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.
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Serotonin Transporter Inhibitors
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Serotonin Transporter Agonists
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Serotonin Transporter Antagonists
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Serotonin Transporter Activators
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Serotonin Transporter Modulators
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Serotonin Transporter Controls
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Serotonin Transporter Substrates
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Serotonin Transporter Ligands
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Serotonin Transporter Related Products (304)
Related Products (304)
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Antibodies (3)
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Coccinine
0 ImagesCoccinine ((-)-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.
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DSP-1053 benzenesulfonate
0 ImagesCat. No.: HY-111419ACAS No.: 1176326-78-5DSP-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.
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4-MeO-MiPT
0 ImagesCat. No.: HY-W682464CAS No.: 96096-53-64-MeO-MiPT is a serotonin transporter (SERT) inhibitor and serotonin 2A receptor (5-HT2A) agonist with pIC50 and IC50 values of 57 nM and 0.43 nM for human SERT, and pEC50 and EC50 values of 23 nM and 2.3 nM for human 5-HT2A, respectively. 4-MeO-MiPT blocks serotonin uptake via SERT, acts as an agonist at 5-HT2A receptors, and exhibits agonist activity at 5-HT1A, 5-HT1D, 5-HT2B, and 5-HT2C receptors. 4-MeO-MiPT can be used for the research of depression.
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Norfenfluramine hydrochloride
0 ImagesSynonyms: (±)-Norfenfluramine hydrochlorideNorfenfluramine 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.
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Tampramine
0 ImagesCat. No.: HY-136514CAS No.: 83166-17-0Tampramine (47), a phenothiazine, could reverse multidrug resistance, with ED50 values of 60 μM (P388 cells) and 60 μM (P388/ADR cells), respectively.
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Sakura-6
0 ImagesCat. No.: HY-P10029CAS No.: 2490708-79-5Sakura-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.
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Tametraline
0 ImagesCat. No.: HY-106493CAS No.: 52795-02-5Synonyms: CP 24441Tametraline (CP 24441) is a norepinephrine reuptake inhibitor. Tametraline can be used for the research of neurological disease, such as depression.
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Zimelidine dihydrochloride (Standard)
0 ImagesCat. No.: HY-110023RCAS No.: 60525-15-7Zimelidine 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.
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SERT-IN-3
0 ImagesCat. No.: HY-160655CAS No.: 289717-03-9SERT-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.
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Paroxetine-d2
0 ImagesCat. No.: HY-111124CAS No.: 923932-43-8Synonyms: BRL29060-d2Paroxetine-d2 (BRL29060-d2) is the deuterated-labeled Paroxetine (HY-122272). Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.
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Desvenlafaxine (Standard)
0 ImagesCat. No.: HY-B0602RCAS No.: 93413-62-8Synonyms: O-Desmethylvenlafaxine (Standard)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.
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JNJ-28583867
0 ImagesCat. No.: HY-119087CAS No.: 892407-39-5JNJ-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.
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AChE-IN-5
0 ImagesCat. No.: HY-144272CAS No.: 3037236-13-5AChE-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.
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D-473
0 ImagesCat. No.: HY-182247CAS No.: 1632000-05-5D-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.
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A6CDQ
0 ImagesCat. No.: HY-182363CAS No.: 1005550-46-8A6CDQ 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.
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SLV310
0 ImagesCat. No.: HY-106194CAS No.: 264869-71-8SLV310 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.
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Z8779877149
0 ImagesCat. No.: HY-181878Synonyms: Z7149Z8779877149 (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.
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(±)-Duloxetine hydrochloride
0 ImagesCat. No.: HY-B0161ECAS No.: 947316-47-4Synonyms: (Rac)-Duloxetine hydrochloride(±)-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.
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PH-064 (tetra(hydrochloride))
0 ImagesCat. No.: HY-10499ACAS No.: 2489449-03-6Synonyms: BIM-46187 tetrahydrochloridePH-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.
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iso-WAY-260022
0 ImagesCat. No.: HY-10427ACAS No.: 1214914-38-1Synonyms: iso-NRI-022iso-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.
