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  • Title: Down-regulation of the rat serotonin transporter upon exposure to a selective serotonin reuptake inhibitor.
    Author: Horschitz S, Hummerich R, Schloss P.
    Journal: Neuroreport; 2001 Jul 20; 12(10):2181-4. PubMed ID: 11447330.
    Abstract:
    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.
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