Peroutka S J
Brain Res. 1985 Sep 30;344(1):167-71. doi: 10.1016/0006-8993(85)91204-1.
Drug interactions with serotonin(1A) 5-HT1A and serotonin(1B) (5-HT1B) binding sites were analyzed in bovine brain membranes. 5-HT1A binding sites were directly labeled with [3H]8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) in bovine hippocampal membranes. 5-HT1B binding sites were labeled by [3H]5-HT in bovine striatal membranes where less than 15% of specific binding sites are sensitive to nanomolar concentrations of 8-OH-DPAT. Each of the 12 agents tested was more potent at the 5-HT1A than 5-HT1B binding site. 5-HT, bufotenine, N,N-dimethyltryptamine (DMT) and quipazine were only slightly more potent at the 5-HT1A binding site. By contrast, 8-OH-DPAT, TVX Q 7821 and buspirone were significantly more potent at [3H]8-OH-DPAT binding sites in bovine hippocampus than at [3H]5-HT binding sites in bovine striatum. These findings suggest that 5-HT1A, and 5-HT1B binding sites have distinct pharmacological profiles and can be directly labeled with appropriate [3H]ligands in specific brain regions.
在牛脑膜中分析了与5-羟色胺（1A）（5-HT1A）和5-羟色胺（1B）（5-HT1B）结合位点的药物相互作用。在牛海马膜中，5-HT1A结合位点用[3H]8-羟基-2-（二正丙基氨基）-四氢萘（8-OH-DPAT）直接标记。在牛纹状体膜中，5-HT1B结合位点用[3H]5-HT标记，其中不到15%的特异性结合位点对纳摩尔浓度的8-OH-DPAT敏感。所测试的12种药物中的每一种在5-HT1A结合位点上比在5-HT1B结合位点上更有效。5-羟色胺、蟾蜍色胺、N，N-二甲基色胺（DMT）和喹哌嗪在5-HT1A结合位点上仅略强一些。相比之下，8-OH-DPAT、TVX Q 7821和丁螺环酮在牛海马中的[3H]8-OH-DPAT结合位点上比在牛纹状体中的[3H]5-HT结合位点上明显更有效。这些发现表明，5-HT1A和5-HT1B结合位点具有不同的药理学特征，并且可以在特定脑区用适当的[3H]配体直接标记。
