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Pathways Recommended:	Membrane Transporter/Ion Channel

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rat serotonin transporters

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By Targets:	5-HT Receptor (4) Serotonin Transporter (3) Akt (1) Aldose Reductase (1) Cytochrome P450 (1) Dopamine Receptor (2) Dopamine Transporter (1) Drug Metabolite (1) Histone Methyltransferase (2) Monoamine Oxidase (1) Prostaglandin Receptor (1)
By Research Areas:	Cancer (1) Cardiovascular Disease (1) Inflammation/Immunology (1) Neurological Disease (8)

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Targets Recommended: Nucleoside Transporters GlyT ATP-binding cassette (ABC) transporters 5-HT Receptor Serotonin Transporter ASCT

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-110023

Zimelidine dihydrochloride	Serotonin Transporter	Neurological Disease
Zimelidine dihydrochloride is an orally active selective serotonin reuptake inhibitor. Zimelidine dihydrochloride competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine dihydrochloride time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine dihydrochloride strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine dihydrochloride exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine dihydrochloride is used for the study of depressive disorders and analgesic tolerance .

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-10427

WAY-260022 NRI-022	Histone Methyltransferase	Neurological Disease
WAY-260022 is a selective norepinephrine reuptake inhibitor with potent inhibitory activity on norepinephrine reuptake. WAY-260022 exhibits excellent selectivity in inhibiting serotonin and dopamine transporters. WAY-260022 also showed oral efficacy in a rat model of thermoregulatory dysfunction .

HY-100057

BMY 28674 6-Hydroxybuspirone; 6'-Hydroxybuspirone; BMS 528215	5-HT Receptor Drug Metabolite Dopamine Receptor	Neurological Disease
BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone (HY-B1115A) and is metabolized by 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). BMY 28674 also inhibits *organic cation transporter* 1** (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner.

HY-182247

D-473	Serotonin Transporter Dopamine Transporter	Neurological Disease
D-473 is an orally active, blood-brain barrier penetrant and serotonin-preferring reuptake inhibitor. D-473 inhibits serotonin, dopamine and norepinephrine transporters, and significantly elevates the extracellular levels of these three neurotransmitters in rat brain regions. D-473 exhibits definite antidepressant-like activity without inducing motor activation. D-473 is widely used in studies related to major depressive disorder .

HY-124186

LR1143	Dopamine Receptor 5-HT Receptor	Neurological Disease
LR1143 is a dopamine transporter (DAT) and 5-HT uptake inhibitor, with IC₅₀ values of 3.4 nM and 112 nM in rats, respectively. LR1143 binds to DAT labeled with the dopamine reuptake inhibitor GBR 12935 (HY-12242A), with an IC₅₀ of 4.4 nM. LR1143 shows lower selectivity for DAT than for serotonin reuptake sites. LR1143 can be used in studies related to cocaine abuse .

HY-N18471

5,7-Dihydroxytryptamine 5,7-DHP	Monoamine Oxidase 5-HT Receptor	Cardiovascular Disease Neurological Disease
5,7-Dihydroxytryptamine (5,7-DHP) is an autofluorescent (λ_ex≈365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons .

HY-116811

AZ-11665362	Prostaglandin Receptor Serotonin Transporter Aldose Reductase Cytochrome P450	Inflammation/Immunology
AZ-11665362 is a CRTh2 (DP2) receptor antagonist with an IC₅₀ of 2.6 nM. AZ-11665362 shows weak activity against aldose reductase, **serotonin transporter, CYP 2C19, and CYP 2C9**. AZ-11665362 lacks measurable inhibitory activity against COX-1 and COX-2. AZ-11665362 can be used for the research of asthma, and other inflammatory diseases .

HY-136700

SB-699551 free base	5-HT Receptor Akt	Neurological Disease Cancer
SB-699551 free base is a selective and brain penetrant 5-HT5A receptor antagonist with a pK_i of 8.2 nM. SB-699551 free base shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 free base disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 free base can be used for the research of anxiety, breast cancer, and Alzheimer's disease .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N18471

5,7-Dihydroxytryptamine 5,7-DHP	Structural Classification Alkaloids Animals Indole Alkaloids Source Classification	Monoamine Oxidase 5-HT Receptor
5,7-Dihydroxytryptamine (5,7-DHP) is an autofluorescent (λ_ex≈365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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rat serotonin transporters

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