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

Serotonin Transporter

5-HTT; SERT; SLC6A4

Serotonin Transporter

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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-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-A0022A
    Azaphen dihydrochloride monohydrate
    		Inhibitor 99.94%
    Azaphen (Pipofezin) dihydrochloride monohydrate is an orally active serotonin reuptake inhibitor. Azaphen dihydrochloride monohydrate potentiates sympathomimetic compound effects. Azaphen dihydrochloride monohydrate can be used for the research of depressive states.
    Azaphen dihydrochloride monohydrate
  • HY-B0304A
    Dapoxetine hydrochloride
    		Inhibitor 99.96%
    Dapoxetine (LY-210448) hydrochloride is an orally active and selective serotonin reuptake inhibitor (SSRI). Dapoxetine hydrochloride can be used for the research of premature ejaculation (PE).
    Dapoxetine 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-148417
    ZZL-7
    		Inhibitor 98.13%
    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-106100A
    Roxindole hydrochloride
    		Inhibitor 99.48%
    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 (DOV-21947; EB-1010) 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-B1490R
    Imipramine hydrochloride (Standard)
    		Inhibitor
    Imipramine (hydrochloride) (Standard) is the analytical standard of Imipramine (hydrochloride). This product is intended for research and analytical applications. 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 hydrochloride (Standard)
  • HY-110023
    Zimelidine dihydrochloride
    		Inhibitor 98.08%
    Zimelidine dihydrochloride is an orally active selective serotonin reuptake inhibitor. Zimelidine dihydrochloride competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine dihydrochloride time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine dihydrochloride strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine dihydrochloride exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine dihydrochloride is used for the study of depressive disorders and analgesic tolerance.
    Zimelidine dihydrochloride
  • 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-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 99.9%
    (S)-Fluoxetine hydrochloride, an antidepressant, is serotonin reuptake inhibitor (SSRI).
    (S)-Fluoxetine hydrochloride
  • HY-B0457R
    Clomipramine hydrochloride (Standard)
    		Inhibitor
    Clomipramine (hydrochloride) (Standard) is the analytical standard of Clomipramine (hydrochloride). This product is intended for research and analytical applications. Clomipramine (Chlorimipramine) hydrochloride is a potent 5-HT reuptake blocker with the IC50 value of 1.5 nM. Clomipramine hydrochloride is a tricyclic antidepressant that can be used for the research of depression and obsessive compulsive disorder (OCD).
    Clomipramine hydrochloride (Standard)
  • HY-B0176AR
    Sertraline hydrochloride (Standard)
    		Inhibitor
    Sertraline (hydrochloride) (Standard) is the analytical standard of Sertraline (hydrochloride). This product is intended for research and analytical applications. Sertraline hydrochloride is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. Sertraline hydrochloride is researched for a number of diseases, such as major depressive disorder and obsessive.
    Sertraline hydrochloride (Standard)
  • 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
  • HY-110289
    (R)-Citalopram oxalate
    		Inhibitor 99.52%
    (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
  • HY-14258AR
    Escitalopram oxalate (Standard)
    		Inhibitor
    Escitalopram (oxalate) (Standard) is the analytical standard of Escitalopram (oxalate). This product is intended for research and analytical applications. Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression.
    Escitalopram oxalate (Standard)
Cat. No. Product Name / Synonyms Application Reactivity