Wouters W, Van Dun J, Leysen J E, Laduron P M
Eur J Pharmacol. 1985 Sep 10;115(1):1-9. doi: 10.1016/0014-2999(85)90577-1.
Serotonin-S2 receptors from rat frontal cortex were solubilized with a mixture of 6.8 mM CHAPS (3-[(3-cholamidopropyl)-dimethylammonio]-1-propane sulphonate) and 1.4 M sodium chloride. This new solubilization procedure solubilized about 40% of the membrane-bound serotonin-S2 receptors in an active form. The solubilized receptors were not sedimented after 1 h of centrifugation at 100 000 X g and they passed freely through 0.20 micron filters. The solubilized preparation showed high affinity binding of [3H]ketanserin and revealed a typical serotonin-S2 receptor profile: binding could be displaced by nanomolar concentrations of different serotonin antagonists and by micromolar concentrations of serotonin agonists. Compounds belonging to other pharmacological classes were poorly, or not active. Upon density gradient sedimentation, Svedberg coefficients of approximately 5 S were found on sucrose gradients made with H2O or D2O as the solvent. This was much lower than the value of 11.5 S previously reported from lysophosphatidylcholine-solubilized serotonin-S2 receptors.
用6.8 mM CHAPS（3-[(3-胆酰胺丙基)-二甲基铵]-1-丙烷磺酸盐）和1.4 M氯化钠的混合物溶解大鼠额叶皮质中的血清素-S2受体。这种新的溶解方法以活性形式溶解了约40%的膜结合血清素-S2受体。溶解的受体在100 000×g离心1小时后不会沉淀，并且可以自由通过0.20微米的滤膜。溶解的制剂显示出对[3H]酮色林的高亲和力结合，并呈现出典型的血清素-S2受体特征：结合可被纳摩尔浓度的不同血清素拮抗剂和微摩尔浓度的血清素激动剂所取代。属于其他药理学类别的化合物活性很低或无活性。在密度梯度沉降时，以H2O或D2O作为溶剂的蔗糖梯度上发现斯维德伯格系数约为5 S。这远低于先前报道的溶血磷脂酰胆碱溶解的血清素-S2受体的11.5 S的值。
