Dopamine Transporter

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

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.

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.