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
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 :

    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