scholarly journals Chronic Exposure to Arsenic in Drinking Water Causes Alterations in Locomotor Activity and Decreases Striatal mRNA for the D2 Dopamine Receptor in CD1 Male Mice

2016 ◽  
Vol 2016 ◽  
pp. 1-10 ◽  
Author(s):  
Claudia Leticia Moreno Ávila ◽  
Jorge H. Limón-Pacheco ◽  
Magda Giordano ◽  
Verónica M. Rodríguez
Keyword(s):  
Drinking Water ◽  
Locomotor Activity ◽  
Dopamine Receptor ◽  
Dopaminergic System ◽  
Arsenic Exposure ◽  
D2 Receptors ◽  
Motor Memory ◽  
Arsenic Toxicity ◽  
D2 Dopamine Receptor ◽  
Cd1 Mice

Arsenic exposure has been associated with sensory, motor, memory, and learning alterations in humans and alterations in locomotor activity, behavioral tasks, and neurotransmitters systems in rodents. In this study, CD1 mice were exposed to 0.5 or 5.0 mg As/L of drinking water for 6 months. Locomotor activity, aggression, interspecific behavior and physical appearance, monoamines levels, and expression of the messenger for dopamine receptors D1 and D2 were assessed. Arsenic exposure produced hypoactivity at six months and other behaviors such as rearing and on-wall rearing and barbering showed both increases and decreases. No alterations on aggressive behavior or monoamines levels in striatum or frontal cortex were observed. A significant decrease in the expression of mRNA for D2 receptors was found in striatum of mice exposed to 5.0 mg As/L. This study provides evidence for the use of dopamine receptor D2 as potential target of arsenic toxicity in the dopaminergic system.

scholarly journals μ-opioid/D2 dopamine receptor pharmacophore containing ligands: Synthesis and pharmacological evaluation

2020 ◽  
Vol 85 (6) ◽  
pp. 711-720
Author(s):  
Ivana Jevtic ◽  
Jelena Penjisevic ◽  
Katarina Savic-Vujovic ◽  
Dragana Srebro ◽  
Sonja Vuckovic ◽  
...  
Keyword(s):  
Dopamine Receptor ◽  
Opioid Receptor ◽  
General Structure ◽  
D2 Receptors ◽  
Antinociceptive Activity ◽  
D2 Dopamine Receptor ◽  
Pharmacological Evaluation ◽  
Pharmacological Tests

Herein, the synthesis and pharmacological evaluation of 13 novel compounds, designed as potential heterobivalent ligands for ?-opioid receptor (MOR) and dopamine D2 receptors (D2DAR), are reported. The compounds consisted of anilido piperidine and N-aryl piperazine moieties, joined by a variable-length methylene linker. The two moieties represent MOR and D2DAR pharmacophores, respectively. The synthesis encompassed four steps, securing the final products in 28?42 % overall yields. The approach has a considerable synthetic potential, providing access to various related structures. Pharmacological tests involved in vitro competitive assay for D2DAR using [3H] spiperon, as a standard radioligand, and in vivo antinociceptive tests for MOR. The measured dopamine affinities were modest to low, while antinociceptive activity was completely absent. Therefore, the compounds of the general structure prepared in this research are unlikely to be useful as opioid?dopamine receptor heterobivalent ligands.

scholarly journals Abundance compensates kinetics: Similar effect of dopamine signals on D1 and D2 receptor populations

2018 ◽  
Author(s):  
Lars Hunger ◽  
Arvind Kumar ◽  
Robert Schmidt
Keyword(s):  
Basal Ganglia ◽  
Dopamine Receptors ◽  
Dopamine Receptor ◽  
D2 Receptors ◽  
D1 Receptors ◽  
Striatal Neurons ◽  
D2 Dopamine Receptor ◽  
Receptor Kinetics ◽  
D1 And D2 Receptors ◽  
Dopamine Receptor Binding

AbstractThe neuromodulator dopamine plays a key role in motivation, reward-related learning and normal motor function. The different affinity of striatal D1 and D2 dopamine receptor types has been argued to constrain the D1 and D2 signalling pathways to phasic and tonic dopamine signals, respectively. However, this view assumes that dopamine receptor kinetics are instantaneous so that the time courses of changes in dopamine concentration and changes in receptor occupation are basically identical. Here we developed a neurochemical model of dopamine receptor binding taking into account the different kinetics and abundance of D1 and D2 receptors in the striatum. Testing a large range of behaviorally-relevant dopamine signals, we found that the D1 and D2 dopamine receptor populations responded very similarly to tonic and phasic dopamine signals. Furthermore, due to slow unbinding rates, both receptor populations integrated dopamine signals over a timescale of minutes. Our model provides a description of how physiological dopamine signals translate into changes in dopamine receptor occupation in the striatum, and explains why dopamine ramps are an effective signal to occupy dopamine receptors. Overall, our model points to the importance of taking into account receptor kinetics for functional considerations of dopamine signalling.Significance statementCurrent models of basal ganglia function are often based on a distinction of two types of dopamine receptors, D1 and D2, with low and high affinity, respectively. Thereby, phasic dopamine signals are believed to mostly affect striatal neurons with D1 receptors, and tonic dopamine signals are believed to mostly affect striatal neurons with D2 receptors. This view does not take into account the rates for the binding and unbinding of dopamine to D1 and D2 receptors. By incorporating these kinetics into a computational model we show that D1 and D2 receptors both respond to phasic and tonic dopamine signals. This has implications for the processing of reward-related and motivational signals in the basal ganglia.

scholarly journals Locomotor Activity in D2 Dopamine Receptor-Deficient Mice Is Determined by Gene Dosage, Genetic Background, and Developmental Adaptations

1998 ◽  
Vol 18 (9) ◽  
pp. 3470-3479 ◽  
Author(s):  
Michele A. Kelly ◽  
Marcelo Rubinstein ◽  
Tamara J. Phillips ◽  
Christina N. Lessov ◽  
Sue Burkhart-Kasch ◽  
...  
Keyword(s):  
Locomotor Activity ◽  
Dopamine Receptor ◽  
Genetic Background ◽  
Gene Dosage ◽  
D2 Dopamine Receptor ◽  
Deficient Mice

Role of trace amine associated receptor 1 (TAAR1) in D2 dopamine receptor-related behavior and signaling

2012 ◽  
Author(s):  
S. Espinoza ◽  
F. Manago ◽  
M. Messa ◽  
T. D. Sotnikova ◽  
M. Caron ◽  
...  
Keyword(s):  
Dopamine Receptor ◽  
D2 Dopamine Receptor ◽  
Trace Amine

Role of Trace Amine Associated Receptor 1 (TAAR1) in D2 Dopamine receptor-related behavior and signaling

2012 ◽  
Author(s):  
S. Espinoza ◽  
F. Manago ◽  
M. Messa ◽  
T. D. Sotnikova ◽  
M. Caron ◽  
...  
Keyword(s):  
Dopamine Receptor ◽  
D2 Dopamine Receptor ◽  
Trace Amine

The effect of ionic environments on the affinity of D2-dopamine receptor radioligands

2005 ◽  
Vol 25 (1_suppl) ◽  
pp. S616-S616
Author(s):  
Christine A Parker ◽  
Julian C Matthews ◽  
John Brown ◽  
Antony D Gee ◽  
Eugenii A Rabiner
Keyword(s):  
Dopamine Receptor ◽  
D2 Dopamine Receptor
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