Dopamine Transporter
DAT; SLC6A3
Dopamine transporter (DAT) is a plasma membrane protein that mediates the reuptake of extracellular dopamine (DA) and controls the spatiotemporal dynamics of dopaminergic neurotransmission. DATs play a key role in terminating dopaminergic signalling and in maintaining a releasable pool of dopamine. DATs help to modulate the concentration of extraneuronal dopamine by actively shuttling released transmitter molecules back across the plasma membrane into dopaminergic neurons, where they can be sequestered for later reuse or enzymatic catabolism.
DAT is a principle target of various psychostimulant, nootropic, and antidepressant drugs, as well as certain drugs used recreationally, including the notoriously addictive stimulant cocaine. DAT ligands have traditionally been divided into two categories: cocaine-like inhibitors and amphetamine-like substrates. DAT is regulated by multiple signaling systems, such as PKC.
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Dopamine Transporter Inhibitors
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Dopamine Transporter Related Products (123)
Related Products (123)
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DAT-IN-1
0 ImagesCat. No.: HY-163138CAS No.: 3033213-24-7DAT-IN-1 (Coumpound 12b) is an atypical DAT inhibitor with a Ki of 8.37 nM. DAT-IN-1 can be used in the study of psychostimulant use disorder (PSUD).
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GBR 12935 fumarate
0 ImagesCat. No.: HY-12242BCAS No.: 1349767-56-1GBR 12935 fumarate is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 fumarate stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 fumarate also prevents the d-Fenfluramine-induced head-twitch response in mice.
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CTDP-32476
0 ImagesCat. No.: HY-123848CAS No.: 928046-68-8CTDP-32476 is a dopamine transporter (DAT) inhibitor with antidepressant activity, exhibiting a Ki value of 12 nM for human DAT and moderate affinity for the norepinephrine transporter (NET). CTDP-32476 blocks DAT to increase extracellular dopamine levels, and induces locomotor stimulation and brain-stimulation reward effects in rats. CTDP-32476 is used in research related to drug addiction.
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CE-103
0 ImagesCat. No.: HY-W1133231CAS No.: 1879038-73-9CE-103 is a selective, blood-brain barrier-permeable dopamine transporter (DAT) inhibitor with an IC50 of 14.73 μM. CE-103 blocks DAT-mediated dopamine reuptake and exhibits antagonistic activity against 5-HT1A. CE-103 reduces working memory errors in the radial arm maze test of rats, decreases the levels of complexes containing phosphorylated DAT (pDAT) and D1R in the hippocampus of rats, and increases the levels of complexes containing D2R and D3R simultaneously. CE-103 can be used in studies related to dopaminergic neurotransmission, working memory and cognitive function.
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Medifoxamine (Standard)
0 ImagesMedifoxamine (Standard) is the analytical standard of Medifoxamine (HY-119468). This product is intended for research and analytical applications. Medifoxamine is an orally active monoamine reuptake inhibitor and antidepressant. Medifoxamine preferentially inhibits presynaptic dopamine reuptake. Medifoxamine acts as an intraocular pressure-lowering agent to reduce intraocular pressure, and also functions as a miotic agent to decrease pupil diameter. Medifoxamine exhibits characteristic properties of antidepressant compounds, including preventing hypothermia induced by Reserpine (HY-N0480) or Apomorphine (HY-12723), potentiating the toxic effects of Yohimbine (HY-N0127) in mice, and reducing immobility behavior in mice and rats in the "behavioral despair" model. Medifoxamine has no anticholinergic activity. Medifoxamine can be used in research related to depression.
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NS2359
0 ImagesCat. No.: HY-120364CAS No.: 195875-68-4Synonyms: GSK372475NS2359 (GSK372475) is a serotonin-norepinephrine-dopamine triple reuptake inhibitor. NS2359 is used for research on depression.
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AC-4-248
0 ImagesCat. No.: HY-161913AC-4-248 is an atypical non-competitive dopamine transporter (DAT) inhibitor and reduces the potency of cocaine to inhibit DAT. AC-4-248 is a non-selective inhibitor of SLC6 transporters with IC50 values for hDAT, hSERT, and hNET of 45.5 μM, 96.2 μM, and 250 μM, respectively.
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AHN 1-055 hydrochloride (Standard)
0 ImagesSynonyms: 3α-Bis-(4-fluorophenyl) Methoxytropane hydrochloride (Standard)AHN 1-055 (hydrochloride) (Standard) is the analytical standard of AHN 1-055 (hydrochloride) (HY-101315). This product is intended for research and analytical applications. AHN 1-055 hydrochloride is a dopamine uptake inhibitor, with an IC50 of 71 nM. AHN 1-055 hydrochloride binds with high affinity to the dopamine transporter (DAT).
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O-2172
0 ImagesCat. No.: HY-169807CAS No.: 521062-92-0O-2172, a carbacyclic analog, is a DAT inhibitor, with IC50 values of 47 nM and 7000 nM for DAT and SERT, respectively.
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UWA-101 hydrochloride
0 ImagesCat. No.: HY-117512CAS No.: 1431520-52-3UWA-101 hydrochloride is a selective and non-cytotoxic DAT/SERT inhibitor, with EC50 values of 3.6 µM and 2.3 µM for inhibiting DAT and SERT, respectively. UWA-101 hydrochloride can alleviate the side effects of dopaminergic agents (such as L-DOPA), such as motor disorders, and lacks psychotropic activity. UWA-101 hydrochloride can be used for research on neurodegenerative diseases such as Parkinson's disease.
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GBR 13098
0 ImagesCat. No.: HY-183482CAS No.: 77862-94-3GBR 13098 is a dopamine transporter inhibitor with a rat IC50 of 43 nM, and exhibits dopaminergic activity in vivo.GBR 13098 selectively blocks dopamine uptake, increasing synaptic dopamine availability, with weaker activity against norepinephrine uptake.GBR 13098 induces ipsilateral circling in lesioned rats and increases locomotor activity in naive mice and habituated rats, with effects attenuated by dopamine receptor antagonism.GBR 13098 reduces DOPA formation in dopamine-rich brain regions and enhances inhibitory responses of substantia nigra zona compacta dopamine neurons to dopamine.GBR 13098 serves as a tool for studying dopaminergic systems.
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Cilobamine methanesulfonate
0 ImagesCat. No.: HY-183457ACAS No.: 69429-85-2Cilobamine methanesulfonate is an orally active antidepressant and a dopamine/norepinephrine reuptake inhibitor. Cilobamine methanesulfonate increases the levels of Aniline hydroxylase and cytochrome P-450 in rat liver. Cilobamine methanesulfonate promotes hypertrophy of the smooth endoplasmic reticulum in rat liver hepatocytes, increases relative liver weight and recoverable microsomal protein. Cilobamine methanesulfonate produces stimulant and anxiogenic effects, and does not inhibit monoamine oxidase. Cilobamine methanesulfonate can be used in the research of depression.
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Tesofensine (Standard)
0 ImagesSynonyms: NS-2330 (Standard)Tesofensine (Standard) is the analytical standard of Tesofensine. This product is intended for research and analytical applications. Tesofensine (NS-2330) is a triple monoamine reuptake inhibitor inducing a potent inhibition of the re-uptake process in the synaptic cleft of the neurotransmitters dopamine (DA; IC50=6.5 nM), norepinephrine (NE;IC50=1.7 nM), and serotonin (5-HT;IC50=11 nM), and with potentials as an anti-obesity agent. Tesofensine is a CNS acting anti-obesity agent.
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Piroheptine
0 ImagesCat. No.: HY-W683866CAS No.: 16378-21-5Piroheptine is a muscarinic acetylcholine receptor (mAChR) antagonist and dopamine reuptake inhibitor. Piroheptine blocks the high-affinity dopamine transport system, prevents MPP+ uptake into dopaminergic neurons, and exerts anticholinergic activity. Piroheptine completely prevents MPTP (HY-W114750)-induced loss of striatal dopamine and DOPAC, and increases striatal dopamine levels. Piroheptine can be used in studies related to Parkinson's disease.
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SPD-473 citrate
0 ImagesSPD-473 citrate is a serotonin/dopamine/norepinephrine reuptake inhibitior.
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N-Methyl-2-phenylpropan-1-amine hydrochloride
0 ImagesCat. No.: HY-W354635CAS No.: 5969-39-1N-Methyl-2-phenylpropan-1-amine hydrochloride is a β-Methylphenethylamine (BMPEA) analog, and has transmitter releasing action at NET and DAT assay.
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Cilobamine
0 ImagesCat. No.: HY-183457CAS No.: 69429-84-1Cilobamine is an orally active antidepressant and a dopamine/norepinephrine reuptake inhibitor. Cilobamine increases the levels of Aniline hydroxylase and cytochrome P-450 in rat liver. Cilobamine promotes hypertrophy of the smooth endoplasmic reticulum in rat liver hepatocytes, increases relative liver weight and recoverable microsomal protein. Cilobamine produces stimulant and anxiogenic effects, and does not inhibit monoamine oxidase. Cilobamine can be used in the research of depression.
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RTI-371
0 ImagesCat. No.: HY-129215CAS No.: 652978-45-5RTI-371 is a highly selective atypical dopamine transporter (DAT) inhibitor that crosses the blood-brain barrier. RTI-371 exhibits potent inhibitory activity in cell lines transfected with human DAT (IC50 = 8.7 nM) and shows high binding affinity for rat DAT with a Ki value of 7.81 nM. RTI-371 also acts as a positive allosteric modulator of the human cannabinoid 1 receptor (hCB1 receptor), enhancing the activity of cannabinoid receptor agonists in a concentration-dependent manner. RTI-371 can be used for the research of Parkinson's disease.
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Vanoxerine dihydrochloride (Standard)
0 ImagesCat. No.: HY-13217RCAS No.: 67469-78-7Synonyms: GBR-12909 dihydrochloride (Standard); I893 dihydrochloride (Standard)Vanoxerine (dihydrochloride) (Standard) is the analytical standard of Vanoxerine (dihydrochloride). This product is intended for research and analytical applications. Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT).
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13-Hydroxyisobakuchiol
0 ImagesCat. No.: HY-N7506CAS No.: 178765-49-6Synonyms: Delta3,2-Hydroxylbakuchiol13-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.
