Lee P H, Chan M Y
Neuropharmacology. 1985 Nov;24(11):1043-50. doi: 10.1016/0028-3908(85)90189-3.
A comparative study of the effect of adrenalectomy, treatment with corticosterone, and imipramine on platelet an synaptosomal uptake was undertaken. One day after adrenalectomy, uptake of 5-hydroxytryptamine (5-HT) in the platelet and the hypothalamus was significantly decreased with an increase in the apparent Km, but the uptake of 5-HT of the cerebral synaptosomes was unchanged. In this group, the Kd of low affinity binding of 5-HT was also increased in the hypothalamic synaptosomes and in the platelet preparations. Treatment with corticosterone (5 mg/kg, i.m.) restored the decrease in the uptake of 5-HT induced by adrenalectomy in the hypothalamic synaptosomes and in the platelets, and significantly increased the uptake of 5-HT of these fractions in sham-operated rats. The binding of 5-HT was unchanged by acute treatment with corticosterone. The effectiveness of imipramine varied with the preparation and treatment group. The IC50 of the cerebral synaptosomal preparation was greater than that of the hypothalamic synaptosomal preparation. Using this latter preparation, the IC50 for imipramine in adrenalectomised, sham-operated and corticosterone-treated rats were found to be 0.04, 0.09 and 0.25 microM, respectively. These changes in sensitivity to imipramine were not reflected in the binding of [3H]imipramine which was unchanged.
对肾上腺切除术、皮质酮治疗及丙咪嗪对血小板和突触体摄取的影响进行了一项比较研究。肾上腺切除术后一天，血小板和下丘脑中5-羟色胺（5-HT）的摄取显著降低，表观米氏常数（Km）增加，但脑突触体中5-HT的摄取未变。在该组中，下丘脑突触体和血小板制剂中5-HT低亲和力结合的解离常数（Kd）也增加。皮质酮（5mg/kg，肌肉注射）治疗可恢复肾上腺切除术诱导的下丘脑突触体和血小板中5-HT摄取的降低，并显著增加假手术大鼠这些组分中5-HT的摄取。急性给予皮质酮对5-HT的结合无影响。丙咪嗪的有效性因制剂和治疗组而异。脑突触体制剂的半数抑制浓度（IC50）大于下丘脑突触体制剂。使用后一种制剂，发现肾上腺切除、假手术和皮质酮治疗大鼠中丙咪嗪的IC50分别为0.04、0.09和0.25微摩尔。对丙咪嗪敏感性的这些变化未反映在[3H]丙咪嗪的结合上，其结合未变。
