scholarly journals Water Extract ofFructus Hordei GerminatusShows Antihyperprolactinemia Activity via Dopamine D2 Receptor

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Xiong Wang ◽  
Li Ma ◽  
En-jing Zhang ◽  
Ji-li Zou ◽  
Hao Guo ◽  
...  
Keyword(s):  
Pc12 Cells ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Water Extract ◽  
Adenosine Monophosphate ◽  
D2 Receptors ◽  
Receptor Expression ◽  
Gh3 Cells ◽  
Serum Prolactin ◽  
Dopamine D2

Objective.Fructus Hordei Germinatusis widely used in treating hyperprolactinemia (hyperPRL) as a kind of Chinese traditional herb in China. In this study, we investigated the anti-hyperPRL activity of water extract ofFructus Hordei Germinatus(WEFHG) and mechanism of action.Methods. Effect of WEFHG on serum prolactin (PRL), estradiol (E2), progesterone (P), follicle-stimulating hormone (FSH), luteinizing hormone (LH), and hypothalamus protein kinase A (PKA) and cyclic adenosine monophosphate (cAMP) levels of hyperPRL rats were investigated. And effect of WEFHG on PRL secretion, D2 receptors, and dopamine transporters (DAT) was studied in MMQ, GH3, and PC12 cells, respectively.Results. WEFHG reduced the secretion of PRL in hyperPRL rats effectively. In MMQ cell, treatment with WEFHG at 1–5 mg/mL significantly suppressed PRL secretion and synthesis. Consistent with a D2-action, WEFHG did not affect PRL in rat pituitary lactotropic tumor-derived GH3 cells that lack the D2 receptor expression but significantly increased the expression of D2 receptors and DAT in PC12 cells. In addition, WEFHG reduced the cAMP and PKA levels of hypothalamus in hyperPRL rats significantly.Conclusions. WEFHG showed anti-hyperPRL activity via dopamine D2 receptor, which was related to the second messenger cAMP and PKA.

scholarly journals Dopamine D2 Receptor Expression Is Altered by Changes in Cellular Iron Levels in PC12 Cells and Rat Brain Tissue

2008 ◽  
Vol 138 (12) ◽  
pp. 2487-2494 ◽  
Author(s):  
Erica L. Unger ◽  
Jason A. Wiesinger ◽  
Lei Hao ◽  
John L. Beard
Keyword(s):  
Rat Brain ◽  
Brain Tissue ◽  
Pc12 Cells ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Receptor Expression ◽  
Dopamine D2 ◽  
Cellular Iron ◽  
Rat Brain Tissue

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 Effect of Zishenpingchan Granule on Neurobehavioral Manifestations and the Activity and Gene Expression of Striatal Dopamine D1 and D2 Receptors of Rats with Levodopa-Induced Dyskinesias

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Qing Ye ◽  
Xiao-Lei Yuan ◽  
Jie Zhou ◽  
Can-xing Yuan ◽  
Xu-ming Yang
Keyword(s):  
Gene Expression ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
D2 Receptors ◽  
Striatal Dopamine ◽  
Control Group ◽  
Indirect Pathway ◽  
Dopamine D2 ◽  
D1 And D2 Receptors ◽  
Neurobehavioral Manifestations

This study was performed to observe the effects of Zishenpingchan granule on neurobehavioral manifestations and the activity and gene expression of striatal dopamine D1 and D2 receptors of rats with levodopa-induced dyskinesias (LID). We established normal control group, LID model group, and TCM intervention group. Each group received treatment for 4 weeks. Artificial neural network (ANN) was applied to excavate the main factor influencing variation in neurobehavioral manifestations of rats with LID. The results showed that overactivation in direct pathway mediated by dopamine D1 receptor and overinhibition in indirect pathway mediated by dopamine D2 receptor may be the main mechanism of LID. TCM increased the efficacy time of LD to ameliorate LID symptoms effectively mainly by upregulating dopamine D2 receptor gene expression.

Dopamine D2 receptor expression in the corticotroph cells of the human normal pituitary gland

Endocrine ◽  
2016 ◽  
Vol 57 (2) ◽  
pp. 314-325 ◽  
Author(s):  
Rosario Pivonello ◽  
Marlijn Waaijers ◽  
Johan M. Kros ◽  
Claudia Pivonello ◽  
Cristina de Angelis ◽  
...  
Keyword(s):  
Pituitary Gland ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Receptor Expression ◽  
Dopamine D2 ◽  
Normal Pituitary Gland

scholarly journals Valenced action/inhibition learning in humans is modulated by a genetic variant linked to dopamine D2 receptor expression

2014 ◽  
Vol 8 ◽  
Author(s):  
Anni Richter ◽  
Marc Guitart-Masip ◽  
Adriana Barman ◽  
Catherine Libeau ◽  
Gusalija Behnisch ◽  
...  
Keyword(s):  
Genetic Variant ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Receptor Expression ◽  
Dopamine D2 ◽  
Action Inhibition

Dopamine D2 Receptor Blockade and Antimigraine Action of Flunarizine

Cephalalgia ◽  
1994 ◽  
Vol 14 (3) ◽  
pp. 235-240 ◽  
Author(s):  
C Wöber ◽  
T Brücke ◽  
C Wöber-Bingöl ◽  
S Asenbaum ◽  
P Wessely ◽  
...  
Keyword(s):  
Single Photon ◽  
Dopamine D2 Receptor ◽  
Photon Emission ◽  
D2 Receptor ◽  
High Specificity ◽  
D2 Receptors ◽  
Binding Potential ◽  
Receptor Blockade ◽  
Dopamine D2

We studied in vivo the influence of flunarizine on dopamine D2 receptors and investigated whether dopamine D2 receptor blockade is involved in its antimigraine action. Eleven migraine patients, treated with flunarizine, 10 mg per day, underwent single photon emission computer tomography (SPECT) using [123I] labeled iodobenzamide, a ligand with high affinity and high specificity for D2 receptors. There was a reduction of the dopamine D2 receptor binding potential in all patients compared to age-matched controls. The efficacy of flunarizine in migraine prophylaxis failed to correlate with the degree of the dopamine D2 receptor blockade. The antimigraine action of flunarizine may not involve antidopaminergic mechanisms.

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