1. Signaling Pathways
  2. Neuronal Signaling
  3. Serotonin Transporter

Serotonin Transporter

5-HTT; SERT; SLC6A4

Serotonin Transporters (SERTs) are integral membrane proteins that transport serotonin from synaptic spaces into presynaptic neurons. SERTs function by reuptaking serotonin in the synaptic cleft, effectively terminating the function of serotonin and halting neuronal transmission. Serotonin reuptake is a critical process to prevent overstimulation of nerves.

Serotonin transporter (SERT) regulates extracellular levels of serotonin (5-hydroxytryptamine, 5HT) in the brain by transporting 5HT into neurons and glial cells. The human SERT (hSERT) is the primary target for drugs used in the treatment of emotional disorders, including depression. hSERT belongs to the solute carrier 6 family that includes a bacterial leucine transporter (LeuT), for which a high resolution crystal structure has become available.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-107370
    Atomoxetine
    Inhibitor
    Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with Ki values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DAEX and NEEX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na+ channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research.
    Atomoxetine
  • HY-B0103AS1
    Fluvoxamine-d4 maleate
    Inhibitor
    Fluvoxamine-d4 (maleate) is the deuterium labeled Fluvoxamine maleate. Fluvoxamine maleate (DU-23000 maleate) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.
    Fluvoxamine-d<sub>4</sub> maleate
  • HY-110289R
    (R)-Citalopram oxalate (Standard)
    Inhibitor
    (R)-Citalopram (oxalate) (Standard) is the analytical standard of (R)-Citalopram (oxalate). This product is intended for research and analytical applications. (R)-Citalopram oxalate is an anticonvulsant, antidepressant and muscle relaxant. (R)-Citalopram oxalate is at least 20-fold weaker than S-citalopram (Escitalopram; HY-14258) as inhibitor of the 5-HT transporter (SERT). (R)-Citalopram oxalate functionally antagonises S-citalopram in vivo and in vitro. (R)-Citalopram oxalate has an effect on the association of Escitalopram with the high affinity primary site, and on its dissociation from the 5-HT transporter, via an allosteric mechanism.
    (R)-Citalopram oxalate (Standard)
  • HY-121203S4
    Citalopram-d3 hydrochloride
    Inhibitor
    Citalopram-d3 hydrochloride is deuterated labeled Citalopram (HY-121203). Citalopram is a racemate mixture of the active S(+)-enantiomer (Escitalopram; HY-14258) and R(-)-enantiomer. Citalopram is an orally active selective serotonin reuptake inhibitor (SSRI). Citalopram is an antidepressant and enhances serotoninergic neurotransmission.
    Citalopram-d<sub>3</sub> hydrochloride
  • HY-133171
    (R)-Norfluoxetine
    Inhibitor
    (R)-Norfluoxetine is the (R)-enantiomer of Norfluoxetine (HY-135556). (R)-Norfluoxetine is a potent serotonin re-uptake inhibitor, with a Ki of 13 nM. (R)-Norfluoxetine can be used for the research of depression.
    (R)-Norfluoxetine
  • HY-B0304
    Dapoxetine
    Inhibitor
    Dapoxetine (LY-210448) is an orally active and selective serotonin reuptake inhibitor (SSRI). Dapoxetine can be used for the research of premature ejaculation (PE).
    Dapoxetine
  • HY-146619
    RAGE/SERT-IN-1
    Inhibitor
    RAGE/SERT-IN-1 is a potent and orally active advanced glycation end products (RAGE) and serotonin transporter (SERT) inhibitor with IC50s of 8.26 μM and 31.09 nM, respectively. RAGE/SERT-IN-1 exhibits significant neuroprotective effect against Aβ25-35-induced neuronal damage and alleviates depressive behavior of mice. RAGE/SERT-IN-1 can be used for researching the comorbidity of Alzheimer's disease and depression.
    RAGE/SERT-IN-1
  • HY-N15636
    Coccinine
    Inhibitor
    Coccinine ((-)-Coccinine) is a weak inhibitor of SERT (IC50: 196.3 μM; Ki: 106.8 μM) and P-gp (IC50: 0.96 mM). Coccinine exhibits significant anti-tumor activity against various cancer cell lines, such as breast cancer (MCF7, Hs578T, MDA-MB-231), colon cancer (HCT-15), and lung cancer (A549). Coccinine can be used in the research of tumors and neurological diseases.
    Coccinine
  • HY-111419A
    DSP-1053 benzenesulfonate
    Inhibitor
    DSP-1053, a benzylpiperidine derivative, is a potent serotonin transporter (SERT) inhibitor with a Ki of 1.02 nM. DSP-1053 shows partial 5-HT1A receptor agonistic activity with a Ki of 5.05 nM. DSP-1053 has antidepressant activity.
    DSP-1053 benzenesulfonate
  • HY-136514
    Tampramine
    Tampramine (47), a phenothiazine, could reverse multidrug resistance, with ED50 values of 60 μM (P388 cells) and 60 μM (P388/ADR cells), respectively.
    Tampramine
  • HY-14794
    Dextromilnacipran
    Inhibitor 99.90%
    Dextromilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Dextromilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC50 of 3.4 μM. (patent WO2013014263A1).
    Dextromilnacipran
  • HY-P10029
    Sakura-6
    Inhibitor
    Sakura-6 is a SERT-nnos interaction promoter that significantly increases the SERT-nnos complex, but reduces the level of SERT on the cell surface. Acute injection of Sakura-6 into the dorsal raphe nucleus (DRN) causes depression-like behavior in mice.
    Sakura-6
  • HY-110023R
    Zimelidine dihydrochloride (Standard)
    Inhibitor
    Zimelidine (dihydrochloride) (Standard) is the analytical standard of Zimelidine (dihydrochloride). This product is intended for research and analytical applications. Zimelidine dihydrochloride is a potent and selective inhibitor of serotonin 5-HT uptake and SERT. Zimelidine dihydrochloride is an antidepressant.
    Zimelidine dihydrochloride (Standard)
  • HY-160655
    SERT-IN-3
    Inhibitor
    SERT-IN-3 (compound 12) is an inhibitor of serotonin transporter (SerT). In pharmacological assays, the IC50 of SERT-IN-3 for SerT was 34.4 nM.
    SERT-IN-3
  • HY-111124
    Paroxetine-d2
    Paroxetine-d2 (CTP 347) is a deuterium labeled Paroxetine (HY-122272). Paroxetine is an oral inhibitor that falls under the category of selective serotonin reuptake inhibitors (SSRIs). Paroxetine is also a very weak norepinephrine (NE) reuptake inhibitor, capable of inducing cell apoptosis and having anti-tumor activity. Paroxetine has antidepressant, anti-anxiety, and pain-relieving effects, and it can help improve conditions like obsessive-compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual anxiety, and chronic headaches.
    Paroxetine-d<sub>2</sub>
  • HY-B0602R
    Desvenlafaxine (Standard)
    Inhibitor
    Desvenlafaxine (Standard) is the analytical standard of Desvenlafaxine. This product is intended for research and analytical applications. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.
    Desvenlafaxine (Standard)
  • HY-119087
    JNJ-28583867
    Inhibitor
    JNJ-28583867 is an orally active and selective histamine H3 receptor antagonist (Ki=10.6 nM) and serotonin transporter (SERT) inhibitor (Ki=3.7 nM). JNJ-28583867 can be used in the research of depression.
    JNJ-28583867
  • HY-144272
    AChE-IN-5
    Inhibitor
    AChE-IN-5 (compound 5) exhibits strong in vitro bioactivity against AChE/5-HT1A/SERT and exhibits good BBB permeability. AChE-IN-5 shows IC50 value 2.29 nM against AChE, EC50 value 58.6 nM against 5-HT1A and IC50 value against SERT. Orally active.
    AChE-IN-5
  • HY-106194
    SLV310
    Inhibitor
    SLV310 is an orally active dopamine D2 receptor antagonist (Ki: 5 nM) and serotonin reuptake receptor inhibitor. SLV310 antagonizes Apomorphine (HY-12723) induced climbing behaviour and 5-HTP (HY-N0122) induced serotonin syndrome like behaviour in mice (ED50: 5.6 and 5.9 mg/kg, p.o.). SLV310 is an antipsychotic compound and can be used for schizophrenia research.
    SLV310
  • HY-B0102C
    (R)-Fluoxetine hydrochloride
    Inhibitor
    (R)-Fluoxetine hydrochloride, an antidepressant, is serotonin reuptake inhibitor (SSRI). (R)-Fluoxetine hydrochloride has modest affinity at the 5-HT2A and 5-HT2C receptors.
    (R)-Fluoxetine hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity