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5-HT transporter

" in MedChemExpress (MCE) Product Catalog:

52

Inhibitors & Agonists

1

Fluorescent Dye

5

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6

Isotope-Labeled Compounds

1

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-107128

    TD-9855 hydrochloride

    Serotonin Transporter Neurological Disease
    Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC50 values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma .
    Ampreloxetine hydrochloride
  • HY-110289

    Serotonin Transporter 5-HT Receptor Neurological Disease
    (R)-Citalopram oxalate is an anticonvulsant, antidepressant and muscle relaxant. (R)-Citalopram oxalate is at least 20-fold weaker than S-citalopram (Escitalopram; HY-14258) as inhibitor of the 5-HT transporter (SERT). (R)-Citalopram oxalate functionally antagonises S-citalopram in vivo and in vitro. (R)-Citalopram oxalate has an effect on the association of Escitalopram with the high affinity primary site, and on its dissociation from the 5-HT transporter, via an allosteric mechanism .
    (R)-Citalopram oxalate
  • HY-B1272
    Desipramine hydrochloride
    Maximum Cited Publications
    11 Publications Verification

    Dopamine Transporter Serotonin Transporter Neurological Disease Cancer
    Desipramine hydrochloride is an inhibitor of norepinephrine transporter (NET), 5-HT transporter (SERT) and dopamine transporter (DAT) with Kis of 4, 61 and 78,720 nM, respectively.
    Desipramine hydrochloride
  • HY-103089

    5-HT Receptor Neurological Disease
    LY393558 is a potent and orally active inhibitor of the 5-HT transporter and an antagonist of 5-HT1B and 5-HT1D receptors. LY393558 increase the extracellular levels of 5-HT in mice model frontal cortex. LY393558 can be used for researching depression .
    LY393558
  • HY-B1213

    5-HT Receptor Bacterial Neurological Disease
    Trimipramine maleate is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively . Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively . Trimipramine maleate has vascular activity and anxiolytic efficacy .
    Trimipramine maleate
  • HY-118010

    (±)-Norfenfluramine

    Serotonin Transporter Neurological Disease
    Norfenfluramine ((±)-Norfenfluramine) is a major and brain-penetrant metabolite of Fenfluramine. Norfenfluramine can interact with 5-HT transporters to release 5-HT from neurons. Norfenfluramine displays antiepileptic effects in vivo .
    Norfenfluramine
  • HY-110289R

    Serotonin Transporter 5-HT Receptor Neurological Disease
    (R)-Citalopram (oxalate) (Standard) is the analytical standard of (R)-Citalopram (oxalate). This product is intended for research and analytical applications. (R)-Citalopram oxalate is an anticonvulsant, antidepressant and muscle relaxant. (R)-Citalopram oxalate is at least 20-fold weaker than S-citalopram (Escitalopram; HY-14258) as inhibitor of the 5-HT transporter (SERT). (R)-Citalopram oxalate functionally antagonises S-citalopram in vivo and in vitro. (R)-Citalopram oxalate has an effect on the association of Escitalopram with the high affinity primary site, and on its dissociation from the 5-HT transporter, via an allosteric mechanism .
    (R)-Citalopram oxalate (Standard)
  • HY-B1272R

    Dopamine Transporter Serotonin Transporter Neurological Disease Cancer
    Desipramine (hydrochloride) (Standard) is the analytical standard of Desipramine (hydrochloride). This product is intended for research and analytical applications. Desipramine hydrochloride is an inhibitor of norepinephrine transporter (NET), 5-HT transporter (SERT) and dopamine transporter (DAT) with Kis of 4, 61 and 78,720 nM, respectively.
    Desipramine hydrochloride (Standard)
  • HY-B1213A

    5-HT Receptor Bacterial Neurological Disease
    Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy .
    Trimipramine
  • HY-B1213R

    5-HT Receptor Bacterial Neurological Disease
    Trimipramine (maleate) (Standard) is the analytical standard of Trimipramine (maleate). This product is intended for research and analytical applications. Trimipramine maleate is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively . Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively . Trimipramine maleate has vascular activity and anxiolytic efficacy .
    Trimipramine maleate (Standard)
  • HY-129985

    DU23811

    Serotonin Transporter 5-HT Receptor Neurological Disease
    Clovoxamine (DU23811) (Compound 35) has binding affinity for serotonin transporter (SERT) (Ki: 61 nM). Clovoxamine is a 5-HT and norepinephrine reuptake (NE) re-uptake inhibitor. Clovoxamine is an antidepressant .
    Clovoxamine
  • HY-121162

    (+)-Mesembrine

    5-HT Receptor Phosphodiesterase (PDE) Neurological Disease
    Mesembrine ((+)-Mesembrine) a main alkaloid that features an aryloctahydroindole skeleton. Mesembrine is a 5-HT transporter inhibitor with a Ki of 1.4 nM. Mesembrine also inhibits phosphodiesterase 4B (PDE4B) with an IC50 of 7.8 μM .
    Mesembrine
  • HY-B0527A
    Amitriptyline hydrochloride
    4 Publications Verification

    Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor Neurological Disease Cancer
    Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .
    Amitriptyline hydrochloride
  • HY-D2335

    Fluorescent Dye Neurological Disease
    SERTlight is a fluorescent agent that can specifically label serotonergic neuronal cell bodies, dendrites, and axonal projections as fluorescent substrates of the serotonin transporter (SERT). SERTlight is orthogonal to various genetically encoded sensors in terms of optics, pharmacology, and operation, enabling multiple imaging. SERTlight allows the use of GRAB5HT sensors to label distal 5HT axonal projections and simultaneously image the release of endogenous 5HT, providing a new multifunctional molecular tool for studying serotonergic systems .
    SERTlight
  • HY-116594A

    Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity .
    OPC-14523 hydrochloride
  • HY-17385
    Atomoxetine hydrochloride
    4 Publications Verification

    Tomoxetine hydrochloride; (R)-Tomoxetine hydrochloride; LY 139603

    Adrenergic Receptor Serotonin Transporter Sodium Channel Neurological Disease Cancer
    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 hydrochloride
  • HY-168021

    Monoamine Oxidase Serotonin Transporter Neurological Disease
    MAO-A/SERT-IN-1 is an inhibitor of MAO-A/serotonin transporter (SERT). MAO-A/SERT-IN-1 can reduce SERT-mediated reuptake of 5-HT and has neuroprotective effects in cell inhibition models. MAO-A/SERT-IN-1 can improve depressive behavior in zebrafish and mice .
    MAO-A/SERT-IN-1
  • HY-B0527AS

    Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor Neurological Disease
    Amitriptyline-d6 (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].
    Amitriptyline-d6 hydrochloride
  • HY-135096

    Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor Neurological Disease
    Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .
    Amitriptyline-d3 hydrochloride
  • HY-116594

    Sigma Receptor 5-HT Receptor Neurological Disease
    OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity .
    OPC-14523 free base
  • HY-B0602S2

    Isotope-Labeled Compounds Serotonin Transporter Neurological Disease
    Desvenlafaxine-d6 is deuterium labeled Desvenlafaxine. 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[1][2].
    Desvenlafaxine-d6
  • HY-B0602S3

    Isotope-Labeled Compounds Serotonin Transporter Neurological Disease
    Desvenlafaxine-d10 is deuterium labeled Desvenlafaxine. 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[1][2].
    Desvenlafaxine-d10
  • HY-B0527AR
    Amitriptyline hydrochloride (Standard)
    4 Publications Verification

    Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Sodium Channel Trk Receptor Neurological Disease Cancer
    Amitriptyline (hydrochloride) (Standard) is the analytical standard of Amitriptyline (hydrochloride). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .
    Amitriptyline hydrochloride (Standard)
  • HY-N0749

    Cholinesterase (ChE) 5-HT Receptor Bacterial Neurological Disease
    Jatrorrhizine is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities . Jatrorrhizine is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE . Jatrorrhizine reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters .
    Jatrorrhizine
  • HY-N0740
    Jatrorrhizine chloride
    1 Publications Verification

    Cholinesterase (ChE) 5-HT Receptor Bacterial Neurological Disease Inflammation/Immunology
    Jatrorrhizine chloride is an alkaloid isolated from?Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities . Jatrorrhizine chloride is a potent and orally active inhibitor of?AChE?(IC50=872 nM) over >115-fold selectivity for BuChE . Jatrorrhizine chloride reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters .
    Jatrorrhizine chloride
  • HY-B0602

    O-Desmethylvenlafaxine

    Serotonin Transporter Neurological Disease
    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
  • HY-N0749A
    Jatrorrhizine hydroxide
    1 Publications Verification

    Cholinesterase (ChE) 5-HT Receptor Bacterial Neurological Disease Inflammation/Immunology
    Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities . Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE . Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters .
    Jatrorrhizine hydroxide
  • HY-107370

    Tomoxetine; (R)-Tomoxetine

    Serotonin Transporter Sodium Channel Neurological Disease Cancer
    Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with Ki values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DAEX and NEEX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na + channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research .
    Atomoxetine
  • HY-17385R

    Adrenergic Receptor Serotonin Transporter Sodium Channel Neurological Disease Cancer
    Atomoxetine (hydrochloride) (Standard) is the analytical standard of Atomoxetine (hydrochloride). This product is intended for research and analytical applications. 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 hydrochloride (Standard)
  • HY-16170

    O-Desmethylvenlafaxine succinate; Wy-45233 succinate

    Serotonin Transporter Neurological Disease Metabolic Disease
    Desvenlafaxine succinate, 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 (DVS) shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter .
    Desvenlafaxine succinate
  • HY-B0602A

    O-Desmethylvenlafaxine succinate hydrate; Desvenlafaxine succinate monohydrate

    Serotonin Transporter Neurological Disease
    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-100057

    6-Hydroxybuspirone; 6'-Hydroxybuspirone; BMS 528215

    5-HT Receptor Dopamine Receptor Neurological Disease
    BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone. It is formed from buspirone via the cytochrome P450 (CYP) isozyme CYP3A4.4. BMY 28674 binds to the serotonin (5-HT) receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe (EC50s are 4 and 1 μM, respectively) and is an antagonist of dopamine D2, D3, and D4 receptors (IC50s are 3.1, 4.9, and 0.85 μM, respectively). It also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner.
    BMY 28674
  • HY-N0740R

    Cholinesterase (ChE) 5-HT Receptor Bacterial Neurological Disease Inflammation/Immunology
    Jatrorrhizine (chloride) (Standard) is the analytical standard of Jatrorrhizine (chloride). This product is intended for research and analytical applications. Jatrorrhizine chloride is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities . Jatrorrhizine chloride is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE . Jatrorrhizine chloride reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters .
    Jatrorrhizine chloride (Standard)
  • HY-14261
    Vilazodone Hydrochloride
    4 Publications Verification

    EMD 68843 Hydrochloride; SB659746A Hydrochloride

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
    Vilazodone Hydrochloride
  • HY-15414
    Vortioxetine
    5+ Cited Publications

    Lu AA 21004

    5-HT Receptor Serotonin Transporter Neurological Disease Cancer
    Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
    Vortioxetine
  • HY-15414A
    Vortioxetine hydrobromide
    5+ Cited Publications

    Lu AA21004 hydrobromide

    5-HT Receptor Serotonin Transporter Neurological Disease Cancer
    Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
    Vortioxetine hydrobromide
  • HY-15414R

    5-HT Receptor Serotonin Transporter Neurological Disease Cancer
    Vortioxetine (Standard) is an analytical standard for Vortioxetine. This product is intended for research and analytical applications. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
    Vortioxetine (Standard)
  • HY-14261R

    5-HT Receptor Serotonin Transporter Neurological Disease
    Vilazodone (Hydrochloride) (Standard) is the analytical standard of Vilazodone (Hydrochloride). This product is intended for research and analytical applications. Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
    Vilazodone Hydrochloride (Standard)
  • HY-15414AS

    Lu AA21004-d8 hydrobromide

    Isotope-Labeled Compounds 5-HT Receptor Serotonin Transporter Neurological Disease
    Vortioxetine-d8 (Lu AA 21004-d8) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
    Vortioxetine-d8 hydrobromide
  • HY-15414S

    Lu AA 21004 d8

    Isotope-Labeled Compounds 5-HT Receptor Serotonin Transporter Neurological Disease
    Vortioxetine-d8 (Lu AA 21004-d8) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .
    Vortioxetine-d8
  • HY-15414S1

    Lu AA 21004-d6

    Serotonin Transporter 5-HT Receptor Isotope-Labeled Compounds Neurological Disease Cancer
    Vortioxetine-d6 (Lu AA 21004-d6) is the deuterium labeled Vortioxetine (HY-B1490A). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM) .
    Vortioxetine-d6
  • HY-A0139

    NSC 108165; Navan; Navane

    Others Others
    Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
    Thiothixene
  • HY-111419

    Serotonin Transporter 5-HT Receptor Neurological Disease
    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-111419A

    Serotonin Transporter 5-HT Receptor Neurological Disease
    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-W052508

    N-Desalkylquetiapine

    5-HT Receptor Neurological Disease
    Norquetiapine is an antidepressant and neuroprotective agent and is the active metabolic component of Quetiapine (HY-14544). Norquetiapine is also a partial 5-HT1A receptor agonist, and a presynaptic α2, 5-HT2C and 5-HT7 b> Receptor antagonist. Norquetiapine can also selectively inhibit norepinephrine transporter (NET), inhibit norepinephrine reuptake, and has potential inhibitory effects on bipolar depression, major depressive disorder, and generalized anxiety disorder. Norquetiapine demonstrated in vivo activity in forced swimming in mice and learned helplessness tests in rats .
    Norquetiapine
  • HY-120464

    SAM-760

    5-HT Receptor Neurological Disease
    PF-05212377 (SAM-760) is an inhibitor for serotonin receptor 5-HT6. PF-05212377 is a substrate for P-gp/non-BCRP human transporter. PF-05212377 exhibits blood brain barrier permeability in non-human primates. PF-05212377 can be used for Alzheimer’s Disease research .
    PF-05212377
  • HY-14348

    5-HT Receptor Dopamine Receptor Neurological Disease
    GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK163090 has antidepressant and anxiolytic activities .
    GSK163090
  • HY-149170

    5-HT Receptor Monoamine Transporter Neurological Disease
    FFN246 is a fluorescent, dual substrate of serotonin transporter (SERT) probe and vesicular monoamine transporter 2 (VMAT2) with excitation and emission spectra 392/427 nm. FFN246 can be used for labeling serotonergic neurons in mouse brain tissue through SERT-dependent accumulation .
    FFN246
  • HY-109067

    VVZ-149

    GlyT 5-HT Receptor P2X Receptor Neurological Disease
    Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain .
    Opiranserin
  • HY-109067A

    VVZ-149 hydrochloride

    GlyT 5-HT Receptor P2X Receptor Neurological Disease
    Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain .
    Opiranserin hydrochloride

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