Milburn C M, Peroutka S J
Department of Neurology, Stanford University Medical Center, California 94305.
J Neurochem. 1989 Jun;52(6):1787-92. doi: 10.1111/j.1471-4159.1989.tb07258.x.
[3H]Quipazine was used to label binding sites in rat brain membranes that display characteristics of a 5-hydroxytryptamine3 (5-HT3) receptor. The radioligand binds with high affinity (KD, 1.2 +/- 0.1 nM) to a saturable population of sites (Bmax, 3.0 +/- 0.4 pmol/g of tissue) that are differentially located in the brain. Specific [3H]quipazine binding is not affected by guanine or adenine nucleotides. ICS 205-930, BRL 43964, Lilly 278584, and zacopride display less than nanomolar affinity for these sites whereas MDL 72222 is approximately one order of magnitude less potent. The pharmacological profile of the binding site is in excellent agreement with that of 5-HT3 receptors characterized in peripheral physiological models. We conclude that [3H]quipazine labels a 5-HT3 receptor in the rat CNS.
[3H]喹哌嗪用于标记大鼠脑膜中显示5-羟色胺3（5-HT3）受体特征的结合位点。该放射性配体以高亲和力（KD，1.2±0.1 nM）与位于脑中不同位置的可饱和位点群体（Bmax，3.0±0.4 pmol/g组织）结合。特异性[3H]喹哌嗪结合不受鸟嘌呤或腺嘌呤核苷酸的影响。ICS 205-930、BRL 43964、礼来278584和扎考必利对这些位点的亲和力小于纳摩尔，而MDL 72222的效力约低一个数量级。该结合位点的药理学特征与外周生理模型中表征的5-HT3受体的药理学特征高度一致。我们得出结论，[3H]喹哌嗪标记大鼠中枢神经系统中的5-HT3受体。
