scholarly journals Striatal CB1 and D2 receptors regulate expression of each other, CRIP1A and delta opioid systems

2013 ◽  
Vol 124 (6) ◽  
pp. 808-820 ◽  
Author(s):  
Lawrence C. Blume ◽  
Caroline E. Bass ◽  
Steven R. Childers ◽  
George D. Dalton ◽  
David C. S. Roberts ◽  
...  
Keyword(s):  
D2 Receptors ◽  
Opioid Systems

Extraversion and Dopamine

1998 ◽  
Vol 3 (1) ◽  
pp. 37-50 ◽  
Author(s):  
Thomas H. Rammsayer
Keyword(s):  
Individual Differences ◽  
D2 Receptor ◽  
D2 Receptors ◽  
Behavioral Differences ◽  
Biological Mechanisms ◽  
Brain Dopamine ◽  
Personality Dimension ◽  
Time Performance ◽  
Reaction Time Performance ◽  
Induced Changes

Recent research suggests that individual differences in brain dopamine (DA) functioning may be related to the personality dimension of extraversion. The present study was designed to further elucidate the biological mechanisms underlying behavioral differences between extraverts and introverts. For this purpose, the differential effects of a pharmacologically induced blockade of mesolimbocortical DA D2 receptors on reaction-time performance were investigated in 24 introverted and 24 extraverted subjects. Introverts were found to be much more susceptible to pharmacologically induced changes in D2 receptor activity than extraverts. This finding provides additional experimental evidence for the notion that individual differences in D2 receptor responsivity may represent a neurobiological substratum for the personality dimension of extraversion.

Quantifying in vivo dopaminergic D2-receptors Bmax and KdVr with microPET® focus after a single injection of [11C]raclopride

2005 ◽  
Vol 25 (1_suppl) ◽  
pp. S649-S649
Author(s):  
Laurent Besret ◽  
Jean-Dominique Gallezot ◽  
Frédéric Dollé ◽  
Philippe Hantraye ◽  
Marie-Claude Grégoire
Keyword(s):  
Single Injection ◽  
D2 Receptors ◽  
Quantifying In

The Expression of Dopamine Receptors Gene and their Potential Role in Targeting Breast Cancer Cells with Selective Agonist and Antagonist Drugs. Could it be the Novel Insight to Therapy?

2019 ◽  
Vol 16 (2) ◽  
pp. 184-197 ◽  
Author(s):  
Hossein Bakhtou ◽  
Asiie Olfatbakhsh ◽  
Abdolkhaegh Deezagi ◽  
Ghasem Ahangari
Keyword(s):  
Breast Cancer ◽  
Gene Expression ◽  
Cancer Cells ◽  
Dopamine Receptors ◽  
Breast Cancer Cells ◽  
D2 Receptors ◽  
Healthy Individuals ◽  
Agonist And Antagonist ◽  
The Mean ◽  
Mcf 7

Background:Breast cancer is one of the common causes of mortality for women in Iran and other parts of the world. The substantial increasing rate of breast cancer in both developed and developing countries warns the scientists to provide more preventive steps and therapeutic measures. This study is conducted to investigate the impact of neurotransmitters (e.g., Dopamine) through their receptors and the importance of cancers via damaging immune system. It also evaluates dopamine receptors gene expression in the women with breast cancer at stages II or III and dopamine receptor D2 (DRD2) related agonist and antagonist drug effects on human breast cancer cells, including MCF-7 and SKBR-3.Methods:The patients were categorized into two groups: 30 native patients who were diagnosed with breast cancer at stages II and III, with the mean age of 44.6 years and they were reported to have the experience of a chronic stress or unpleasant life event. The second group included 30 individuals with the mean age of 39 years as the control group. In order to determine the RNA concentration in all samples, the RNA samples were extracted and cDNA was synthesized. The MCF-7 cells and SKBR-3 cells were treated with dopamine receptors agonists and antagonists. The MTT test was conducted to identify oxidative and reductive enzymes and to specify appropriate dosage at four concentrations of dopamine and Cabergoline on MCF-7 and SKBR-3 cells. Immunofluorescence staining was done by the use of a mixed dye containing acridine orange and ethidiume bromide on account of differentiating between apoptotic and necrotic cells. Flow cytometry assay was an applied method to differentiate necrotic from apoptotic cells.Results:Sixty seven and thirty three percent of the patients were related to stages II and III, respectively. About sixty three percent of the patients expressed ER, while fifty seven percent expressed PR. Thirty seven percent of the patients were identified as HER-2 positive. All types of D2-receptors were expressed in PBMC of patients with breast cancer and healthy individuals. The expression of the whole dopamine receptor subtypes (DRD2-DRD4) was carried out on MCF-7 cell line. The results of RT-PCR confirmed the expression of DRD2 on SKBR-3 cells, whereas the other types of D2- receptors did not have an expression. The remarkable differences in gene expression rates between patients and healthy individuals were revealed in the result of the Real-time PCR analysis. The over expression in DRD2 and DRD4 genes of PBMCs was observed in the patients with breast cancer at stages II and III. The great amount of apoptosis and necrosis occurred after the treatment of MCF-7 cells by Cabergoline from 25 to 100 µmolL-1 concentrations.Conclusion:This study revealed the features of dopamine receptors associated with apoptosis induction in breast cancer cells. Moreover, the use of D2-agonist based on dopamine receptors expression in various breast tumoral cells could be promising as a new insight of complementary therapy in breast cancer.

The Effect of PAOPA, a Novel Allosteric Modulator of Dopamine D2 Receptors, on Select Signaling Proteins Following Sub-Chronic Administration in the Rat

2020 ◽  
Vol 13 ◽  
Author(s):  
Ritesh Daya ◽  
Joella Ho ◽  
Sharon Thomson ◽  
Jayant Bhandari ◽  
Ram K. Mishra
Keyword(s):  
Frontal Cortex ◽  
Mechanism Of Action ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Dorsal Striatum ◽  
D2 Receptors ◽  
Dopamine D2 ◽  
Therapeutic Mechanism ◽  
Clinical Models ◽  
G Protein Coupled

Background: Allosteric modulators of G-protein coupled receptors regulate receptor activity by binding to sites other than the active site and have emerged as a new and highly desirable class of drugs. PAOPA (3(R)-[(2(S)- pyrrolidinylcarbonyl)amino]-2-oxo-1-pyrrolidineacetamide), a peptidomimetic analog of Prolyl-Leucyl-Glycinamide, is a potent dopamine D2 receptor allosteric modulator. PAOPA has shown therapeutic effects in pre-clinical models of schizophrenia and extrapyramidal dysfunction. Objective: in this study, we sought to examine the biomolecular underpinnings of PAOPA‘s therapeutic outcomes in preclinical models of schizophrenia. Method: Following sub-chronic (daily for 7 days) administration of PAOPA, we assessed levels of dopamine D2 receptors, receptor kinases (GRK2 (G protein-coupled receptor kinase 2) and Arrestin-3), and phosphorylated mitogenactivated protein kinase (MAPKs), namely, extracellular signal-regulated kinases (ERK1/2) in the hippocampus, medial pre-frontal cortex, nucleus accumbens, pre-frontal cortex, and dorsal striatum via protein quantification. Results: Following 7 days of daily PAOPA treatment, we observed decreased GRK2 and increased dopamine D2 receptor expression in the dorsal striatum. These findings potentially underscore PAOPA’s therapeutic mechanism of action for the positive-like symptoms of schizophrenia in pre-clinical animal models. Additionally, we observed a decline in GRK2 in the hippocampus and an increase in phosphorylated ERK1 in the pre-frontal cortex, suggestive of a role for PAOPA in treating cognitive and/or affective dysfunction in pre-clinical models. Conclusion: While further studies are required to elucidate PAOPA’s mechanism of action, this study builds on prior investigations and develops an early framework to describe the therapeutic mechanism of action of PAOPA.

scholarly journals 371 STRIATAL DOPAMINE D2 RECEPTORS ATTENUATE NEUROPATHIC HYPERSENSITIVITY IN THE RAT

2007 ◽  
Vol 11 (S1) ◽  
pp. S165-S165
Author(s):  
O.B. Ansah ◽  
H. Leite-Almeida ◽  
H. Wei ◽  
A. Pertovaara
Keyword(s):  
D2 Receptors ◽  
Dopamine D2 Receptors ◽  
Striatal Dopamine ◽  
Dopamine D2

Ontogeny of locomotor activity and grooming in the young rat: role of dopamine D1 and D2 receptors

1990 ◽  
Vol 186 (2-3) ◽  
pp. 223-230 ◽  
Author(s):  
Sanders A. McDougall ◽  
Timothy F. Arnold ◽  
Arthur J. Nonneman
Keyword(s):  
Locomotor Activity ◽  
D2 Receptors ◽  
D1 And D2 Receptors ◽  
Young Rat
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