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Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist
TLDR
The crystal structure of the human dopamine D3 receptor in complex with the small molecule D2R/D3R-specific antagonist eticlopride reveals important features of the ligand binding pocket and extracellular loops.
The binding sites for cocaine and dopamine in the dopamine transporter overlap
TLDR
The models suggest that the binding site for cocaine and cocaine analogs is deeply buried between transmembrane segments 1, 3, 6 and 8, and overlaps with the binding sites for the substrates dopamine and amphetamine, as well as for benztropine-like DAT inhibitors.
Dopamine Agonist-Induced Yawning in Rats: A Dopamine D3 Receptor-Mediated Behavior
TLDR
It is reported that dopamine D2/D3 agonists elicit dose-dependent yawning behavior in rats, resulting in an inverted U-shaped dose-response curve.
Time-resolved FRET between GPCR ligands reveals oligomers in native tissues.
TLDR
A time-resolved FRET strategy based on receptor labeling with selective fluorescent ligands was developed and applied to native tissues and succeeded in demonstrating the presence of oxytocin receptor dimers and/or oligomers in mammary gland.
Current perspectives on selective dopamine D3 receptor antagonists as pharmacotherapeutics for addictions and related disorders
TLDR
Preclinical evidence in support of the efficacy of selective DA D3 receptor antagonists in animal models of drug addiction will be reviewed and translational research from preclinical efficacy studies to so‐called proof‐of‐concept studies for drug addiction indications will be discussed.
Cooperative transcription activation by Nurr1 and Pitx3 induces embryonic stem cell maturation to the midbrain dopamine neuron phenotype.
TLDR
It is shown that Nurr1 and Pitx3 cooperatively promote terminal maturation to the midbrain DA neuron phenotype in murine and human ES cell cultures.
PG01037, a novel dopamine D3 receptor antagonist, inhibits the effects of methamphetamine in rats
TLDR
The data suggest that the novel D3 antagonist PG01037 significantly attenuates the rewarding effects as assessed by progressive-ratio self-administration and brain stimulation reward, and inhibits methamphetamine-associated cue-induced reinstatement of drug-seeking behavior These findings support the potential use of PG010 37 or other selective D3 antagonists in the treatment of methamphetamine addiction.
Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.
Dopamine D3 receptor subtypes have been hypothesized to play a pivotal role in modulating the reinforcing and drug-seeking effects induced by cocaine. However, definitive pharmacological
Effects of selective dopaminergic compounds on a delay-discounting task
TLDR
None of the selective agonists and antagonists tested reduced impulsive choice, so further research is needed to determine if direct dopaminergic agonists or antagonists may be therapeutically useful in the treatment of impulse-control disorders.
Visualization of Dopamine Transporter Trafficking in Live Neurons by Use of Fluorescent Cocaine Analogs
TLDR
Novel fluorescently tagged cocaine analogs are used to visualize DAT and DAT trafficking in cultured live midbrain dopaminergic neurons and challenge the paradigm that trafficking and cellular distribution of endogenous DAT is subject to regulation by PKC.
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