A plasma membrane protein called dopamine transporter (DAT) mediates extracellular dopamine (DA) reuptake and regulates the spatiotemporal dynamics of dopaminergic neurotransmission. DATs are essential for stopping dopaminergic signaling and preserving a dopamine pool that can be released. DATs actively shuttle released transmitter molecules back across the plasma membrane into dopaminergic neurons, where they can be sequestered for later use or enzymatic catabolism. This helps to modulate the concentration of extraneuronal dopamine.
DAT is the primary target of a number of psychostimulants, nootropics, antidepressants, and some recreational drugs, such as the notoriously addictive stimulant cocaine. Cocaine-like inhibitors and amphetamine-like substrates are the two categories into which DAT ligands have traditionally been divided. A number of signaling systems, including PKC, control DAT.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V71787 | (R)-Phenylpiracetam (MRZ 9547) | 949925-07-9 | (R)-Phenylpiracetam (MRZ 9547) is a dopamine transporter (DAT) inhibitor (antagonist) with Ki and IC50 of 14.8 μM and 65.5 μM respectively. |
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V121983 | (R,S)-MDDMA | (R,S)-MDDMA is an MDMA analog that does not possess the psychostimulant effects of its parent compound, but still retains some of the serotonin-releasing activity. | |
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V122154 | (S)-CE-123 | 2378384-49-5 | (S)-CE-123 is a novel, highly effective and selective atypical dopamine transporter (DAT) inhibitor. In an uptake inhibition assay conducted in HEK293 cells stably expressing the human DAT isoform, its EC50 value was 2.76 μM. |
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V71786 | 13-Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol) | 178765-49-6 | 13-Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol) is extracted from Psoralea corylifolia and is an analog of Bakuchiol. |
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V124051 | 2,4,5-Trimethoxycinnamic acid | 24160-53-0 | 2,4,5-Trimethoxycinnamic acid is its metabolite. |
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V71788 | 3-CPMT (Tropine 4-chlorobenzhydryl ether hydrochloride) | 14008-79-8 | 3-CPMT (Tropine 4-chlorobenzyl ether HCl) is a potent dopamine uptake inhibitor. |
|
V71785 | 5,7-Dimethoxyluteolin | 90363-40-9 | 5,7-Dimethoxyluteolin, a 5,7-dimethylluteolin analogue, is a dopamine transporter (DAT) activator with EC50 of 3.417 μM. |
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V127372 | 6-Chloro-5-(2-chloroethyl)oxindole | 118289-55-7 | 6-Chloro-5-(2-chloroethyl)oxindole is an impurity of ziprasidone, which is a substrate of the human dopamine transporter (hDAT). |
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V99861 | AC-4-248 | AC-4-248 is an atypical noncompetitive dopamine transporter (DAT) inhibitor that reduces the inhibitory potency of cocaine on DAT. | |
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V71784 | AHN 1-055 hydrochloride (3α-Bis-(4-fluorophenyl) Methoxytropane hydrochloride) | 202646-03-5 | AHN 1-055 HCl is a dopamine uptake inhibitor (antagonist) with IC50 of 71 nM. |
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V128770 | AMPA receptor modulator-12 | AMPA receptor modulator-12 is an orally administered AMPA receptor positive allosteric modulator. | |
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V70652 | CAD031 | 2071209-49-7 | CAD031 is an analogue of the AD/Alzheimer's disease targeting agent J147 with neuro-protection and memory-enhancing properties. |
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V131371 | Cendifensine | 1034048-49-1 | Cendifensine is a monoamine reuptake inhibitor that inhibits serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). |
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V131968 | CM699 | 1259949-84-2 | CM699 is a potent dual inhibitor of dopamine transporter (DAT) and Sigma receptor (σR), with IC50 values of 311 nM and 14.1 nM, respectively. |
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V133152 | D-473 | 1632000-05-5 | D-473 is an orally effective, blood-brain barrier-crossing reuptake inhibitor that preferentially targets serotonin. |
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V111247 | DAM-001 | 1090396-31-8 | DAM-001 (Z236004662) is a potent, non-competitive allosteric inhibitor that inhibits the human dopamine transporter (hDAT). Its IC50 values are 24.70 μM and 1.026 μM in the presence and absence of the allosteric inhibitor nomiphenecin, respectively. |
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V85137 | DAT-IN-1 | ||
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V70004 | Desipramine-d3 (desipramine hydrochloride-d3; desipramine hydrochloride-d3) | 65100-49-4 | Desipramine-d3 is deuterium labelled Desipramine. |
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V70006 | Desipramine-d4 (desipramine hydrochloride-d4; desipramine hydrochloride-d4) | 61361-34-0 | Desipramine-d4 is the deuterium labelled form of Desipramine. |
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V115489 | DOV-102,677 | 410074-75-8 | DOV-102,677 is an orally effective triple monoamine neurotransmitter reuptake inhibitor that simultaneously inhibits dopamine transporter (DAT) (IC50 = 129 nM; Ki = 222 nM), norepinephrine transporter (NET) (IC50 = 103 nM; Ki = 1030 nM) and serotonin transporter (SERT) (IC50 = 133 nM; Ki = 740 nM). |
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