Schotte A, Maloteaux J M, Laduron P M
Eur J Pharmacol. 1984 May 4;100(3-4):329-33. doi: 10.1016/0014-2999(84)90009-8.
Serotonin S2-receptors were solubilized from human brain by means of the mild detergent, lysolecithin. Previous studies have shown that the serotonin S2-receptors in human brain are mainly enriched in the cortex. A total particulate fraction from human cortex was treated with 0.25% lysolecithin. [3H]Ketanserin binding sites from the soluble extract showed the binding characteristics of S2-receptors: potent 5HT antagonists like pirenperone, methysergide and pipamperone competed for [3H]ketanserin binding at nanomolar concentrations. The agonists bufotenin and serotonin themselves were more active than the potent dopamine agonist tetraline. Binding was saturable with a low KD (1.07 nM) and reversible. There was a good correlation between the drug potencies in both soluble and membrane preparations and also with the IC50 values previously obtained in membrane preparations and soluble extract from rat brain. Therefore, lysolecithin allows serotonin S2-receptors from human brain to be obtained in a molecularly dispersed form with the same high affinity properties as in the original membranes.
通过温和去污剂溶血卵磷脂从人脑中溶解血清素S2受体。先前的研究表明，人脑中的血清素S2受体主要富集于皮质。用人皮质的总微粒体部分与0.25%的溶血卵磷脂进行处理。可溶性提取物中的[3H]酮色林结合位点显示出S2受体的结合特性：强效5-羟色胺拮抗剂如哌仑西平、麦角酰二乙胺和匹泮哌隆在纳摩尔浓度下竞争[3H]酮色林结合。激动剂蟾蜍色胺和血清素本身比强效多巴胺激动剂四氢萘更具活性。结合具有低解离常数（1.07 nM）的饱和性且可逆。在可溶性制剂和膜制剂中的药物效力之间以及与先前在大鼠脑的膜制剂和可溶性提取物中获得的半数抑制浓度（IC50）值之间存在良好的相关性。因此，溶血卵磷脂可使人脑中的血清素S2受体以分子分散形式获得，具有与原始膜相同的高亲和力特性。
