Dudai Y, Zvi S
Comp Biochem Physiol C Comp Pharmacol Toxicol. 1984;77(1):145-51. doi: 10.1016/0742-8413(84)90143-9.
[3H]Octopamine binds to a particulate preparation from heads of Drosophila melanogaster at a level of 0.5 +/- 0.1 pmol/mg protein, with an apparent dissociation constant of 6.0 +/- 0.9 x 10(-9) M at 26 degrees C. The binding is reduced or abolished by heat, trypsin, detergents, sulfhydryl reagents and EDTA. Low concentrations of MgCl2 or CaCl2 increase binding but high ionic strength is inhibitory. Low concentrations of dihydroergotamine, phentolamine, clonidine, chlorimipramine and chlorpromazine, but not of serotonin and propranolol, displace the labeled biogenic amine from its binding sites. The stable GTP analogue, guanosine-5'-(beta-gamma-imido)triphosphate (Gpp(NH)p), at the microM range, decreases the maximal number of the high-affinity [3H]octopamine-binding sites. The properties of the [3H]octopamine-binding sites are compared to the properties of octopamine receptors as revealed by stimulation of adenylate cyclase in insects, including Drosophila.
[3H]章鱼胺以0.5±0.1皮摩尔/毫克蛋白质的水平与黑腹果蝇头部的微粒体制剂结合，在26℃时其表观解离常数为6.0±0.9×10⁻⁹ M。加热、胰蛋白酶、去污剂、巯基试剂和乙二胺四乙酸可降低或消除这种结合。低浓度的氯化镁或氯化钙可增加结合，但高离子强度具有抑制作用。低浓度的二氢麦角胺、酚妥拉明、可乐定、氯米帕明和氯丙嗪（但血清素和普萘洛尔不会）可使标记的生物胺从其结合位点上 displaced 。微摩尔范围内的稳定鸟苷三磷酸类似物鸟苷-5'-（β-γ-亚氨基）三磷酸（Gpp(NH)p）可减少高亲和力[3H]章鱼胺结合位点的最大数量。将[3H]章鱼胺结合位点的特性与通过刺激包括果蝇在内的昆虫中的腺苷酸环化酶所揭示的章鱼胺受体的特性进行了比较。 （注：原文中“displace the labeled biogenic amine from its binding sites”的“displace”在这个语境下不好准确翻译，暂保留英文表述）
