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-B0161D
    (R)-Duloxetine hydrochloride
    Inhibitor
    (R)-Duloxetine (LY248686) Hydrochloride is a napthalenyloxy-substituted amine utilized in binding studies with human serum albumin, and unlike its enantiomer (S)-Duloxetine, it exhibits limited efficacy as a dual serotonin and norepinephrine reuptake inhibitor (SNRI).
    (R)-Duloxetine hydrochloride
  • HY-129305
    Tampramine fumarate
    Inhibitor
    Tampramine fumarate is a potent, selective, noncompetitive NE reuptake inhibitor. Tampramine fumarate has antidepressant activity. Tampramine fumarate can be used in research of depression.
    Tampramine fumarate
  • HY-101684A
    Nitroxazepine hydrochloride
    Inhibitor
    Nitroxazepine hydrochloride is a tricyclic antidepressant (TCA) for the study of depression. Nitroxazepine acts as a serotonin-norepinephrine reuptake inhibitor.
    Nitroxazepine hydrochloride
  • 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, a R-(-) enantiomers of Citalopram (HY-121203), is a serotonin reuptake inhibitor. (R)-Citalopram oxalate is at least 20-fold weaker than S-citalopram (HY-14258) as inhibitor of the 5-HT transporter (SERT). (R)-Citalopram oxalate can be used for research of depression.
    (R)-Citalopram oxalate (Standard)
  • HY-179063
    5-HT2A receptor agonist-13
    Inhibitor
    5-HT2A receptor agonist-13 (Compound 28c) is a partial agonist of the 5-HT2A receptor, with an EC50 value of 416.9 nM and a Ki value of 113.9 nM. 5-HT2A receptor agonist-13 exhibits very weak agonistic activity towards the 5-HT2B receptor (EC50 = 120.2 nM), D2 receptor (Ki = 1298 nM), and has no activity towards the 5-HT2C receptor. 5-HT2A receptor agonist-13 exhibits weak inhibitory activity on the serotonin transporter (SERT) (EC50 = 977.2 nM). 5-HT2A receptor agonist-13 has antidepressant activity in mouse models and does not induce hallucinogenic behavior. 5-HT2A receptor agonist-13 can be used for the study of major depressive disorder (MDD) and treatment-resistant depression (TRD).
    5-HT2A receptor agonist-13
  • 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-106041A
    Sercloremine hydrochloride
    Inhibitor
    Sercloremine hydrochloride (CGP 4718A) is a selective and reversible MAO-A and 5-HT-uptake inhibitor. Sercloremine hydrochloride can be used in the research of depression.
    Sercloremine hydrochloride
  • HY-186169B
    (R,S)-MDDMA
    (R,S)-MDDMA is an MDMA analog that lacks the psychostimulant effects of its parent compound. (R,S)-MDDMA still retains partial serotonin-releasing activity.
    (R,S)-MDDMA
  • HY-175721
    UCD0820
    Inhibitor
    UCD0820 is a Serotonin transporter (SERT) inhibitor that acts as a partial serotonin releasing agent (SRA). UCD0820 can be used for depression, addiction and post-traumatic stress disorder (PTSD) research.
    UCD0820
  • HY-14472S1
    Tesofensine-13C,d3
    Inhibitor
    Tesofensine-13C,d3 (NS-2330-13C,d3) is the deuterium and 13C-labeled Tesofensine (HY-14472). Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent. Tesofensine is a CNS acting anti-obesity agent.
    Tesofensine-<sup>13</sup>C,d<sub>3</sub>
  • 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-182735
    BMS-570520
    Inhibitor
    BMS-570520 is an orally bioavailable CCR3 antagonist with an IC50 of 1.9 nM against hCCR3 and an IC50 of 1300 nM against hCYP2D6. BMS-570520 inhibits CYP2D6, but shows low activity against off-target G protein-coupled receptors, biogenic amine transporters, and the hERG potassium channel. BMS-570520 regulates chemotaxis, calcium mobilization, and anti-inflammatory pathways. BMS-570520 can be used in research related to asthma, allergic rhinitis, and contact dermatitis.
    BMS-570520
  • HY-W707780
    Nor mianserin hydrochloride
    99.48%
    Nor mianserin hydrochloride, demethylated derivative of Mianserin (HY-B0188), is a serotonin antagonist. Nor mianserin hydrochloride can be used for the research of diseases related to serotonin metabolism disorders and histamine metabolism disorders.
    Nor mianserin hydrochloride
  • 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-W707158
    Norfenfluramine hydrochloride
    Norfenfluramine hydrochloride ((±)-Norfenfluramine hydrochloride) is a major and brain-penetrant metabolite of Fenfluramine. Norfenfluramine hydrochloride can interact with 5-HT transporters to release 5-HT from neurons. Norfenfluramine hydrochloride displays antiepileptic effects in vivo.
    Norfenfluramine hydrochloride
  • 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
Cat. No. Product Name / Synonyms Application Reactivity