类固醇对去甲丙咪嗪及其他抗抑郁药抑制血小板5-羟色胺摄取的影响。

Effect of steroids on the inhibition of platelet 5HT uptake by desipramine and other antidepressants.

作者信息

Lee P H, Chan M Y

出版信息

Eur J Pharmacol. 1984 Nov 13;106(2):255-62. doi: 10.1016/0014-2999(84)90712-x.

Abstract

The inhibitory effect of desipramine on platelet 5HT uptake was tested ex vivo and in vitro in control, adrenalectomised and triamcinolone-treated rats. In both situations, the inhibitory effect of desipramine was augmented in adrenalectomised rats and decreased in triamcinolone-treated rats. These changes in desipramine sensitivity were accompanied by changes in the uptake kinetic components, Km and Vmax. In in vitro studies, the IC50 of clomipramine, fluvoxamine, zimelidine, imipramine and nomifensine was decreased in adrenalectomised rat platelets and increased in corticosterone-, dexamethasone- or triamcinolone-treated rat platelets. Deoxycorticosterone had no effect. Testosterone only affected the IC50 of desipramine and nomifensine.

摘要

在对照、肾上腺切除和曲安西龙治疗的大鼠中，对去甲丙咪嗪对血小板5-羟色胺摄取的抑制作用进行了体内外测试。在这两种情况下，去甲丙咪嗪在肾上腺切除大鼠中的抑制作用增强，而在曲安西龙治疗的大鼠中则减弱。去甲丙咪嗪敏感性的这些变化伴随着摄取动力学成分Km和Vmax的变化。在体外研究中，氯米帕明、氟伏沙明、齐美利定、丙咪嗪和诺米芬辛的IC50在肾上腺切除的大鼠血小板中降低，而在皮质酮、地塞米松或曲安西龙治疗的大鼠血小板中升高。脱氧皮质酮没有作用。睾酮仅影响去甲丙咪嗪和诺米芬辛的IC50。