Down-regulation of the rat serotonin transporter upon exposure to a selective serotonin reuptake inhibitor.

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.

journal_name

Neuroreport

journal_title

Neuroreport

authors

Horschitz S,Hummerich R,Schloss P

doi

10.1097/00001756-200107200-00027

subject

Has Abstract

pub_date

2001-07-20 00:00:00

pages

2181-4

issue

10

eissn

0959-4965

issn

1473-558X

journal_volume

12

pub_type

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