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https://www.readbyqxmd.com/read/28921163/discriminative-stimulus-properties-of-the-atypical-antipsychotic-amisulpride-comparison-to-its-isomers-and-to-other-benzamide-derivatives-antipsychotic-antidepressant-and-antianxiety-drugs-in-c57bl-6-mice
#1
Timothy J Donahue, Todd M Hillhouse, Kevin A Webster, Richard Young, Eliseu O De Oliveira, Joseph H Porter
RATIONALE: Racemic (RS)-amisulpride (Solian(®)) is an atypical antipsychotic drug used to treat schizophrenia and dysthymia. Blockade of dopamine D2/D3 and/or serotonin 5-HT7 receptors is implicated in its pharmacological effects. While the (S)-amisulpride isomer possesses a robust discriminative cue, discriminative stimulus properties of (RS)-amisulpride have not been evaluated. OBJECTIVES: The present study established (RS)-amisulpride as a discriminative stimulus and assessed amisulpride-like effects of amisulpride stereoisomers, other benzamide derivatives, and antipsychotic, antidepressant, and anxiolytic drugs...
September 18, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28918929/vitamin-d-receptor-targeted-treatment-to-prevent-pathological-dedifferentiation-of-pancreatic-%C3%AE-cells-under-hyperglycaemic-stress
#2
A Neelankal John, Z Iqbal, S Colley, G Morahan, M Makishima, F-X Jiang
Dedifferentiation has been identified as one of the causes of β-cell failure resulting in type 2 diabetes (T2D). This study tested whether increasing vitamin D receptor (VDR) expression prevents dedifferentiation of β cells in a high-glucose state in vitro. Culturing a mouse insulinoma cell line (MIN6) in a high-glucose environment decreased VDR expression. However, increased VDR following vitamin D3 (VD3) treatment improved insulin release of early-passage MIN6 and insulin index of db/- (heterozygous) islets to levels seen in normal functional islets...
September 11, 2017: Diabetes & Metabolism
https://www.readbyqxmd.com/read/28915830/biological-effects-of-combined-resveratrol-and-vitamin-d3-on-ovarian-tissue
#3
Francesca Uberti, Vera Morsanuto, Silvio Aprile, Sabrina Ghirlanda, Ian Stoppa, Andrea Cochis, Giorgio Grosa, Lia Rimondini, Claudio Molinari
BACKGROUND: Resveratrol (3,5,4'-trihydroxy-trans-stilbene) is a natural antioxidant polyphenol able to exert a wide range of biological effect on several tissues. Despite its important beneficial properties, it has a low water solubility, which limits its therapeutic applications in humans. Resveratrol also acts as a phytoestrogen that modulates estrogen receptor (ER)-mediated transcription. In addition, it has been shown that ovarian tissues benefit greatly from vitamin D3, which exerts its beneficial effects through VDR receptors...
September 15, 2017: Journal of Ovarian Research
https://www.readbyqxmd.com/read/28905271/pharmacokinetics-of-a-new-oral-vitamin-d-receptor-activator-2-methylene-19-nor-20s-1%C3%AE-25-dihydroxyvitamin-d3-in-patients-with-chronic-kidney-disease-and-secondary-hyperparathyroidism-on-hemodialysis
#4
Richa Pandey, Julia B Zella, Jinge G Zhu, Lori A Plum, Margaret Clagett-Dame, William J Blaser, Wendy Bedale, Hector F DeLuca, Daniel W Coyne
BACKGROUND: 2-Methylene-19-nor-(20S)-1α,25-dihydroxyvitamin D3 (DP001 or 2MD) is a novel, potent 1α-hydroxylated vitamin D analog that binds to the vitamin D receptor and suppresses parathyroid hormone synthesis and secretion with potential for an improved safety profile compared to existing active vitamin D analogs. The purpose of this study was to evaluate the pharmacokinetics of DP001 given orally after hemodialysis. METHODS: DP001 (550 ng) was given orally to 11 hemodialysis patients with secondary hyperparathyroidism after each dialysis session (3 times/week) for 4 weeks...
September 13, 2017: Drugs in R&D
https://www.readbyqxmd.com/read/28904008/mechanisms-in-endocrinology-clinical-and-pharmacogenetic-aspects-of-the-growth-hormone-receptor-polymorphism
#5
Cesar Luiz Boguszewski, Edna Jesus Litenski Barbosa, Per-Arne Svensson, Gudmundur Johannsson, Camilla A M Glad
Pharmacogenetics aims to maximize the beneficial effects of a medical therapy by identifying genetic finger prints from responders and non-responders and, thereby, improving safety and efficacy profile of the drug. Most subjects who are deficient in growth hormone (GHD) are candidates for recombinant human GH (rhGH) therapy. To date, it is well established that even after adjustments for several clinical variables, such as age, gender, body composition and the age at onset of the GHD, response to rhGH treatment is highly variable among individuals, part of which is believed to be due to genetic factors within the GH system...
September 13, 2017: European Journal of Endocrinology
https://www.readbyqxmd.com/read/28895569/the-effects-of-the-monoamine-stabilizer-osu6162-on-binge-like-eating-and-cue-controlled-food-seeking-behavior-in-rats
#6
K Feltmann, C Giuliano, B J Everitt, P Steensland, J Alsiö
Binge eating disorder (BED) is characterized by recurring episodes of excessive consumption of palatable food and an increased sensitivity to food cues. Patients with BED display an addiction-like symptomatology and the dopamine system might be a potential treatment target. The clinically safe monoamine stabilizer (-)-OSU6162 (OSU6162) restores dopaminergic dysfunction in long-term alcohol drinking rats and shows promise as a novel treatment for alcohol use disorder. Here, the effects of OSU6162 on consummatory (binge-like eating) and appetitive (cue-controlled seeking) behavior motivated by chocolate-flavored sucrose pellets were evaluated in non-food-restricted male Lister Hooded rats...
September 12, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28894299/dhea-inhibits-acute-microglia-mediated-inflammation-through-activation-of-the-trka-akt1-2-creb-jmjd3-pathway
#7
V I Alexaki, G Fodelianaki, A Neuwirth, C Mund, A Kourgiantaki, E Ieronimaki, K Lyroni, M Troullinaki, C Fujii, W Kanczkowski, A Ziogas, M Peitzsch, S Grossklaus, B Sönnichsen, A Gravanis, S R Bornstein, I Charalampopoulos, C Tsatsanis, T Chavakis
Dehydroepiandrosterone (DHEA) is the most abundant circulating steroid hormone in humans, produced by the adrenals, the gonads and the brain. DHEA was previously shown to bind to the nerve growth factor receptor, tropomyosin-related kinase A (TrkA), and to thereby exert neuroprotective effects. Here we show that DHEA reduces microglia-mediated inflammation in an acute lipopolysaccharide-induced neuro-inflammation model in mice and in cultured microglia in vitro. DHEA regulates microglial inflammatory responses through phosphorylation of TrkA and subsequent activation of a pathway involving Akt1/Akt2 and cAMP response element-binding protein...
September 12, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28893622/differential-expression-of-vitamin-d-associated-enzymes-and-receptors-in-brain-cell-subtypes
#8
Véréna Landel, Delphine Stephan, Xiaoying Cui, Darryl Eyles, François Feron
Accumulating evidence indicates that the active form of vitamin D, 1,25(OH)2D3, can be considered as a neurosteroid. However, the cerebral expression of vitamin D-associated enzymes and receptors remains controversial. With the idea of carrying out a comparative study in mind, we compared the transcript expression of Cyp27a1, Cyp27b1, Cyp24a1, Vdr and Pdia3 in purified cultures of astrocytes, endothelial cells, microglia, neurons and oligodendrocytes. We observed that endothelial cells and neurons can possibly transform the inactive cholecalciferol into 25(OH)D3...
September 8, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28888944/the-novel-dopamine-d3-receptor-antagonists-partial-agonists-cab2-015-and-bak4-54-inhibit-oxycodone-taking-and-oxycodone-seeking-behavior-in-rats
#9
Zhi-Bing You, Jun-Tao Gao, Guo-Hua Bi, Yi He, Comfort Boateng, Jianjing Cao, Eliot L Gardner, Amy Hauck Newman, Zheng-Xiong Xi
The use of prescription opioid analgesics, particularly oxycodone, has dramatically increased, and parallels escalated opioid abuse and drug-related deaths worldwide. Understanding the molecular mechanisms underlying the development of opioid dependence and expanding treatment options to counter prescription opioid abuse has become a critical public health matter. In the present study, we first evaluated the reinforcing effects of oxycodone in a rat model of self-administration and then explored the potential utility of two novel high affinity dopamine D3 receptor (D3R) antagonists/partial agonists, CAB2-015 and BAK4-54, for treatment of prescription opioid abuse and dependence...
September 6, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28887147/both-ligand-and-vdr-expression-levels-critically-determine-the-effect-of-1%C3%AE-25-dihydroxyvitamin-d3-on-osteoblast-differentiation
#10
Dongqing Yang, Paul H Anderson, Asiri R Wijenayaka, Kate R Barratt, Rahma Triliana, Catherine J M Stapledon, Hong Zhou, David M Findlay, Howard A Morris, Gerald J Atkins
Previous studies have shown that 1α,25-dihydroxyvitamin D3 (1,25D) through vitamin D receptor (VDR) signalling has both catabolic and anabolic effects on osteoblast differentiation. However, the mechanism of these differential effects by 1,25D is not fully understood. In this study, mice with three different genetic backgrounds, representing a normal VDR level (wild-type, WT), VDR over-expression specifically in mature osteoblasts (ObVDR-B6) and global VDR knockout (VDRKO), were utilised to generate primary osteoblast-like cultures to further elucidate the effects of 1,25D on osteoblast differentiation...
September 5, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28886458/a-novel-psychoanalytical-approach-an-electrochemical-ligand-binding-assay-to-screen-antipsychotics
#11
Tugba Kilic, Valerie Brunner, Laurent Audoly, Sandro Carrara
Schizophrenia treatment may see a paradigm shift due to development of new atypical antipsychotic drugs (APDs), with better tolerability due to more selective dopamine (DA) receptor blockade. Monitoring of these APD candidates in biological fluids is of great importance to reduce the development cost, to clarify the mechanism of action and ultimately to support the demonstration of efficacy of these molecules. Electrochemical approaches have attracted great attention for monitoring DA and APD levels but none of the methods developed so far aimed to screen APD candidates...
August 30, 2017: Biosensors & Bioelectronics
https://www.readbyqxmd.com/read/28885847/regulation-of-reduced-folate-carrier-rfc-by-vitamin-d-receptor-at-the-blood-brain-barrier
#12
Camille Alam, Md Tozammel Hoque, Richard H Finnell, I David Goldman, Reina Bendayan
Folates are essential for brain development and function. Folate transport in mammalian tissues is mediated by three major folate transport systems, i.e., reduced folate carrier (RFC), proton-coupled folate transporter (PCFT) and folate receptor alpha (FRα), known to be regulated by ligand-activated nuclear receptors such as vitamin D receptor (VDR). Folate uptake at the choroid plexus, which requires the actions of both FRα and PCFT, is critical to cerebral folate delivery. Inactivating FRα or PCFT mutations cause severe cerebral folate deficiency resulting in early childhood neurodegeneration...
September 8, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28883634/association-of-the-resolvin-precursor-17-hdha-but-not-d-or-e-series-resolvins-with-heat-pain-sensitivity-and-osteoarthritis-pain-in-humans
#13
Ana M Valdes, Srinivasarao Ravipati, Cristina Menni, Abhishek Abhishek, Sarah Metrustry, Juliette Harris, Ayrun Nessa, Frances M K Williams, Tim D Spector, Michael Doherty, Victoria Chapman, David A Barrett
Resolvins are omega-3 fatty acid derived potent bioactive lipids that resolve inflammation and modulate transient receptor potential channels. Exogenous administration of the resolvin precursor 17-HDHA shows a strong analgesic effect in animal models of osteoarthritis and acute inflammatory pain, but has not been studied in humans. Our aim was to assess the role of 17-HDHA and resolvins in heat pain sensitivity and in osteoarthritis pain in humans. Resolvins D1, D2, D3, D5, E1 and 17-HDHA, were measured by liquid chromatography-mass spectrometry and tested for association with heat pain thresholds in 250 healthy volunteers who had undergone quantitative sensory testing...
September 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28878195/1-945-25-dihydroxyvitamin-d3-attenuates-tgf-946-induced-pro-fibrotic-effects-in-human-lung-epithelial-cells-through-inhibition-of-epithelial-mesenchymal-transition
#14
Fei Jiang, Yong Yang, Lian Xue, Bingyan Li, Zengli Zhang
Pulmonary fibrosis is a progressive fibrotic lung disease of persisting lung injury and ineffective wound repair, with poor prognosis. Epithelial-mesenchymal transition (EMT) of alveolar epithelia cells is an early event in the development of pulmonary fibrosis, and transforming growth factor β (TGF-β) is an acknowledged inducer of EMT. Epidemiological studies demonstrated that serum levels of 25-hydroxy-vitamin D were associated with the presence of fibrosis diseases. We investigated whether vitamin D attenuated TGF-β-induced pro-fibrotic effects through inhibiting EMT in human alveolar epithelia A549 cells...
September 6, 2017: Nutrients
https://www.readbyqxmd.com/read/28876961/vitamin-d-replacement-improves-tear-osmolarity-in-patients-with-vitamin-d-deficiency
#15
Muhammed Kizilgul, Seyfullah Kan, Ozgur Ozcelik, Selvihan Beysel, Mahmut Apaydin, Bekir Ucan, Erman Cakal
BACKGROUND: Vitamin D deficiency is a common health problem worldwide. Many parts of the human eye, including the epithelium of the cornea, lens, ciliary body, and retinal pigment epithelium, as well as the corneal endothelium, ganglion cell layer, and retinal photoreceptors, contain vitamin D receptor (VDR). Dry eye is also a common health problem. An adequate tear film is required for maintaining health and function of the eye. Tear hyperosmolarity is considered to be the cause of ocular surface inflammation, symptoms, and tissue damage...
September 6, 2017: Seminars in Ophthalmology
https://www.readbyqxmd.com/read/28870774/ets-transcription-factor-family-member-gabpa-contributes-to-vitamin-d-receptor-target-gene-regulation
#16
Sabine Seuter, Antonio Neme, Carsten Carlberg
Binding motifs of the ETS-domain transcription factor GABPA are found with high significance below the summits of the vitamin D receptor (VDR) cistrome. VDR is the nuclear receptor for the biologically most active vitamin D metabolite 1α,25-dihydroxyvitamin D3 (1,25(OH)2D3). In this study, we determined the GABPA cistrome in THP-1 human monocytes and found that it is comprised of 3822 genomic loci, some 20% of which were modulated by 1,25(OH)2D3. The GABPA cistrome showed a high overlap rate with accessible chromatin and the pioneer transcription factor PU...
September 11, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28862080/evaluation-of-brain-targeted-chitosan-nanoparticles-through-blood-brain-barrier-cerebral-microvessel-endothelial-cells
#17
Adem Sahin, Digdem Yoyen-Ermis, Secil Caban-Toktas, Utku Horzum, Yesim Aktas, Patrick Couvreur, Gunes Esendagli, Yilmaz Capan
The blood-brain barrier is the major problem for the treatment of central nervous system diseases. A previous study from our group showed that the brain-targeted chitosan nanoparticles-loaded with large peptide moieties can rapidly cross the barrier and provide neuroprotection. The present study aims to determine the efficacy of the brain-targeted chitosan nanoparticles' uptake by the human blood-brain barrier cerebral microvessel endothelial cells (hCMECs) and to investigate the underlying mechanisms for enhanced cellular entry...
September 1, 2017: Journal of Microencapsulation
https://www.readbyqxmd.com/read/28860545/1%C3%AE-20s-dihydroxyvitamin-d3-interacts-with-vitamin-d-receptor-crystal-structure-and-route-of-chemical-synthesis
#18
Zongtao Lin, Hao Chen, Anna Y Belorusova, John C Bollinger, Edith K Y Tang, Zorica Janjetovic, Tae-Kang Kim, Zhongzhi Wu, Duane D Miller, Andrzej T Slominski, Arnold E Postlethwaite, Robert C Tuckey, Natacha Rochel, Wei Li
1α,20S-Dihydroxyvitamin D3 [1,20S(OH)2D3], a natural and bioactive vitamin D3 metabolite, was chemically synthesized for the first time. X-ray crystallography analysis of intermediate 15 confirmed its 1α-OH configuration. 1,20S(OH)2D3 interacts with the vitamin D receptor (VDR), with similar potency to its native ligand, 1α,25-dihydroxyvitamin D3 [1,25(OH)2D3] as illustrated by its ability to stimulate translocation of the VDR to the nucleus, stimulate VDRE-reporter activity, regulate VDR downstream genes (VDR, CYP24A1, TRPV6 and CYP27B1), and inhibit the production of inflammatory markers (IFNγ and IL1β)...
August 31, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28857231/challenges-in-the-development-of-dopamine-d2-and-d3-selective-radiotracers-for-pet-imaging-studies
#19
Robert H Mach, Robert R Luedtke
The dopamine D2-like receptors (i.e., D2/3 receptors) have been the most extensively studied CNS receptor with PET. The three different radiotracers which have been used in these studies are [(11) C]raclopride, [(18) F]fallypride, and [(11) C]PHNO. Since these radiotracers have a high affinity for both dopamine D2 and D3 receptors, the density of dopamine receptors in the CNS is reported as the D2/3 binding potential, which reflects a measure of the density of both receptor subtypes. Although the development of D2- and D3-selective PET radiotracers has been an active area of research for many years, this by and large presents an unmet need in the area of translational PET imaging studies...
August 31, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28855798/abnormalities-of-dopamine-d3-receptor-signaling-in-the-diseased-brain
#20
REVIEW
G Aleph Prieto
Dopamine D3 receptors (D3R) modulate neuronal activity in several brain regions including cortex, striatum, cerebellum, and hippocampus. A growing body of evidence suggests that aberrant D3R signaling contributes to multiple brain diseases, such as Parkinson's disease, essential tremor, schizophrenia, and addiction. In line with these findings, D3R has emerged as a potential target in the treatment of neurological disorders. However, the mechanisms underlying neuronal D3R signaling are poorly understood, either in healthy or diseased brain...
2017: Journal of Central Nervous System Disease
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