Soskić V, Petrović J
Biochem Pharmacol. 1986 Dec 1;35(23):4229-36. doi: 10.1016/0006-2952(86)90700-8.
Dopamine D2 receptors were solubilized from synaptosomal membranes of the bovine caudate nucleus using a novel zwitterionic detergent 3-[(3-deoxycholamidopropyl)-dimethylammonio]-1-propane sulfonate (DCHAPS) supplemented with 1,2-propylene glycol. Optimal conditions for solubilization were: 0.12% DCHAPS, 5% 1,2-propylene glycol, 8 mg/ml membrane protein, 30 min, 4 degrees and the yield of the D2 receptors was 36.1%. The soluble extract retained the ability to bind [3H]spiperone. This binding was of high affinity (Kd = 2.28 +/- 0.16 nM), reversible and saturable (Bmax = 1.68 +/- 0.06 pmol/mg protein). The order of potencies of dopamine agonists and antagonists for inhibition of binding, paralleled that observed on membrane-bound D2 receptors (correlation factor r = 0.96). The stereo-specificity of solubilized receptors toward the pairs (+)-[(-)butaclamol, cis(Z)-]trans(E)flupenthixol and dihydroergosine/dihydroergosinine was pronounced.
使用一种新型两性离子去污剂3-[(3-脱氧胆酰胺丙基)-二甲基铵]-1-丙烷磺酸盐（DCHAPS）并添加1,2-丙二醇，从牛尾状核的突触体膜中溶解多巴胺D2受体。溶解的最佳条件为：0.12% DCHAPS、5% 1,2-丙二醇、8 mg/ml膜蛋白、30分钟、4℃，D2受体的产率为36.1%。可溶性提取物保留了结合[3H]螺哌隆的能力。这种结合具有高亲和力（Kd = 2.28 +/- 0.16 nM）、可逆且可饱和（Bmax = 1.68 +/- 0.06 pmol/mg蛋白）。多巴胺激动剂和拮抗剂抑制结合的效力顺序与在膜结合D2受体上观察到的顺序平行（相关系数r = 0.96）。溶解的受体对（+）-[（-）布他拉莫、顺式（Z）-]反式（E）氟哌噻吨和二氢麦角碱/二氢麦角异碱对的立体特异性明显。
