Phillips O M, Wood K M, Williams D C
J Neurochem. 1984 Aug;43(2):479-86. doi: 10.1111/j.1471-4159.1984.tb00924.x.
Apparent specific binding of [3H]imipramine to human platelet membranes at high concentrations of imipramine showed deviation from that expected of a single binding site, a result consistent with a low-affinity binding site. The deviation was due to displaceable, saturable binding to the glass fibre filters used in the assays. Imipramine, chloripramine, desipramine, and fluoxetine inhibited binding to filters whereas 5-hydroxytryptamine and ethanol were ineffective. Experimental conditions were developed that eliminated filter binding, allowing assay of high- and low-affinity binding to membranes. Failure to correct for filter binding may lead to overestimation of binding parameters, Bmax and KD for high-affinity binding to membranes, and may also be misinterpreted as indicating a low-affinity binding component in both platelet and brain membranes. Low-affinity binding (KD less than 2 microM) of imipramine to human platelet membranes was demonstrated and its significance discussed.
在高浓度丙咪嗪存在下，[3H]丙咪嗪与人血小板膜的表观特异性结合显示出与单一结合位点预期情况的偏差，这一结果与低亲和力结合位点相符。该偏差是由于与测定中使用的玻璃纤维滤膜存在可置换的、可饱和的结合。丙咪嗪、氯丙咪嗪、去甲丙咪嗪和氟西汀可抑制与滤膜的结合，而5-羟色胺和乙醇则无效。开发了消除滤膜结合的实验条件，从而能够测定与膜的高亲和力和低亲和力结合。未能校正滤膜结合可能导致高估与膜高亲和力结合的结合参数Bmax和KD，还可能被误解为表明在血小板膜和脑膜中都存在低亲和力结合成分。已证实丙咪嗪与人血小板膜的低亲和力结合（KD小于2 microM）并对其意义进行了讨论。
