- Signalwege
- Neuronal Signaling
- Dopamine Transporter
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 Verwandte Produkte (115)
Verwandte Produkte (115)
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NMDAR antagonist 5
0 ImagesArt. -Nr.: HY-173398CAS. Nr.: 3038464-68-2NMDAR antagonist 5 (Compound A17) is a multi-target antagonist against NMDAR and monoamine transporters (SERT、DAT and NET). NMDAR antagonist 5 shows good NMDAR antagonistic potency (IC50 = 0.3 μM) and monoamine transporter activities (SERT IC50 = 1.1 μM、DAT IC50 = 0.7 μM、NET IC50 = 2.7 μM). NMDAR antagonist 5 is highly safe and has low toxicity (hepatotoxicity and nephrotoxicity (IC50 > 100 μM); cardiotoxicity (IC50 = 24.5 μM)). NMDAR antagonist 5 has antidepressant effects and can be used in the study of depression. -
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Levophacetoperane
0 ImagesArt. -Nr.: HY-119409CAS. Nr.: 24558-01-8Synonyms: Phacetoperane free baseLevophacetoperane (Phacetoperane free base) competitively inhibits the uptake of norepinephrin and dopamine. -
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SKF-83566 (Standard)
0 ImagesArt. -Nr.: HY-103430ARCAS. Nr.: 99295-33-7SKF-83566 (Standard) is the analytical standard of SKF-83566 (HY-103430A). This product is intended for research and analytical applications. SKF-83566 is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a Ki value of approximately 0.4-0.56 nM. SKF-83566 modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway. SKF-83566 acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2). SKF-83566 competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation. SKF-83566 is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect"). -
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Lobeline hydrochloride (Standard)
0 ImagesSynonyms: α-Lobeline hydrochloride (Standard); L-Lobeline hydrochloride (Standard)Lobeline (hydrochloride) (Standard) is the analytical standard of Lobeline (hydrochloride). This product is intended for research and analytical applications. Lobeline (α-Lobeline) hydrochloride is a brain-penetrant nicotinic receptor agonist. Lobeline hydrochloride increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline hydrochloride is effective in smoking cessation. -
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Fipexide hydrochloride (Standard)
0 ImagesFipexide (hydrochloride) (Standard) is the analytical standard of Fipexide (hydrochloride). This product is intended for research and analytical applications. Fipexide hydrochloride, a parachloro-phenossiacetic acid derivative, is an orally active nootropic agent. Fipexide hydrochloride reduces striatal adenylate cyclase activity. Fipexide hydrochloride has positive effect on cognitive performance by dopaminergic neurotransmission. Fipexide hydrochloride is used for senile dementia research. Fipexide hydrochloride acts as a chemical inducer in callus formation, shoot regeneration and Agrobacterium infection. -
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6-APDB
0 ImagesArt. -Nr.: HY-W680886CAS. Nr.: 152623-93-36-APDB is a class of monoamine neurotransmitter releaser and Monoamine Transporter modulator that exerts selective effects on human monoamine transporters and acts as a partial agonist at 5-HT2 family receptors. For NET, 6-APDB has an IC50 of 0.56 μM and a Ki of 18 μM; for SERT, it has an IC50 of 2.3 μM and a Ki of 23 μM; for DAT, it has an IC50 of 33 μM and a Ki of >30 μM, and affinity for rat and mouse TAAR1, with Ki values of 1.0 μM and 0.21 μM, respectively. 6-APDB inhibits norepinephrine and 5-HT reuptake, mediates the release of three types of monoamine neurotransmitters, shows a dose-dependent biphasic locomotor effect in mice, and fully substitutes the discriminative stimulus effect of MDMA. 6-APDB shows no significant cytotoxicity at high concentrations, and possesses empathogenic psychoactivity, potential hallucinogenic effects, and behavioral effects associated with intermittent abuse. -
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Levophacetoperane hydrochloride (Standard)
0 ImagesArt. -Nr.: HY-101631RCAS. Nr.: 23257-56-9Levophacetoperane (hydrochloride) (Standard) is the analytical standard of Levophacetoperane (hydrochloride) (HY-101631). This product is intended for research and analytical applications. Levophacetoperane inhibits in vitro in a competitive manner, norepinephrin uptake and dopamine uptake. -
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Diclofensine hydrochloride (Standard)
0 ImagesArt. -Nr.: HY-18610RCAS. Nr.: 34041-84-4Synonyms: Ro 8-4650 hydrochloride (Standard)Diclofensine (Ro 8-4650) hydrochloride (Standard) is the analytical standard of Diclofensine hydrochloride. This product is intended for research and analytical applications. Diclofensine hydrochloride is an orally active neuronal monoamine uptake inhibitor. Diclofensine hydrochloride blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine hydrochloride potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine hydrochloride produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine hydrochloride can be used in the research of moderate to severe depression. -
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Amitifadine
0 ImagesArt. -Nr.: HY-18332CAS. Nr.: 410074-73-6Synonyms: DOV-21947; EB-1010Amitifadine (DOV-21947; EB-1010) is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC50s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively. -
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Fourphit
0 ImagesArt. -Nr.: HY-187585CAS. Nr.: 104639-01-2Fourphit is a dopamine transporter (DAT) inhibitor and phencyclidine (PCP) receptor binding agent. Fourphit irreversibly acylates the DAT [3H]methylphenidate binding site, reversibly binds to the PCP receptor, and sensitizes neuronal L-type DHP calcium channels. Fourphit attenuates K+-stimulated 45Ca2+ uptake at high concentrations, and after its pretreatment, Nifedipine (HY-B0284) effectively inhibits this uptake without affecting resting calcium uptake. Fourphit reduces cocaine-induced hyperactivity, decreases cocaine-induced rearing frequency, enhances cocaine-induced thigmotaxis, elicits an acute increase in locomotor activity, and suppresses dark-cycle activity. Fourphit is used in research related to cocaine abuse and addiction. -
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Bisacodyl (Standard)
0 ImagesBisacodyl (Standard) is the analytical standard of Bisacodyl. This product is intended for research and analytical applications. Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect. -
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Fipexide (Standard)
0 ImagesArt. -Nr.: HY-B1124RCAS. Nr.: 34161-24-5Fipexide (Standard) is the analytical standard of Fipexide. This product is intended for research and analytical applications. Fipexide, a parachloro-phenossiacetic acid derivative, is an orally active nootropic agent. Fipexide reduces striatal adenylate cyclase activity. Fipexide has positive effect on cognitive performance by dopaminergic neurotransmission. Fipexide is used for senile dementia research. Fipexide acts as a chemical inducer in callus formation, shoot regeneration and Agrobacterium infection. -
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DAT-IN-1
0 ImagesArt. -Nr.: HY-163138CAS. Nr.: 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 ImagesArt. -Nr.: HY-12242BCAS. Nr.: 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 ImagesArt. -Nr.: HY-123848CAS. Nr.: 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 ImagesArt. -Nr.: HY-W1133231CAS. Nr.: 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 ImagesArt. -Nr.: HY-120364CAS. Nr.: 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 ImagesArt. -Nr.: 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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