Lin J, Hu B R
Zhongguo Yao Li Xue Bao. 1989 May;10(3):193-7.
[3H]Flunitrazepam binding to benzodiazepine receptors solubilized by the detergent 3-[(3-cholamidopropyl)-dimethyl-ammonio]-l-propanesulfonate (CHAPS) was saturable and showed non-linear Scatchard plot with KD1 0.31 nmol/L and KD2 6.7 nmol/L. The affinities of soluble receptors to benzodiazepine were consistent with P2 membrane. One radioactive zone was found by SDS-PAGE after photoaffinity labelling of soluble membrane and the apparent molecular weight of 55,000 was reported. [3H]Flunitrazepam binding to soluble receptors was enhanced by GABA, NaCl or KCl and barbiturates, but inhibited by bicuculline and picrotoxinin. The enhancement of GABA on [3H]flunitrazepam binding was amplified by NaCl or KCl and antagonized by bicuculline and picrotoxinin. These results suggest that the benzodiazepine receptors solubilized by CHAPS have their pharmacological properties and are still associated with GABA receptors and chloride channel.
[3H]氟硝西泮与经去污剂3-[(3-胆酰胺丙基)-二甲基铵]-1-丙烷磺酸盐（CHAPS）增溶的苯二氮䓬受体的结合具有饱和性，且呈现非线性Scatchard图，解离常数KD1为0.31 nmol/L，KD2为6.7 nmol/L。可溶性受体对苯二氮䓬的亲和力与P2膜一致。对可溶性膜进行光亲和标记后，通过SDS-PAGE发现一个放射性条带，报道其表观分子量为55,000。[3H]氟硝西泮与可溶性受体的结合可被γ-氨基丁酸（GABA）、氯化钠（NaCl）或氯化钾（KCl）以及巴比妥类药物增强，但被荷包牡丹碱和印防己毒素抑制。NaCl或KCl可增强GABA对[3H]氟硝西泮结合的增强作用，而荷包牡丹碱和印防己毒素可拮抗该作用。这些结果表明，经CHAPS增溶的苯二氮䓬受体具有其药理学特性，并且仍与GABA受体和氯离子通道相关联。
