III. Conformational shifts at the benzodiazepine receptor related to the binding of agonists antagonists and inverse agonists
III. Conformational shifts at the benzodiazepine receptor related to the binding of agonists antagonists and inverse agonists
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DOI：
10.1016/0024-3205(86)90318-8
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发表时间：
1986
期刊：
影响因子：
6.1
通讯作者：
A. Walser
中科院分区：
文献类型：
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作者：
R. Fryer;C. Cook;N. W. Gilman;A. Walser
1948 Conformational Shifts at the BZR Vol. 39，No. 21，1986体外研究表明，BZ激动剂可增强GABA与其受体的结合，反向激动剂可抑制GABA结合，而拮抗剂可逆转这两种作用，但对GABA结合无影响（2）。相反的作用，即在存在或不存在GABA的情况下配体与BZR的结合，遵循相同的模式。激动剂的亲和力被GABA增强，反向激动剂的亲和力在GABA存在下降低，并且GABA对拮抗剂的亲和力没有影响（3，4）。据推测，活性的这些差异是由于各种配体在BZR上的构象变化引起的（5，6，7）。我们以前提出了一个模型，其中有两个主要位点，用于基于化合物的结构相关性在BZR上结合配体（苯并二氮杂卓类和非苯并二氮杂卓类），其IC 50值在nM范围内[图2和3]（8，9）。
1948 Conformational Shifts at the BZR Vol. 39, No. 21, 1986 vitro studies have shown that BZ agonists enhance the binding of GABA to its receptor, inverse agonists inhibit GABA binding while antagonists which reverse both of these effects have no influence on GABA binding (2). The reverse effect, that is binding of the ligands to the BZR in the presence or absence of GABA, follows the same pattern. The affinity of agonists is enhanced by GABA, the affinity of inverse agonists is decreased in the presence of GABA, and there is no effect of GABA on the affinity of antagonists (3, 4). It has been postulated that these differences in activity are due to conformational changes effected at the BZR by the various ligands (5, 6, 7).We have previously proposed a model, in which there are two major sites, for binding of ligands at the BZR based a structural correlation of compounds (both benzodiazepines and non-benzodiazepines) which have IC50 values in the nM range [FIG. 2 and 3](8, 9).
儿童简明精神病评定量表。
影响因子：
--
作者：
Overall,JE;Pfefferbaum,B
通讯作者：
Pfefferbaum,B