Computer-assisted determination of benzodiazepine receptor heterogeneity.
Computer-assisted determination of benzodiazepine receptor heterogeneity.
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计算机辅助测定苯二氮卓受体异质性。
DOI：
10.1016/0014-2999(84)90242-5
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发表时间：
1984
影响因子：
5
通讯作者：
Loew,G
中科院分区：
文献类型：
--
作者：
Toll,L;Keys,C;Spangler,D;Loew,G
在0°C下，使用计算机化的加权非线性最小二乘回归分析，研究了全大鼠脑细胞膜上苯二氮卓类受体异质性的存在。同时分析了[3 H]氟硝西泮和[3 H]β-咔啉乙酯自身和交叉竞争研究的数据，以及各种已知和新型苯二氮卓受体配体对两种标记配体的抑制数据。最佳拟合数据的结合模型表明存在至少两个独立的结合位点。苯二氮卓类药物氟硝西泮和2′-Cl-地西泮在两个位点的亲和力略有差异。β-咔啉和Cl 218，872的亲和力差异较大，在苯二氮卓类的低亲和力位点具有较高的亲和力。类似的实验可能有助于确定GABA对苯二氮卓类受体亲和力的影响。
The presence of benzodiazepine receptor heterogeneity was investigated on whole rat brain membranes, at 0°C, using computerized, weighted nonlinear least-squares regression analysis. Data from [3H]flunitrazepam and [3H]β-carboline ethyl ester self and cross-competition studies were analyzed simultaneously with data from the inhibition of both labeled ligands by various known and novel benzodiazepine receptor ligands. The binding model which best fits the data indicated the presence of at least two independent binding sites. The benzodiazepines flunitrazepam and 2′-Cl-diazepam showed a small difference in affinity at the two sites. The β-carbolines and Cl 218,872 showed a larger difference in affinity, and had higher affinities at the lower affinity site for the benzodiazepines. Analogous experiments could be useful in the determination of the effect of GABA on benzodiazepine receptor affinities.