2. シグナル伝達
  3. Neuronal Signaling
  4. Dopamine Transporter

Dopamine Transporter

DAT; SLC6A3

Dopamine Transporter

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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.

Dopamine Transporter 関連製品 (100):

製品番号 製品名 製品効果 純度 構造式
  • HY-158013A
    JJC8-088 dioxalate Inhibitor 99.73%
    JJC8-088 dioxalate is the dioxalate salt form of JJC8-088 (HY-158013). JJC8-088 dioxalate is a derivative of modafinil. JJC8-088 dioxalate is an inhibitor for dopamine transporter (DAT). JJC8-088 dioxalate exhibits behavioral characteristics similar to cocaine in rat models, and can be to study psychostimulant use disorders.
    JJC8-088 dioxalate
  • HY-18610A
    Diclofensine Inhibitor 98.46%
    Diclofensine (Ro 8-46500) is an orally active neuronal monoamine uptake inhibitor. Diclofensine 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 potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine can be used in the research of moderate to severe depression.
    Diclofensine
  • HY-12242A
    GBR 12935 Inhibitor
    GBR 12935 is a potent, and selective dopamine reuptake inhibitor, with the binding constant (Kd) of 1.08 nM in COS-7 cells. GBR 12935 stimulates the locomotion activity in different mice strains but fails to induce stereotypy. Thus, GBR 12935 also prevents the d-Fenfluramine-induced head-twitch response in mice.
    GBR 12935
  • HY-W009666
    6-Chloro-5-(2-chloroethyl)oxindole Control
    6-Chloro-5-(2-chloroethyl)oxindole (Imp Z2) is an impurity of Ziprasidone (HY-14542), a substrate of the human dopamine transporter (hDAT).
    6-Chloro-5-(2-chloroethyl)oxindole
  • HY-18610S
    Diclofensine-d3 (hydrochloride)
    Diclofensine-d3 (Ro-8-4650-d3) hydrochloride is the deuterium labeled Diclofensine hydrochloride. 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.
    Diclofensine-d<sub>3</sub> (hydrochloride)
  • HY-162511
    IP2015 Inhibitor
    IP2015 is an inhibitor for monoamine reuptake, that inhibits the reuptake of dopamine, serotonin (5-HT), and noradrenaline. IP2015 increases release of central dopamine and peripheral nitric oxide (NO), causes the NO-mediated relaxation of erectile tissue, and thus induces erection in rat model.
    IP2015
  • HY-163154
    JJC8-091 Inhibitor
    JJC8-091 is a potent dopamine transporter (DAT) inhibitor with Ki values of 230, 97800 nM for DAT, SERT, respectively. JJC8-091 has the potential for the research of psychostimulant use disorders (PSUD).
    JJC8-091
  • HY-128420
    Lobeline sulfate
    Lobeline (α-Lobeline) sulfate is a brain-penetrant nicotinic receptor agonist. Lobeline sulfate increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline sulfate is effective in smoking cessation.
    Lobeline sulfate
  • HY-121813
    Rimcazole
    Rimcazole (BW 234U) is a potent antipsychotic agent. Rimcazole also is a competitive antagonist of sigma sites. Rimcazole can be used for the research of acute schizophrenic diseases.
    Rimcazole
  • HY-14840A
    (R)-Phenylpiracetam Inhibitor
    (R)-Phenylpiracetam (MRZ 9547) is a dopamine transporter (DAT) inhibitor (Ki: 14.8 μM; IC50: 65.5 μM). (R)-Phenylpiracetam can be used for the research of the neurological or neuropsychiatric disorders.
    (R)-Phenylpiracetam
  • HY-173475
    CM699 Inhibitor
    CM699 is a potent Dopamine Transporter (DAT) and Sigma-receptor (σR) dual inhibitor with IC50s of 311 and 14.1 nM, respectively.
    CM699
  • HY-158014
    JJC8-089 Inhibitor
    JJC8-089 is a dopamine transporter (DAT) inhibitor that may improve motivational dysfunction and increase effortful behavior in goal-directed activities. JJC8-089 significantly reversed the low-effort effects induced by the VMAT-2 inhibitor Tetrabenazine (HY-B0590) in rats and increased the choice of high-effort fixed-ratio 5-bar presses versus food intake. .
    JJC8-089
  • HY-14472S1
    Tesofensine-13C,d3 Inhibitor
    Tesofensine-13C,d3 (NS-2330-13C,d3) is the deuterium and 13C-labeled Tesofensine (HY-14472). 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.
    Tesofensine-<sup>13</sup>C,d<sub>3</sub>
  • HY-182091
    CYD-1-79 Inhibitor
    CYD-1-79 is a selective positive allosteric modulator of 5-HT2C receptor. CYD-1-79 potentiates 5-HT-evoked intracellular calcium release via a topographically distinct allosteric site. CYD-1-79 shows significant inhibition of binding at dopamine D3 receptor, DAT, and α2A/α2B adrenergic receptors. CYD-1-79 modulates 5-HT2C receptor-mediated spontaneous ambulation in rodents and synergizes with a low dose of a 5-HT2C receptor agonist. CYD-1-79 attenuates relapse vulnerability of psychoactive substance in a rodent self-administration model. CYD-1-79 can be used for the research of neurological disease.
    CYD-1-79
  • HY-174282
    RDS-04-010 Inhibitor 98.84%
    RDS-04-010 is an atypical dopamine transporter (DAT) inhibitor. RDS-04-010 has the effect of inhibiting cocaine intake and seeking behavior. RDS-04-010 exerts its modulatory effect mainly by binding to the inward conformation of DAT, thereby reducing the reinforcing effect of cocaine. RDS-04-010 can be used in the study of cocaine use disorder (CUD).
    RDS-04-010
  • HY-163155
    RDS03-94 Inhibitor
    RDS03-94 is a dopamine transporter (DAT) inhibitor. RDS03-94 reduces hERG/DAT ratio.
    RDS03-94
  • HY-158013
    JJC8-088 Inhibitor
    JJC8-088, a Modafinil-derived ligand, is a dopamine transporter (DAT) inhibitor with a Ki of 2.53 nM. JJC8-088 dioxalate can be to study psychostimulant use disorders.
    JJC8-088
  • HY-182247
    D-473 Inhibitor
    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.
    D-473
  • HY-183324
    AMPA receptor modulator-12
    AMPA receptor modulator-12 is an orally acrive AMPA receptor positive allosteric modulator. AMPA receptor modulator-12 also exhibits moderate binding affinity for the human dopamine transporter with a Kd of 1.57 μM. AMPA receptor modulator-12 enhances AMPA receptor-mediated ion currents, delays channel deactivation. AMPA receptor modulator-12 prolongs sleep latency, reduces sleep duration, extends forced swimming time, improves rotarod endurance, and alleviates acute sleep deprivation-related behavioral deficits. AMPA receptor modulator-12 does not increase spontaneous locomotion. AMPA receptor modulator-12 can be used for the research of narcolepsy and fatigue-related conditions.
    AMPA receptor modulator-12
  • HY-10427A
    iso-WAY-260022 Inhibitor
    iso-WAY-260022 (Compound 13R) is an orally active, brain-penetrant and selective norepinephrine transporter (hNET) inhibitor with an IC50 value of 140 nM. iso-WAY-260022 also shows inhibitory effects on human serotonin (hSERT) and dopamine transporters (hDAT). iso-WAY-260022 inhibits norepinephrine reuptake and increases hypothalamic norepinephrine levels to regulate thermoregulatory center function. iso-WAY-260022 is promising for research of vasomotor symptoms, such as menopausal hot flushes, night sweats.
    iso-WAY-260022