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 (115)
Related Products (115)
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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.
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GBR 12935 dihydrochloride (Standard)
0 ImagesGBR 12935 (dihydrochloride) (Standard) is the analytical standard of GBR 12935 (dihydrochloride). This product is intended for research and analytical applications. GBR 12935 dihydrochloride is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 dihydrochloride stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 dihydrochloride also prevents the d-Fenfluramine-induced head-twitch response in mice.
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KM822
0 ImagesCat. No.: HY-128319CAS No.: 497926-94-0KM822 is a dopamine transporter (DAT) inhibitor with an IC50 of 2.2 μM against hDAT and an IC50 of 10.4 μM against C. elegans DAT-1. KM822 binds to the allosteric A2 site in the extracellular vestibule of outward-facing DAT, reduces the affinity of psychostimulants and phenethylamine psychostimulants for DAT, and inhibits dopamine transport function. KM822 attenuates the behaviors induced by psychostimulants and phenethylamine psychostimulants in planarians and C. elegans, does not induce locomotor effects on its own, and exhibits specificity for DAT. KM822 can serve as a molecular probe for investigating the allosteric regulation of DAT function. KM822 is applicable to studies related to psychostimulant use disorders.
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SRI-32743
0 ImagesCat. No.: HY-175535CAS No.: 1940118-42-2SRI-32743 is an allosteric human dopamine transporter (hDAT) modulator (IC50=9.86 μM). SRI-32743 is promising for research of HIV-Tat-induced neurotoxicity.
