Biomaterial Database

Antagonists and substrates differentially regulate serotonin transporter cell surface expression in serotonergic neurons. 2010

Katharina Kittler, and Thorsten Lau, and Patrick Schloss

Biochemical Laboratory, Central Institute of Mental Health, J5, 68159 Mannheim, Germany.

The serotonin transporter (SERT) terminates serotonergic neurotransmission by the rapid removal of serotonin (5-hydroxytryptamine, 5-HT) from the extracellular space back into serotonergic neurons. SERT therefore controls the concentration of extracellular 5-HT, and thus one mechanism to regulate the efficacy of serotonergic neurotransmission is via modulation of the density of SERT molecules on the cell membrane. We have studied the effects of prolonged exposure to various selective serotonin re-uptake inhibitors (SSRIs), as well as cocaine and the transport substrates 5-HT and 3,4-methylenedioxy-methamphetamine (MDMA), on SERT cell surface expression in cultured serotonergic neurons. This was achieved via quantification of the amount of cell surface-expressed SERT molecules using antibody detection combined with confocal laser scanning microscopy. Our results show that exposure to the SSRIs citalopram, fluoxetine, sertraline and paroxetine all induced SERT internalization, but with different efficacies. The substrates 5-HT and MDMA also induced SERT internalization, while cocaine elevated SERT cell surface expression.

UI	MeSH Term	Description	Entries
D009474	Neurons	The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.	Nerve Cells,Cell, Nerve,Cells, Nerve,Nerve Cell,Neuron
D002460	Cell Line	Established cell cultures that have the potential to propagate indefinitely.	Cell Lines,Line, Cell,Lines, Cell
D003042	Cocaine	An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.	Cocaine HCl,Cocaine Hydrochloride,HCl, Cocaine,Hydrochloride, Cocaine
D005786	Gene Expression Regulation	Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation.	Gene Action Regulation,Regulation of Gene Expression,Expression Regulation, Gene,Regulation, Gene Action,Regulation, Gene Expression
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D012701	Serotonin	A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.	5-HT,5-Hydroxytryptamine,3-(2-Aminoethyl)-1H-indol-5-ol,Enteramine,Hippophaine,Hydroxytryptamine,5 Hydroxytryptamine
D015283	Citalopram	A furancarbonitrile that is one of the SELECTIVE SEROTONIN REUPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from TARDIVE DYSKINESIA in preference to tricyclic antidepressants, which aggravate dyskinesia.	Celexa,Citalopram Hydrobromide,Cytalopram,Lu-10-171,Seropram,Lu10171
D017367	Selective Serotonin Reuptake Inhibitors	Compounds that specifically inhibit the reuptake of serotonin in the brain.	5-HT Uptake Inhibitor,5-HT Uptake Inhibitors,5-Hydroxytryptamine Uptake Inhibitor,5-Hydroxytryptamine Uptake Inhibitors,SSRIs,Selective Serotonin Reuptake Inhibitor,Serotonin Reuptake Inhibitor,Serotonin Reuptake Inhibitors,Serotonin Uptake Inhibitor,Serotonin Uptake Inhibitors,Inhibitors, 5-HT Uptake,Inhibitors, 5-Hydroxytryptamine Uptake,Inhibitors, Serotonin Reuptake,Inhibitors, Serotonin Uptake,Reuptake Inhibitors, Serotonin,Uptake Inhibitors, 5-HT,Uptake Inhibitors, 5-Hydroxytryptamine,Uptake Inhibitors, Serotonin,Inhibitor, 5-HT Uptake,Inhibitor, 5-Hydroxytryptamine Uptake,Inhibitor, Serotonin Reuptake,Inhibitor, Serotonin Uptake,Reuptake Inhibitor, Serotonin,Uptake Inhibitor, 5-HT,Uptake Inhibitor, 5-Hydroxytryptamine,Uptake Inhibitor, Serotonin
D050486	Serotonin Plasma Membrane Transport Proteins	Sodium chloride-dependent neurotransmitter symporters located primarily on the PLASMA MEMBRANE of serotonergic neurons. They are different than SEROTONIN RECEPTORS, which signal cellular responses to SEROTONIN. They remove SEROTONIN from the EXTRACELLULAR SPACE by high affinity reuptake into PRESYNAPTIC TERMINALS. Regulates signal amplitude and duration at serotonergic synapses and is the site of action of the SELECTIVE SEROTONIN REUPTAKE INHIBITORS.	Neurotransmitter Transport Proteins, Serotonin-Specific,Neurotransmitter Transporters, Serotonin-Specific,Serotonin Plasma Membrane Transporter Proteins,5-Hydroxytryptamine Plasma Membrane Transport Protein,5HT Transporter,Platelet Serotonin Transporter,SERT Proteins,SLC6A4 Protein,Serotonectin,Serotonin Transporter,Serotonin Transporter, Platelets,Sodium-Dependent Serotonin Transporter,Solute Carrier Family 6, Member 4 Protein,5 Hydroxytryptamine Plasma Membrane Transport Protein,Neurotransmitter Transport Proteins, Serotonin Specific,Neurotransmitter Transporters, Serotonin Specific,Platelets Serotonin Transporter,Serotonin Transporter, Platelet,Serotonin Transporter, Sodium-Dependent,Serotonin-Specific Neurotransmitter Transporters,Sodium Dependent Serotonin Transporter,Transporter, Sodium-Dependent Serotonin
D018817	N-Methyl-3,4-methylenedioxyamphetamine	An N-substituted amphetamine analog. It is a widely abused drug classified as a hallucinogen and causes marked, long-lasting changes in brain serotonergic systems. It is commonly referred to as MDMA or ecstasy.	MDMA,Methylenedioxymethamphetamine,Ecstasy (Drug),N-Methyl-3,4-methylenedioxyamphetamine Hydrochloride,Hydrochloride, N-Methyl-3,4-methylenedioxyamphetamine,N Methyl 3,4 methylenedioxyamphetamine,N Methyl 3,4 methylenedioxyamphetamine Hydrochloride