Peroutka S J
Department of Neurology, Stanford University Medical Center, CA 94305.
Naunyn Schmiedebergs Arch Pharmacol. 1988 Nov;338(5):472-5. doi: 10.1007/BF00179316.
The specific binding of 3H-quipazine to putative 5-HT3 receptors was analyzed in multiple species. Specific and saturable binding of the radioligand could be detected in both rat (KD = 1.2 nM; Bmax = 3.0 pmol/g) and pig (KD = 1.3 +/- 0.2 nM; Bmax = 1.5 +/- 0.2 p/mol/g) cortical membranes. By contrast, no significant specific binding of 3H-quipazine could be detected in human, cow, dog, turtle, mouse, guinea pig, chicken or rabbit brain membranes. These data indicate that marked species variations exist in the presence and/or density of 5-HT3 membrane recognition sites in the central nervous system.
在多个物种中分析了³H-喹哌嗪与假定的5-羟色胺3（5-HT3）受体的特异性结合。在大鼠（解离常数KD = 1.2纳摩尔；最大结合量Bmax = 3.0皮摩尔/克）和猪（KD = 1.3±0.2纳摩尔；Bmax = 1.5±0.2皮摩尔/克）的皮质膜中均能检测到放射性配体的特异性和饱和性结合。相比之下，在人、牛、狗、龟、小鼠、豚鼠、鸡或兔的脑膜中未检测到³H-喹哌嗪的显著特异性结合。这些数据表明，中枢神经系统中5-HT3膜识别位点的存在和/或密度存在明显的物种差异。
