5-HT Transporters

5-HT transporters (serotonin transporters, SERT) are sodium- and chloride-dependent members of the solute carrier family 6 (SLC6) found widely distributed throughout the brain. They are responsible for re-uptake of 5-HT and undergo a conformational change to move molecules.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
2341 A 80426 mesylate
5-HT uptake inhibitor and α2 antagonist
4456 Amitriptyline hydrochloride
5-HT and noradrenalin re-uptake inhibitor; also TrkA/B agonist
4357 Bicifadine hydrochloride
Noradrenalin, 5-HT and dopamine re-uptake inhibitor
2322 BTS 54-505 hydrochloride
Potent SNRI; active metabolite of sibutramine (Cat. No. 2290)
1427 Citalopram hydrobromide
Highly potent and selective 5-HT uptake inhibitor
0457 Clomipramine hydrochloride
5-HT re-uptake inhibitor
2833 Cocaine hydrochloride
Inhibitor of monoamine transporters
4358 Dapoxetine hydrochloride
Selective serotonin reuptake inhibitor
2695 Dexfenfluramine hydrochloride
5-HT re-uptake inhibitor. Also stimulates 5-HT release
3428 DMT
SERT inhibitor. Also endogenous σ1 ligand and 5-HT2A agonist
4798 (S)-Duloxetine hydrochloride
Potent 5-HT and NA reuptake inhibitor; also blocks dopamine reuptake
4796 Escitalopram oxalate
Selective serotonin reuptake inhibitor (SSRI)
0927 Fluoxetine hydrochloride
5-HT reuptake inhibitor
1033 Fluvoxamine maleate
5-HT re-uptake inhibitor
1588 Indatraline hydrochloride
Potent 5-HT uptake inhibitor; also inhibits dopamine and noradrenalin uptake
2545 Lofepramine
5-HT and noradrenalin re-uptake inhibitor (SNRI)
3350 LY 393558
Dual 5-HT re-uptake inhibitor and 5-HT1B/1D antagonist
2148 (±)-McN 5652
Potent, orally active 5-HT uptake inhibitor. Also inhibits noradrenalin and dopamine uptake in vitro
3027 (±)-MDMA hydrochloride
Inhibitor of 5-HT and dopamine uptake; hallucinogenic
4443 Mephedrone hydrochloride
Inhibits synaptosomal dopamine and 5-HT uptake
3286 Milnacipran hydrochloride
5-HT and noradrenalin re-uptake inhibitor (SNRI)
2777 Nefazodone hydrochloride
5-HT uptake inhibitor and 5-HT2A antagonist. Antidepressant
2141 Paroxetine maleate
Highly potent and selective 5-HT uptake inhibitor
2395 Sertraline hydrochloride
5-HT re-uptake inhibitor
2290 Sibutramine hydrochloride
5-HT and noradrenalin re-uptake inhibitor (SNRI)
2175 Tetrabenazine
Potent inhibitor of vesicular monoamine transport; depletes 5-HT stores
2917 Venlafaxine hydrochloride
Dual serotonin/noradrenalin re-uptake inhibitor
6202 Vilazodone hydrochloride
Potent SSRI and 5-HT1A partial agonist; antidepressant
4194 WY 45233 succinate
Dual serotonin/noradrenalin re-uptake inhibitor
1767 Zimelidine dihydrochloride
Selective 5-HT uptake inhibitor

Substrates

Cat No Product Name / Activity
5573 Chlorphentermine hydrochloride
Serotonin transporter substrate; appetite suppressant

Other

Cat No Product Name / Activity
5763 (R)-Citalopram oxalate
Enantiomer of escitalopram oxalate (Cat. No. 1427)
3547 Serotonin hydrochloride
Endogenous substrate
1972 Tianeptine sodium salt
Selective facilitator of 5-HT uptake; antidepressant

5-HT transporters (serotonin transporters, SERT) are sodium- and chloride-dependent members of the solute carrier family 6 (SLC6) found widely distributed throughout the brain. They are responsible for re-uptake of 5-HT and undergo a conformational change to move one or more molecules per cycle.

Structural motifs include 12-TM domains, extracellular loops, cytoplasmic C- and N-termini, putative phosphorylation sites acting as potential targets for PKA and PKC and regions essential for 5-HT selective affinity. There is evidence to suggest that SERTs are linked to neuroticism, sexual behavior, alcoholism, clinical depression, hypertension and obsessive-compulsive disorder.

External sources of pharmacological information for 5-HT Transporters :

    Literature for 5-HT Transporters

    Neurodegeneration

    Neurodegeneration Product Guide

    A collection of over 275 products for neurodegeneration research, the guide includes research tools for the study of:

    • Alzheimer's disease
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    5-HT Receptors

    5-HT Receptors Scientific Review

    Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.

    5-HT Transporter Gene Data

    Species Gene Symbol Gene Accession No. Protein Accession No.
    Human SLC6A4 NM_001045 P31645
    Mouse Slc6a4 NM_010484 Q60857
    Rat Slc6a4 NM_013034 P31652