下凹。结合数据的非线性回归分析显示，存在两个群体的毒蕈碱受体具有1.83和123 nM的解离常数和85和1320 fmol/mg蛋白质的结合能力，分别。竞争性抑制实验表明，[3 H]CD结合很容易被几种毒蕈碱激动剂和拮抗剂取代。[3 H]CD结合的立体特异性在竞争性抑制实验中使用的立体异构体的苯甲环丁烷和乙酰-β-甲基胆碱被证明。右乙替米特的效力是左乙替米特的10，000倍，l-乙酰-β-甲基胆碱的效力是d-乙酰-β-甲基胆碱的520倍。各种非毒蕈碱胆碱能药物在10 μM浓度下不能有效抑制[3 H]CD结合。
Muscarinic receptor binding was measured in rat forebrain preparations using the muscarinic agonist, [3H]cis methyldioxolane ([3H]CD). The results of equilibrium binding studies using [3H]CD concentrations between 0.5–64 nM showed that [3H]CD binding did not saturate in this concentration range, although the binding isotherm was concave downward. Nonlinear regression analysis of the binding data revealed the presence of two populations of muscarinic receptors having dissociation constants of 1.83 and 123 nM and binding capacities of 85 and 1320 fmol/mg protein, respectively. Competitive inhibition experiments showed that [3H]CD binding was readily displaced by several muscarinic agonists and antagonists. The stereospecificity of [3H]CD binding was demonstrated in competitive inhibition experiments using the stereoisomers of benzetimide and acetyl-β-methylcholine. Dexetimide was 10,000 times more potent than levetimide and l-acetyl-β-methylcholine was 520 times more potent than d-acetyl-β-methylcholine. A variety of nonmuscarinic cholinergic drugs were not effective at inhibiting [3H]CD binding at a concentration of 10 μM.