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NET/SERT

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Serotonin Transporter (28) 5-HT Receptor (12) Adrenergic Receptor (9) Akt (4) Aminotransferases (Transaminases) (1) Apoptosis (4) Dopamine Receptor (3) Dopamine Transporter (14) Drug Derivative (1) Histamine Receptor (5) Histone Methyltransferase (2) iGluR (2) Isotope-Labeled Compounds (6) mAChR (5) Monoamine Transporter (8) mTOR (4) P-glycoprotein (4) PI3K (4) Potassium Channel (4) Reference Standards (4) Sigma Receptor (1) Sodium Channel (6) Trk Receptor (9)
By Research Areas:	Endocrinology (5) Inflammation/Immunology (9) Metabolic Disease (4) Neurological Disease (39)

By Targets:

Serotonin Transporter (28)

5-HT Receptor (12)

Adrenergic Receptor (9)

Akt (4)

Aminotransferases (Transaminases) (1)

Apoptosis (4)

Dopamine Receptor (3)

Dopamine Transporter (14)

Drug Derivative (1)

Histamine Receptor (5)

Histone Methyltransferase (2)

iGluR (2)

Isotope-Labeled Compounds (6)

mAChR (5)

Monoamine Transporter (8)

mTOR (4)

P-glycoprotein (4)

PI3K (4)

Potassium Channel (4)

Reference Standards (4)

Sigma Receptor (1)

Sodium Channel (6)

Trk Receptor (9)

By Research Areas:

Endocrinology (5)

Inflammation/Immunology (9)

Metabolic Disease (4)

Neurological Disease (39)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Serotonin Transporter

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* (K_i = 3.45 nM) and *NET* (K_i = 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 K_i = 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) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 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 .

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* (K_i = 3.45 nM) and *NET* (K_i = 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 K_i = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 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 .

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 .

HY-B0168B

Levomilnacipran hydrochloride 1 Publications Verification (1S,2R)-Milnacipran hydrochloride; F-2695 hydrochloride	Serotonin Transporter Trk Receptor PI3K Akt mTOR P-glycoprotein	Neurological Disease Inflammation/Immunology
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 K_i 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 .

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 (K_i values are 5 nM, 77 nM and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .

HY-135615A

Desmethyl Sibutramine hydrochloride N-Desmethylsibutramine hydrochloride	Serotonin Transporter	Neurological Disease Metabolic Disease
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 .

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 .

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* (K_i = 3.45 nM) and *NET* (K_i = 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 K_i = 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) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 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.

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 K_is 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 K_i 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 .

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* (K_i = 3.45 nM) and *NET* (K_i = 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 K_i = 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) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 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.

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 .

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 K_i = 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 .

HY-156807

LY 367265	Serotonin Transporter 5-HT Receptor	Neurological Disease
LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder .

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 .

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) .

HY-182244

SERT/NET-IN-1	Serotonin Transporter 5-HT Receptor	Endocrinology
SERT/NET-IN-1 is a blood-brain barrier-permeable *SERT* and *NET* inhibitor, with an IC₅₀ of 11.2 nM against human *SERT* and an IC₅₀ of 32.0 nM against human *NET. SERT/NET-IN-1 blocks 5-HT reuptake to enhance serotonergic signaling. SERT/NET-IN-1 also blocks norepinephrine reuptake to enhance central noradrenergic transmission and inhibits the ejaculatory reflex. SERT/NET-IN-1 prolongs ejaculatory latency, reduces ejaculation frequency and preserves sexual function. SERT/NET-IN-1 exhibits cross-species microsomal metabolic stability, shows acceptable oral brain exposure in rats, and has favorable safety profiles. SERT/NET*-IN-1 can be used in studies related to premature ejaculation .

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 K_i of 0.14, 54 and 3 nM, respectively .

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 K_i of 0.14, 54 and 3 nM, respectively .

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; K_i = 222 nM), norepinephrine (NET) (IC₅₀ = 103 nM; K_i = 1030 nM), and serotonin (SERT) (IC₅₀ = 133 nM; K_i = 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 .

HY-14794A

Levomilnacipran (1S,2R)-Milnacipran; F2695	Serotonin Transporter Trk Receptor PI3K mTOR P-glycoprotein Akt	Neurological Disease Inflammation/Immunology
Levomilnacipran ((1S,2R)-Milnacipran) is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran is a serotonin and norepinephrine reuptake inhibitor, with IC₅₀ values of 10.5 nM and 19.0 nM, and K_i values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression .

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 .

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) .

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 .

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 .

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) .

HY-135615

Desmethyl Sibutramine N-Desmethylsibutramine	Serotonin Transporter	Neurological Disease Metabolic Disease
Desmethyl Sibutramine, the secondary metabolite of Sibutramine, is an orally active norepinephrine transporter (NET) and serotonin transporter (SERT) inhibitor. Desmethyl Sibutramine can be used in the research of obesity and appetite suppressant .

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 (K_i values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively) .

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) .

HY-135615AR

Desmethyl Sibutramine hydrochloride (Standard) N-Desmethylsibutramine hydrochloride (Standard)	Reference Standards Serotonin Transporter	Neurological Disease Metabolic Disease
Desmethyl Sibutramine (hydrochloride) (Standard) is the analytical standard of Desmethyl Sibutramine (hydrochloride). This product is intended for research and analytical applications. 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 .

HY-121212R

Icosabutate (Standard)	Aminotransferases (Transaminases) Reference Standards Others	Metabolic Disease Inflammation/Immunology
Desmethyl Sibutramine (hydrochloride) (Standard) is the analytical standard of Desmethyl Sibutramine (hydrochloride). This product is intended for research and analytical applications. 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 .

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 .

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 K_i of 10 nM. σ1 Receptor antagonist 4 is weakly active at σ2 receptor (K_i of 370 nM) and has no activity at dopamine (DAT), serotonin (SERT), and norepinephrine (NET) transporters .

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 .

HY-14794AS

Levomilnacipran-d10 hydrochloride (1S,2R)-Milnacipran-d10 hydrochloride; F2695-d10 hydrochloride	Isotope-Labeled Compounds Serotonin Transporter Trk Receptor PI3K mTOR P-glycoprotein Akt	Neurological Disease Inflammation/Immunology
Levomilnacipran-d₁₀ ((1S,2R)-Milnacipran-d₁₀) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). 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 K_i 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 .

HY-B0168BS

Levomilnacipran-d5 hydrochloride (1S,2R)-Milnacipran-d5 hydrochloride; F-2695-d5 hydrochloride	Isotope-Labeled Compounds Serotonin Transporter Trk Receptor PI3K Akt mTOR P-glycoprotein	Neurological Disease Inflammation/Immunology
Levomilnacipran-d5 ((1S,2R)-Milnacipran-d5) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). 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 K_i 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 .

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) .

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 .

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 K_i of 18 μM; for *SERT, it has an IC₅₀* of 2.3 μM and a K_i of 23 μM; for DAT, it has an IC₅₀ of 33 μM and a K_i of >30 μM, and affinity for rat and mouse TAAR1, with K_i 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 .

HY-179568

F3288-0031	Monoamine Transporter	Neurological Disease
F3288-0031 is a brain-penetrant norepinephrine transporter (NET) allosteric inhibitor with inhibitory rates of 73.5% at 20 μM. F3288-0031 binds within the inner vestibule of *NET, stabilizing the inward-open state and has a preferential NET/SERT* inhibition with pIC₅₀ = 5.9. F3288-0031 shows no detectable off-target functional activity in vitro. F3288-0031 demonstrates robust antidepressant-like efficacy in vivo without confounding locomotor effects, F3288-0031 can be used for depressive disorder and related neuropsychiatric conditions .

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 .

HY-181828

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

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N7506

13-Hydroxyisobakuchiol Delta3,2-Hydroxylbakuchiol	Structural Classification Monophenols Leguminosae Phenols Psoralea corylifolia L. Plants Source Classification	Monoamine Transporter Dopamine Transporter
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 .

Cat. No.	Product Name	Chemical Structure

HY-B0527AS

Amitriptyline-d6 hydrochloride
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* (K_i = 3.45 nM) and *NET* (K_i = 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 K_i = 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) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 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

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 (K_i = 3.45 nM) and NET (K_i = 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 K_i = 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) (K_i = 11-24 nM), H1 receptors (K_i = 0.5-1.1 nM), adrenergic α1 receptors (K_i = 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.

HY-B0457S

Clomipramine-d3 hydrochloride
Clomipramine-d₃ (hydrochloride) is a deuterium labeled Clomipramine hydrochloride. Clomipramine hydrochloride is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with K_i of 0.14, 54 and 3 nM, respectively .

HY-B0457AS

Clomipramine-d3
Clomipramine-d₃ is the deuterium labeled Clomipramine. Clomipramine is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with K_i of 0.14, 54 and 3 nM, respectively .

HY-107370AS

(Rac)-Atomoxetine-d7 hydrochloride
(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) .

HY-17385S

Atomoxetine-d5 hydrochloride
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) .

HY-14794AS

Levomilnacipran-d10 hydrochloride

Levomilnacipran-d₁₀ ((1S,2R)-Milnacipran-d₁₀) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). 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 K_i 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 .

HY-B0168BS

Levomilnacipran-d5 hydrochloride

Levomilnacipran-d5 ((1S,2R)-Milnacipran-d5) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). 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 K_i 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 .

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