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慢性地塞米松和阿米替林治疗后大鼠血小板中5-羟色胺摄取及丙咪嗪结合情况

Serotonin uptake and imipramine binding in rat platelets after chronic dexamethasone and amitriptyline treatment.

作者信息

Chan M Y, Lee P H

出版信息

Pharmacol Res Commun. 1985 Jul;17(7):619-32. doi: 10.1016/0031-6989(85)90069-4.

Abstract

Chronic adrenocorticotrophin treatment was shown to decrease platelet 5HT uptake, increase Km and decrease Vmax. Similarly, chronic dexamethasone treatment decreased 5HT uptake, but had no effect on the Kd and Bmax of high affinity imipramine binding sites in the platelets. Chronic amitriptyline treatment induced similar changes, with the exception that the drug induced a decrease in the number of high affinity imipramine binding sites. Chronic dexamethasone treatment potentiated the effects of amitriptyline and decreased the IC50 of imipramine and desipramine as 5HT uptake inhibitors in vitro. The results suggest that whereas 5HT uptake is related to high affinity imipramine binding sites, it can be modified independently of the high affinity imipramine binding.

摘要

长期促肾上腺皮质激素治疗可降低血小板对5-羟色胺(5HT)的摄取,增加米氏常数(Km)并降低最大反应速度(Vmax)。同样,长期地塞米松治疗也会降低5HT摄取,但对血小板中高亲和力丙咪嗪结合位点的解离常数(Kd)和最大结合容量(Bmax)没有影响。长期阿米替林治疗会引起类似变化,不同的是该药物会导致高亲和力丙咪嗪结合位点数量减少。长期地塞米松治疗可增强阿米替林的作用,并降低丙咪嗪和去甲丙咪嗪作为5HT摄取抑制剂在体外的半数抑制浓度(IC50)。结果表明,虽然5HT摄取与高亲和力丙咪嗪结合位点有关,但它可以独立于高亲和力丙咪嗪结合而被改变。

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