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Pathways Recommended:	Membrane Transporter/Ion Channel

Results for "

5-HT Transporters Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (18) Adenylate Cyclase (2) Adrenergic Receptor (5) Bacterial (4) Cholinesterase (ChE) (3) Dopamine Receptor (3) Dopamine Transporter (1) Histamine Receptor (4) mAChR (4) Phosphodiesterase (PDE) (1) Serotonin Transporter (13) Sodium Channel (6) Trk Receptor (4)
By Research Areas:	Cancer (4) Inflammation/Immunology (2) Neurological Disease (22)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: 5-HT Receptor GlyT

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B1272

Desipramine hydrochloride Maximum Cited Publications 10 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 K_is of 4, 61 and 78,720 nM, respectively.

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-110289

(R)-Citalopram oxalate	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 .

HY-103089

LY393558	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 .

HY-129985

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

HY-121162

Mesembrine (+)-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 K_i of 1.4 nM. Mesembrine also inhibits phosphodiesterase 4B (PDE4B) with an IC₅₀ of 7.8 μM .

HY-B0527A

Amitriptyline hydrochloride 3 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 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	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].

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-17385

Atomoxetine hydrochloride 3 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 K_i 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 .

HY-B0527AR

Amitriptyline hydrochloride (Standard)	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 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-N0749

Jatrorrhizine	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 .

HY-N0740

Jatrorrhizine chloride	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 .

HY-B1213

Trimipramine maleate	5-HT Receptor Bacterial	Neurological Disease
Trimipramine maleate is a 5-HT receptor antagonist, with pK_i binding values of 6.39, 8.10, 4.66 for 5-HT_1C, 5-HT₂ and 5-HT_1A, 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 .

HY-B1213A

Trimipramine
Trimipramine is a 5-HT receptor antagonist, with pK_i binding values of 6.39, 8.10, 4.66 for 5-HT_1C, 5-HT₂ and 5-HT_1A, 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 .

HY-N0749A

Jatrorrhizine hydroxide	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 .

HY-107370

Atomoxetine Tomoxetine; (R)-Tomoxetine	Serotonin Transporter Sodium Channel	Neurological Disease
Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with K_i values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DA_EX and NE_EX 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 .

HY-14261

Vilazodone Hydrochloride 3 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-HT_1A* receptor partial agonist.

HY-111419

DSP-1053	Serotonin Transporter 5-HT Receptor	Neurological Disease
DSP-1053, a benzylpiperidine derivative, is a potent Serotonin Transporter (SERT) inhibitor with a K_i of 1.02 nM. DSP-1053 shows partial 5-HT_1A receptor agonistic activity with a K_i of 5.05 nM. DSP-1053 has antidepressant activity .

HY-111419A

DSP-1053 benzenesulfonate	Serotonin Transporter 5-HT Receptor	Neurological Disease
DSP-1053, a benzylpiperidine derivative, is a potent *serotonin transporter* (SERT)** inhibitor with a K_i of 1.02 nM. DSP-1053 shows partial 5-HT_1A receptor agonistic activity with a K_i of 5.05 nM. DSP-1053 has antidepressant activity .

HY-14348

GSK163090	5-HT Receptor Dopamine Receptor	Neurological Disease
GSK163090 is a potent, selective and orally active 5-HT_1A/1B/1D receptor antagonist with pK_i values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pK_i value of 6.1. GSK163090 has antidepressant and anxiolytic activities .

HY-103430

SKF-83566 hydrobromide	Dopamine Receptor 5-HT Receptor Adenylate Cyclase	Neurological Disease
SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT₂ receptor (K_i=11 nM) . SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC₅₀ of 5.7 μM . SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC₂) over AC₁ and AC₅ in the isolated rabbit thoracic aorta . SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation .

HY-103430A

SKF-83566 1 Publications Verification	Dopamine Receptor 5-HT Receptor Adenylate Cyclase	Neurological Disease
SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT₂ receptor (K_i=11 nM) . SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC₅₀ of 5.7 μM . SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC₁ and AC₅ in the isolated rabbit thoracic aorta . SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0740

Jatrorrhizine chloride	Alkaloids Monophenols Source classification Ranunculaceae Coptis chinensis Franch. Phenols Plants Isoquinoline Alkaloids	Cholinesterase (ChE) 5-HT Receptor Bacterial
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 .

HY-N0749A

Jatrorrhizine hydroxide	Alkaloids Monophenols Source classification Ranunculaceae Coptis chinensis Franch. Phenols Plants Isoquinoline Alkaloids	Cholinesterase (ChE) 5-HT Receptor Bacterial
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 .

HY-121162

Mesembrine (+)-Mesembrine	Alkaloids other families Pyrrole Alkaloids Source classification Plants	5-HT Receptor Phosphodiesterase (PDE)
Mesembrine ((+)-Mesembrine) a main alkaloid that features an aryloctahydroindole skeleton. Mesembrine is a **5-HT transporter** inhibitor with a K_i of 1.4 nM. Mesembrine also inhibits phosphodiesterase 4B (PDE4B) with an IC₅₀ of 7.8 μM .

HY-N0749

Jatrorrhizine	Alkaloids Monophenols other families Source classification Phenols Plants Isoquinoline Alkaloids	Cholinesterase (ChE) 5-HT Receptor Bacterial
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 .

Cat. No.	Product Name	Chemical Structure

HY-B0527AS

Amitriptyline-d6 hydrochloride
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

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].

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