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-N0173
    Cinchonidine
    Inhibitor 99.62%
    Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with Kis of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities.
    Cinchonidine
  • HY-A0022A
    Azaphen dihydrochloride monohydrate
    Inhibitor 99.94%
    Pipofezine(Azafen or Azaphen) is a potent inhibitor of the reuptake of serotonin.
    Azaphen dihydrochloride monohydrate
  • HY-W052508
    Norquetiapine
    Inhibitor 99.95%
    Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation.
    Norquetiapine
  • HY-B0492A
    Paroxetine hydrochloride hemihydrate
    Inhibitor 99.96%
    Paroxetine hydrochloride hemihydrate is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an antidepressant and has GRK2 inhibitory ability with IC50 of 14 μM.
    Paroxetine hydrochloride hemihydrate
  • HY-148565
    SERT-IN-2
    Inhibitor 98.06%
    SERT-IN-2 is a potent SERT inhibitor (IC50=0.58 nM) with promising anti-depression efficacy. SERT-IN-2 shows good bioavailability of 83.28% in rats. SERT-IN-2 can cross the blood-brain barrier.
    SERT-IN-2
  • HY-B0161
    Duloxetine
    Inhibitor 99.92%
    Duloxetine is a serotonin-norepinephrine reuptake inhibitor with a Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).
    Duloxetine
  • HY-148417
    ZZL-7
    Inhibitor 98.09%
    ZZL-7 is a fast-onset antidepressant agent. ZZL-7 works by disrupting the interaction between the serotonin transporter (SERT) and neuronal nitric oxide synthase (nNOS) in the dorsal raphe nucleus (DRN). ZZL-7 can cross the blood-brain barrier readily. ZZL-7 can be used for the research of major depressive disorder (MDD).
    ZZL-7
  • HY-B0168B
    Levomilnacipran hydrochloride
    Inhibitor 99.95%
    Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression.
    Levomilnacipran hydrochloride
  • HY-B0602A
    Desvenlafaxine succinate hydrate
    Inhibitor 99.82%
    Desvenlafaxine succinate hydrate, 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 succinate hydrate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.
    Desvenlafaxine succinate hydrate
  • HY-106100A
    Roxindole hydrochloride
    Inhibitor 99.53%
    Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities.
    Roxindole hydrochloride
  • HY-B0527AR
    Amitriptyline hydrochloride (Standard)
    Inhibitor
    Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline hydrochloride (Standard)
  • HY-18332A
    Amitifadine hydrochloride
    Inhibitor 99.64%
    Amitifadine hydrochloride is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC50s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.
    Amitifadine hydrochloride
  • HY-B0196AS1
    Venlafaxine-d6 hydrochloride
    Inhibitor 98.18%
    Venlafaxine-d6 (hydrochloride) is the deuterium labeled Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant.
    Venlafaxine-d<sub>6</sub> hydrochloride
  • HY-B0527AS
    Amitriptyline-d6 hydrochloride
    Inhibitor 99.65%
    Amitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline-d<sub>6</sub> hydrochloride
  • HY-10792A
    Eplivanserin (mixture)
    Inhibitor 99.68%
    Eplivanserin mixture (SR-46349 mixture) is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1.
    Eplivanserin (mixture)
  • HY-B0102B
    (S)-Fluoxetine hydrochloride
    Inhibitor 99.5%
    (S)-Fluoxetine hydrochloride, an antidepressant, is serotonin reuptake inhibitor (SSRI).
    (S)-Fluoxetine hydrochloride
  • HY-110023
    Zimelidine dihydrochloride
    Inhibitor 98.27%
    Zimelidine dihydrochloride is a potent and selective inhibitor of serotonin 5-HT uptake and SERT. Zimelidine dihydrochloride is an antidepressant.
    Zimelidine dihydrochloride
  • HY-111419
    DSP-1053
    Inhibitor 99.75%
    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
  • HY-B1490S
    Imipramine-d4 hydrochloride
    Inhibitor 99.95%
    Imipramine-d4 (hydrochloride) is the deuterium labeled Imipramine hydrochloride. Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is a Fascin1 inhibitor with antitumor activities. Imipramine hydrochloride also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects.
    Imipramine-d<sub>4</sub> hydrochloride
  • HY-135615A
    Desmethyl Sibutramine hydrochloride
    Inhibitor 99.74%
    Desmethyl Sibutramine hydrochloride, the secondary metabolite of Sibutramine, is an orally active norepinephrine transporter (NET) and serotonin transporter (SERT) inhibitor. Desmethyl Sibutramine hydrochloride can be used in the research of obesity and appetite suppressant.
    Desmethyl Sibutramine hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity