Improved potency of escitalopram on the human serotonin transporter: demonstration of an ex vivo assay technique.
Improved potency of escitalopram on the human serotonin transporter: demonstration of an ex vivo assay technique.
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提高艾司西酞普兰对人血清素转运蛋白的效力：离体测定技术的演示。
DOI：
10.1097/01.jcp.0000116647.91923.66
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发表时间：
2004
影响因子：
2.9
通讯作者：
Hobby,HMac
中科院分区：
文献类型：
--
作者：
Rausch,JeffreyL;Corley,KatinaM;Hobby,HMac
将艾司西酞普兰（“Lexapro”，s-西酞普兰，LU-26-054）的效力与外消旋西酞普兰（“Celexa”）的效力进行比较，使用来自药物处理的正常对照的血浆样品进行血小板中人血清素[5-羟色胺（5-HT）]转运抑制的测定。可获得4小时和24天给药的样品。数据表明，在给药后4小时内，每种药物的5-HT转运抑制作用均充分显现，到24天治疗时，血小板转运抑制作用未显著增加。此外，艾司西酞普兰和西酞普兰存在剂量-反应关系，随着剂量的增加，5-HT转运抑制作用增强。从数据中可以明显看出，艾司西酞普兰在抑制人血小板5-HT转运方面比其外消旋体更有效。30毫克艾司西酞普兰的效果近似于60毫克外消旋西酞普兰的效果，同样，10毫克艾司西酞普兰的效果近似于20毫克外消旋西酞普兰的效果。这是首次证明艾司西酞普兰对人体5-HT转运蛋白的药效学作用。结果证明其在人5-HT转运蛋白位点的上级效力。
The potency of escitalopram (" Lexapro," s-citalopram, LU-26-054) was compared with that of racemic citalopram (" Celexa") using plasma samples from drug-treated normal controls applied to an assay of human serotonin [5-hydroxytryptamine (5-HT)] transport inhibition in blood platelets. Samples were available for both 4-hour and 24-day drug administration. The data indicated that 5-HT transport inhibition was fully manifest for each drug within 4 hours of administration, without significant increase in platelet transport inhibition by 24-day treatment. In addition, a dose-response relationship could be seen for escitalopram and citalopram with increasing 5-HT transport inhibition observed with increasing dose. It was evident from the data that escitalopram was significantly more potent than its racemate in inhibiting human platelet 5-HT transport. Thirty milligrams of escitalopram approximated the effect of 60 mg of racemic citalopram, and similarly, 10 mg of escitalopram approximated that of 20 mg of its racemate. This is the first demonstration of escitalopram's pharmacodynamic effect on the human 5-HT transporter. The results demonstrate its superior potency at the human 5-HT transporter site.