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-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-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-106493
    Tametraline
    Inhibitor
    Tametraline (CP 24441) is a norepinephrine reuptake inhibitor. Tametraline can be used for the research of neurological disease, such as depression.
    Tametraline
  • HY-110023R
    Zimelidine dihydrochloride (Standard)
    Inhibitor
    Zimelidine dihydrochloride (Standard) is the analytical standard of Zimelidine dihydrochloride (HY-110023). This product is intended for research and analytical applications. 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 (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-182247
    D-473
    Inhibitor
    D-473 is an orally active, blood-brain barrier penetrant and serotonin-preferring reuptake inhibitor. D-473 inhibits serotonin, dopamine and norepinephrine transporters, and significantly elevates the extracellular levels of these three neurotransmitters in rat brain regions. D-473 exhibits definite antidepressant-like activity without inducing motor activation. D-473 is widely used in studies related to major depressive disorder.
    D-473
  • HY-182363
    A6CDQ
    A6CDQ is a human organic cation transporter (hOCT) inhibitor with antidepressant-like activity that can cross the blood-brain barrier. A6CDQ potently inhibits the transport activities mediated by hOCT1, hOCT2 and hOCT3. A6CDQ exhibits significant antidepressant-like effects in the mouse tail suspension test. A6CDQ can be used in studies related to depression.
    A6CDQ
  • 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-181878
    Z8779877149
    Ligand
    Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (Ki=198 nM), α2A adrenergic receptor (Ki=180 nM; EC50=440 nM) and 5-HT2A receptor (EC50=172 nM, Emax=76%). Z8779877149 inhibits 5-HT reuptake and activates Gi and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders.
    Z8779877149
  • HY-B0161E
    (±)-Duloxetine hydrochloride
    Inhibitor
    (±)-Duloxetine ((Rac)-Duloxetine) hydrochloride is the racemate of Duloxetine hydrochloride. Duloxetine hydrochloride, a serotonin-norepinephrine reuptake inhibitor, can be used for diabetic neuropathic pain and fibromyalgia as well as major depressive disorder research.
    (±)-Duloxetine hydrochloride
  • HY-10499A
    PH-064 (tetra(hydrochloride))
    Inhibitor
    PH-064 tetrahydrochloride (BIM-46187 tetrahydrochloride) is an orally active inhibitor of the heterotrimeric G-protein complex. PH-064 tetrahydrochloride inhibits SERT activity and attenuates shear stress-induced Akt phosphorylation. PH-064 tetrahydrochloride has potent anti-hyperalgesia activity. PH-064 tetrahydrochloride inhibits G protein-coupled receptor-dependent tumorigenesis. PH-064 tetrahydrochloride can be used in the study of pain (e.g., inflammatory pain, neuropathic pain), GPCR-dependent tumors, and inflammatory lung injury.
    PH-064 (tetra(hydrochloride))
  • HY-10427A
    iso-WAY-260022
    Inhibitor
    iso-WAY-260022 (Compound 13R) is an orally active, brain-penetrant and selective norepinephrine transporter (hNET) inhibitor with an IC50 value of 140 nM. iso-WAY-260022 also shows inhibitory effects on human serotonin (hSERT) and dopamine transporters (hDAT). iso-WAY-260022 inhibits norepinephrine reuptake and increases hypothalamic norepinephrine levels to regulate thermoregulatory center function. iso-WAY-260022 is promising for research of vasomotor symptoms, such as menopausal hot flushes, night sweats.
    iso-WAY-260022
  • HY-B0304AS1
    Dapoxetine-d6 hydrochloride
    Inhibitor
    Dapoxetine-d6 (LY-210448-d6) hydrochloride is the deuterium labeled Dapoxetine hydrochloride. Dapoxetine hydrochloride is a short-acting selective serotonin reuptake inhibitor (SSRI)
    Dapoxetine-d<sub>6</sub> hydrochloride
  • HY-B0304AS2
    (rac)-Dapoxetine-d6 hydrochloride
    (rac)-Dapoxetine-d6 (hydrochloride) is the deuterium labeled (rac)-Dapoxetine hydrochloride.
    (rac)-Dapoxetine-d<sub>6</sub> hydrochloride
  • HY-17385S1
    Atomoxetine-d7 hydrochloride
    Atomoxetine-d7 hydrochloride (Tomoxetine-d7 hydrochloride) is the deuterium labeled Atomoxetine hydrochloride (HY-17385). Atomoxetine (Tomoxetine) hydrochloride is a selective noradrenaline reuptake inhibitor with Ki values of 5 nM, 77 nM and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine hydrochloride is a potent Na+ channels (VGSCs) blocker. Atomoxetine hydrochloride can be used for attention-deficit hyperactivity disorder (ADHD) research.
    Atomoxetine-d<sub>7</sub> hydrochloride
  • HY-B0196S1
    Venlafaxine-d6-1
    Inhibitor 99.9%
    Venlafaxine-d6-1 is deuterium labeled Venlafaxine. Venlafaxine (Wy 45030) is an orally active, potent serotonin (5-HT)/norepinephrine (NE) reuptake dual inhibitor. Venlafaxine is an antidepressant.
    Venlafaxine-d<sub>6</sub>-1
Cat. No. Product Name / Synonyms Application Reactivity