期刊
NEUROREPORT
卷 12, 期 10, 页码 2181-2184出版社
LIPPINCOTT WILLIAMS & WILKINS
DOI: 10.1097/00001756-200107200-00027
关键词
antidepressants; regulation; serotonin; transporter; uptake
The serotonin transporter (SERT) terminates serotonergic neurotransmission by rapid reuptake of 5-hydroxytryptamine (5-HT) into the nerve terminal or axonal varicosities. SERT represents the target. of various antidepressants which inhibit 5-HT transport and are widely used for the pharmacotherapy of depression. Here. we have analyzed the function of SERT stably expressed in HEK 293 cells upon exposure to citalopram, a selective serotonin reuptake inhibitor (SSRI), with respect to 5-HT transport activity and protein expression as estimated by ligand binding experiments. Our results show that long-term exposure to an SSRI causes a down-regulation of transport activity as revealed by a reduction of the maximal transport rate, without affecting substrate affinity, accompanied by a decrease in ligand binding sites. NeuroReport 12:2181-2184 (C) 2001 Lippincott Williams & Wilkins.
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