Heuring R E, Schlegel J R, Peroutka S J
Eur J Pharmacol. 1986 Mar 18;122(2):279-82. doi: 10.1016/0014-2999(86)90114-7.
The interaction of RU 24969 with [3H]5-hydroxytryptamine ([3H]5-HT) binding to non-5-HT1A binding sites was analyzed in nine species. Non-5-HT1A binding was defined as specific [3H]5-HT binding observed in the presence of 100 nM 8-OH-DPAT. Computer-assisted iterative curve fitting of RU 24969 competition studies indicate that RU 24969 distinguishes two distinct components of non-5-HT1A sites in rat and mouse brain. These two binding components display apparent Ki values of 0.33-0.39 and 66-130 nM for RU 24969. By contrast, RU 24969 competition for non-5-HT1A binding in guinea-pig, cow, human, dog, chicken, turtle and frog brain membranes is consistent with a homogeneous population of [3H]5-HT binding sites. This population of sites displays apparent Ki values of 23-130 nM for RU 24969 and appear to be analogous to the low affinity component of non-5-HT1A sites identified in rat and mouse.
在九个物种中分析了RU 24969与[3H]5-羟色胺（[3H]5-HT）结合至非5-HT1A结合位点的相互作用。非5-HT1A结合定义为在100 nM 8-OH-DPAT存在下观察到的特异性[3H]5-HT结合。RU 24969竞争研究的计算机辅助迭代曲线拟合表明，RU 24969区分了大鼠和小鼠脑中非5-HT1A位点的两个不同成分。这两个结合成分对RU 24969的表观Ki值分别为0.33 - 0.39 nM和66 - 130 nM。相比之下，RU 24969对豚鼠、牛、人、狗、鸡、龟和蛙脑膜中与非5-HT1A结合的竞争情况与[3H]5-HT结合位点的均匀群体一致。该位点群体对RU 24969的表观Ki值为23 - 130 nM，似乎类似于在大鼠和小鼠中鉴定出的非5-HT1A位点的低亲和力成分。
