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DAT/NET/SERT

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30

Inhibitors & Agonists

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5

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0527A
    Amitriptyline hydrochloride
    Maximum Cited Publications
    8 Publications Verification

    		 Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    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
  • HY-B0527
    Amitriptyline
    Maximum Cited Publications
    8 Publications Verification

    		 Serotonin Transporter Trk Receptor Sodium Channel 5-HT Receptor Histamine Receptor Adrenergic Receptor mAChR Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline 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 is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline 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 can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
    Amitriptyline
  • HY-19907
    Liafensine

    BMS-820836

    		 Dopamine Transporter Monoamine Transporter Serotonin Transporter Neurological Disease
    Liafensine (BMS-820836) is an orally active, blood-brain barrier-permeable monoamine reuptake inhibitor, with an IC50 of 5.67 nM against DAT, 1.08 nM against SERT, and 7.99 nM against NET. Liafensine binds to DAT to block dopamine reuptake. Liafensine binds to SERT to block serotonin reuptake. Liafensine binds to NET to block norepinephrine reuptake. Liafensine can be used in studies related to depression .
    Liafensine
  • HY-133116
    4-Hydroxyatomoxetine

    		Adrenergic Receptor Neurological Disease
    4-Hydroxyatomoxetine is an active metabolite of Atomoxetine. 4-Hydroxyatomoxetine is metabolized by the enzyme cytochrome P450 2D6 (CYP2D6). Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
    4-Hydroxyatomoxetine
  • HY-N7506
    13-Hydroxyisobakuchiol

    Delta3,2-Hydroxylbakuchiol

    		 Monoamine Transporter Dopamine Transporter Neurological Disease
    13-Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) that can be isolated from Psoralea corylifolia (L.), is a potent selective monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC50 = 0.58 μM) and norepinephrine transporter (NET) (IC50 = 0.69 μM) than for the serotonin transporter (SERT) (IC50 = 312.02 μM). 13-Hydroxyisobakuchiol increases the activity of intact mice and improves the decreased activity of reserpinized mice in vivo. 13-Hydroxyisobakuchiol can be used for the research of disorders such as Parkinson's disease and depression .
    13-Hydroxyisobakuchiol
  • HY-B0527AR
    Amitriptyline hydrochloride (Standard)
    4 Publications Verification

    		 Reference Standards Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    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-135096
    Amitriptyline-d3 hydrochloride

    		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-B0527AS
    Amitriptyline-d6 hydrochloride

    		Isotope-Labeled Compounds Serotonin Transporter 5-HT Receptor Histamine Receptor mAChR Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    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-d6 hydrochloride
  • HY-178907
    SERT/5-HT-IN-1

    		Serotonin Transporter 5-HT Receptor Neurological Disease
    SERT/5-HT-IN-1 (compound D17) is an orally active and potent dual target inhibitor of SERT/5-HT3A (SERT IC50 = 1.5 nM, NET IC50 = 49 nM, DAT IC50 = 91 nM, 5-HT3A Ki = 12 nM). SERT/5-HT-IN-1 has an IC50 of 39 nM to 5-HT3A. SERT/5-HT-IN-1 has a lower risk of liver, kidney, and cardiac toxicity. SERT/5-HT-IN-1 can be used for research on depressive disorders .
    SERT/5-HT-IN-1
  • HY-W703376
    2-(tert-Butylamino)-1-phenylpropan-1-one hydrochloride

    		Serotonin Transporter Monoamine Transporter Dopamine Transporter Neurological Disease
    2-(tert-Butylamino)-1-phenylpropan-1-one hydrochloride (Compound Imp.1) is a non-selective monoamine transporter (DAT/NET/SERT) agonist. tert-Butylcathinone hydrochloride is promising for research of depressive disorders .
    2-(tert-Butylamino)-1-phenylpropan-1-one hydrochloride
  • HY-126158
    SRI-29574

    		Dopamine Transporter Serotonin Transporter Neurological Disease
    SRI-29574 is an allosteric modulator of the dopamine transporter (DAT). SRI-29574 partially inhibits the uptake of the DAT (IC50=2.3 nM) and also partially inhibits the uptake of the serotonin transporter (SERT) and norepinephrine transporter (NET). SRI-29574 may serve as a useful probe to study the function and regulatory mechanisms of DAT .
    SRI-29574
  • HY-172421
    Cendifensine

    		Monoamine Transporter Serotonin Transporter Dopamine Transporter Neurological Disease
    Cendifensine is the inhibitor for monoamine reuptake that inhibits the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT) .
    Cendifensine
  • HY-107128
    Ampreloxetine hydrochloride

    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-B0457S
    Clomipramine-d3 hydrochloride

    Chlorimipramine-d3 hydrochloride; G-34586-d3 hydrochloride; NSC-169865-d3 hydrochloride

    		 Serotonin Transporter Dopamine Receptor Neurological Disease
    Clomipramine-d3 (hydrochloride) is a deuterium labeled Clomipramine hydrochloride. Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively .
    Clomipramine-d3 hydrochloride
  • HY-B0457AS
    Clomipramine-d3

    Chlorimipramine-d3; G-34586-d3; NSC-169865-d3

    		 Isotope-Labeled Compounds Serotonin Transporter Dopamine Receptor Neurological Disease
    Clomipramine-d3 is the deuterium labeled Clomipramine. Clomipramine is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively .
    Clomipramine-d3
  • HY-107370AS
    (Rac)-Atomoxetine-d7 hydrochloride

    (Rac)-Tomoxetine d7 hydrochloride; (Rac)-LY 139603 d7

    		 Serotonin Transporter Sodium Channel Isotope-Labeled Compounds Neurological Disease
    (Rac)-Atomoxetine-d7 (hydrochloride) is a deuterium labeled (Rac)-Atomoxetine hydrochloride. (Rac)-Atomoxetine hydrochloride is a racemic form of Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
    (Rac)-Atomoxetine-d7 hydrochloride
  • HY-173398
    NMDAR antagonist 5

    		iGluR Monoamine Transporter Serotonin Transporter Dopamine Transporter Neurological Disease
    NMDAR antagonist 5 (Compound A17) is a multi-target antagonist against NMDAR and monoamine transporters (SERT、DAT and NET). NMDAR antagonist 5 shows good NMDAR antagonistic potency (IC50 = 0.3 μM) and monoamine transporter activities (SERT IC50 = 1.1 μM、DAT IC50 = 0.7 μM、NET IC50 = 2.7 μM). NMDAR antagonist 5 is highly safe and has low toxicity (hepatotoxicity and nephrotoxicity (IC50 > 100 μM); cardiotoxicity (IC50 = 24.5 μM)). NMDAR antagonist 5 has antidepressant effects and can be used in the study of depression .
    NMDAR antagonist 5
  • HY-18332B
    DOV-102,677

    		Dopamine Transporter Adrenergic Receptor 5-HT Receptor Neurological Disease
    DOV-102,677 is an orally sctive triple monoamine neurotransmitter reuptake inhibitor that simultaneously inhibits the dopamine (DAT) (IC50 = 129 nM; Ki = 222 nM), norepinephrine (NET) (IC50 = 103 nM; Ki = 1030 nM), and serotonin (SERT) (IC50 = 133 nM; Ki = 740 nM) transporters. DOV-102,677 demonstrated significant antidepressant-like activity and sensory-motor gating regulatory effects in mouse experiments. DOV-102,677 can be used for research on depression .
    DOV-102,677
  • HY-162585
    5-HT1AR agonist 1

    		5-HT Receptor Neurological Disease
    5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including 5-HT1AR agonist with an EC50 value of 34 nM, SERT reuptake ihibitor (IC50 =12 nM), NET reuptake inhibitor (IC50 =78 nM) and DAT reuptake inhibitor (IC50 =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs .
    5-HT1AR agonist 1
  • HY-172029
    3,4-Methylenedioxy pyrovalerone metabolite 2 hydrochloride

    		Monoamine Transporter Neurological Disease
    3,4-Methylenedioxy pyrovalerone metabolite 2 hydrochloride is an analog of Pyrovalerone. Pyrovalerone inhibits the dopamine transporter (DAT)，serotonin transporter (SERT)，and the norepinephrine transporter (NET) .
    3,4-Methylenedioxy pyrovalerone metabolite 2 hydrochloride
  • HY-110223
    Atomoxetine-d3 hydrochloride

    		Adrenergic Receptor Neurological Disease
    Atomoxetine-d3 hydrochloride is the deuterium labeled Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
    Atomoxetine-d3 hydrochloride
  • HY-17385S
    Atomoxetine-d5 hydrochloride

    Tomoxetine-d5 hydrochloride; LY 139603-d5 ; (R)-Tomoxetine-d5 hydrochloride

    		 Isotope-Labeled Compounds Adrenergic Receptor Neurological Disease
    Atomoxetine-d5 (hydrochloride) is the deuterium labeled Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .
    Atomoxetine-d5 hydrochloride
  • HY-116062A
    JNJ-7925476

    		Histone Methyltransferase Neurological Disease
    JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
    JNJ-7925476
  • HY-108513
    σ1 Receptor antagonist 4

    		Sigma Receptor Neurological Disease
    σ1 Receptor antagonist 4 (compound TC1) is a selective sigma1 (σ1) receptor antagonist with a Ki of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (Ki of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters .
    σ1 Receptor antagonist 4
  • HY-117542
    D595

    		Histone Methyltransferase Neurological Disease
    D595 is a phenylethylamine calcium channel blocker with potent negative inotropic activity. D595 has shown significant efficacy in its corresponding pharmacological studies, especially in inhibiting the uptake of monoamine neurotransmitters. D595 has high affinity in binding to the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET). Structural adjustments of D595, especially changes in the hydroxyl stereochemistry, significantly affect its interaction with the transporters, showing a specific preference for stereoisomers .
    D595
  • HY-172763
    EDMA hydrochloride

    		Drug Derivative Serotonin Transporter Dopamine Transporter 5-HT Receptor Neurological Disease
    EDMA hydrochloride is a derivative of MDMA. EDMA hydrochloride is a substrate for multiple neurotransmitter transporters, including serotonin transporter (SERT), dopamine transporter (DAT), and norepinephrine transporter (NET). EDMA hydrochloride has 5-HT releasing activity at SERT (EC50 = 117 nM) and MPP + releasing activity at DAT (EC50 = 597 nM) and NET (EC50 = 325 nM) .
    EDMA hydrochloride
  • HY-W680886
    6-APDB

    		Monoamine Transporter Serotonin Transporter Dopamine Transporter 5-HT Receptor Neurological Disease
    6-APDB is a class of monoamine neurotransmitter releaser and Monoamine Transporter modulator that exerts selective effects on human monoamine transporters and acts as a partial agonist at 5-HT2 family receptors. For NET, 6-APDB has an IC50 of 0.56 μM and a Ki of 18 μM; for SERT, it has an IC50 of 2.3 μM and a Ki of 23 μM; for DAT, it has an IC50 of 33 μM and a Ki of >30 μM, and affinity for rat and mouse TAAR1, with Ki values of 1.0 μM and 0.21 μM, respectively. 6-APDB inhibits norepinephrine and 5-HT reuptake, mediates the release of three types of monoamine neurotransmitters, shows a dose-dependent biphasic locomotor effect in mice, and fully substitutes the discriminative stimulus effect of MDMA. 6-APDB shows no significant cytotoxicity at high concentrations, and possesses empathogenic psychoactivity, potential hallucinogenic effects, and behavioral effects associated with intermittent abuse .
    6-APDB
  • HY-107128R
    Ampreloxetine hydrochloride (Standard)

    TD-9855 hydrochloride (Standard)

    		 Reference Standards Serotonin Transporter Neurological Disease
    Ampreloxetine hydrochloride (Standard) (TD-9855 hydrochloride (Standard)) is the analytical standard of Ampreloxetine (hydrochloride) (HY-107128). This product is intended for research and analytical applications. 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 (Standard)
  • HY-186169B
    (R,S)-MDDMA

    		Serotonin Transporter Dopamine Transporter Neurological Disease
    (R,S)-MDDMA is an MDMA analog that lacks the psychostimulant effects of its parent compound. (R,S)-MDDMA still retains partial serotonin-releasing activity .
    (R,S)-MDDMA
  • HY-181828
    SePP

    		iGluR Dopamine Receptor Neurological Disease
    SePP is a blood-brain barrier-permeable NMDAR antagonist and dopamine/norepinephrine reuptake inhibitor, with a Ki of 28.7 nM for rat NMDAR. SePP exerts anticonvulsant effects. SePP can be used in research related to fragile X syndrome .
    SePP

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