Hall J M, Frankham P A, Strange P G
J Neurochem. 1983 Dec;41(6):1526-32. doi: 10.1111/j.1471-4159.1983.tb00859.x.
The use of cholate (in the presence of sodium chloride) is described for solubilising brain D2 dopamine receptors. The method described gives in high yield a preparation of solubilised D2 receptors which when assayed by [3H]spiperone binding show little interference from nonspecific and nonstereospecific binding sites. Characterisation by ultrafiltration, electron microscopy, gel filtration, and sucrose density gradient centrifugation has been achieved, showing the receptors to be truly solubilised. Pharmacological characterisation using [3H]spiperone binding suggested the presence of serotonergic S2 receptors in addition to D2 receptors. The pharmacological properties of the solubilised D2 receptors show a good correlation with those of membrane-bound receptors, although ligand binding affinities are lower in the solubilised preparation.
描述了使用胆酸盐（在氯化钠存在下）溶解脑D2多巴胺受体的方法。所述方法以高产率得到溶解的D2受体制剂，通过[3H]螺哌隆结合测定时，该制剂显示出非特异性和非立体特异性结合位点的干扰很小。已通过超滤、电子显微镜、凝胶过滤和蔗糖密度梯度离心进行了表征，表明受体确实已溶解。使用[3H]螺哌隆结合的药理学表征表明，除了D2受体外，还存在5-羟色胺能S2受体。溶解的D2受体的药理学特性与膜结合受体的药理学特性具有良好的相关性，尽管在溶解制剂中配体结合亲和力较低。
