Dopamine Transporter

Radafaxine hydrochloride (GW-353162A) is a DAT (dopamine transporter) and NET(norepinephrine transporter) transporters inhibitor, and nAChR family modulator.

IDT307 is a fluorescent substrate targeting the dopamine transporter (DAT). As an analog of the organic cation MPP+, it exhibits specific fluorescent properties that enable the visualization of DAT activity in various biological contexts. This compound is valuable for research applications focusing on dopamine signaling, drug interactions, and neurodegenerative disease models.

LR1143 is a potent inhibitor of the dopamine transporter (DAT), exhibiting an IC50 value of 3.4 nM in rat models. This compound also inhibits 5-HT uptake, with an IC50 of 112 nM, indicating its broader influence on serotonin reuptake sites. LR1143 demonstrates a strong binding affinity for DAT, as evidenced by its interaction with the dopamine reuptake inhibitor GBR 12935, and offers utility in research focused on cocaine abuse and other neuropharmacological studies.

DOV-102,677 is a potent triple reuptake inhibitor targeting the dopamine transporter (DAT), norepinephrine transporter (NET), and serotonin transporter (SERT). It exhibits inhibitory potency with IC50 values of 129 nM for DAT, 103 nM for NET, and 133 nM for SERT. This compound has shown significant antidepressant-like effects and modulates sensory-motor gating in preclinical mouse models. DOV-102,677 is suitable for investigations into the mechanisms of depression and related neuropharmacological research.

EDMA hydrochloride is a derivative of MDMA that acts primarily as a substrate for various neurotransmitter transporters, including the serotonin transporter (SERT), dopamine transporter (DAT), and norepinephrine transporter (NET). This compound exhibits significant biological activity, demonstrating 5-HT releasing capability at SERT with an EC50 of 117 nM, as well as MPP+ releasing activity at DAT (EC50 = 597 nM) and NET (EC50 = 325 nM). EDMA hydrochloride is utilized in research applications related to neurotransmitter dynamics and psychoactive substance studies.

TFEB Activator 2 is a potent oral compound that effectively crosses the blood-brain barrier, targeting the dopamine transporter (DAT). It promotes TFEB nuclear translocation and enhances lysosome biogenesis through modulation of the DAT-CDK9-TFEB signaling pathway. With demonstrated neuroprotective properties, this reagent is valuable for research applications related to Alzheimer's disease and other neurodegenerative conditions.

EEDQ is a carboxylate activator and an irreversible antagonist at the 5HT2c receptors. It effectively reduces [3H]β-CIT binding to the dopamine transporter (DAT) in rat caudate-putamen (CPu) homogenates with an IC50 value of 78.3 μM. Additionally, EEDQ has demonstrated the ability to inhibit contralateral rotation behavior, making it a useful tool for studying dopamine signaling and behavioral responses in neuropharmacological research.

SKF-83566 is a selective antagonist of the D1-like dopamine receptors, specifically targeting the dopamine D1 and D5 receptors. This compound exhibits potent inhibition of the dopamine transporter (DAT) with an IC50 of 5.7 μM, and shows competitive antagonism at the vascular 5-HT2 receptor. In addition, SKF-83566 selectively inhibits adenylyl cyclase 2 (AC2) over AC1 and AC5, making it relevant for research into neurological disorders such as Parkinson's disease and studies focused on alleviating nicotine cravings.

SKF-83566 hydrobromide is a selective antagonist of the D1-like dopamine receptors, exhibiting high blood-brain barrier permeability and oral bioavailability. This compound functions as a competitive inhibitor of the dopamine transporter (DAT), with an IC50 of 5.7 μM, and demonstrates a weaker antagonistic effect on the vascular 5-HT2 receptor (Ki=11 nM). Additionally, SKF-83566 selectively inhibits adenylyl cyclase 2 (AC2) over AC1 and AC5, making it a valuable tool for studying Parkinson's disease and nicotine dependence.

LH2-051 is a selective dopamine transporter (DAT) inhibitor with a Ki of 0.95 μM, effectively blocking DAT-mediated dopamine uptake with an IC50 of 3.0 μM. This compound also promotes the nuclear translocation of transcription factor EB (TFEB), enhancing lysosome biogenesis. LH2-051 has demonstrated potential in improving cognitive function in amyloid precursor protein (APP)/Presenilin 1 (PS1) mouse models, making it valuable for research focused on Alzheimer’s disease mechanisms and therapies.

SRI-32743 is an allosteric modulator of the human dopamine transporter (hDAT) with an IC50 value of 9.86 μM. This compound is of particular interest for research into HIV-Tat-induced neurotoxicity. Its modulation of hDAT may provide insights into the neurobiological mechanisms underlying dopamine dysregulation in various neurotoxic conditions.