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https://www.readbyqxmd.com/read/28440817/effects-of-dopamine-d2-d3-receptor-antagonism-on-human-planning-and-spatial-working-memory
#1
M Naef, U Müller, A Linssen, L Clark, T W Robbins, C Eisenegger
Psychopharmacological studies in humans suggest important roles for dopamine (DA) D2 receptors in human executive functions, such as cognitive planning and spatial working memory (SWM). However, studies that investigate an impairment of such functions using the selective DA D2/3 receptor antagonist sulpiride have yielded inconsistent results, perhaps because relatively low doses were used. We believe we report for the first time, the effects of a higher (800 mg p.o.) single dose of sulpiride as well as of genetic variation in the DA receptor D2 gene (DA receptor D2 Taq1A polymorphism), on planning and working memory...
April 25, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28433688/vitamin-d-downregulates-the-il-23-receptor-pathway-in-human-mucosal-ilc3
#2
Viktoria Konya, Paulo Czarnewski, Marianne Forkel, Anna Rao, Efthymia Kokkinou, Eduardo J Villablanca, Sven Almer, Ulrik Lindforss, Danielle Friberg, Charlotte Höög, Peter Bergman, Jenny Mjösberg
BACKGROUND: Vitamin D deficiency is a risk factor for inflammatory bowel disease (IBD). The IL-23-driven tissue-resident ILC3 play essential roles in intestinal immunity, and targeting IL-23/12 is a promising approach in IBD therapy. OBJECTIVE: We set out to define the role of 1α,25-dihydroxy vitamin D3 (1,25D) in regulating functional responses of human mucosal ILC3 to IL-23 plus IL-1β stimulation. METHODS: Transcriptomes of sorted tonsil ILC3 were assessed by microarray analysis...
April 19, 2017: Journal of Allergy and Clinical Immunology
https://www.readbyqxmd.com/read/28430709/vitamin-d3-repressed-astrocyte-activation-following-lipopolysaccharide-stimulation-in-vitro-and-in-neonatal-rats
#3
Ke-Ping Jiao, Shao-Min Li, Wen-Yan Lv, Ming-Liang Jv, Hai-Yan He
Vitamin D3 has been reported to be an immunity modulator and high levels of vitamin D3 are correlated with a decreased risk for developing diseases in the central nervous system. Astrocytes are important immune cells and contribute toward inflammation during neurological diseases. The vitamin D receptor has been reported to be expressed in astrocytes; however, the effect of vitamin D3 on astrocyte activation has not been studied. Here, we found that lipopolysaccharide stimulation in astrocytes could enhance the expression of vitamin D receptor and Cyp27B1, which encodes the enzyme for converting vitamin D3 into its active form...
April 20, 2017: Neuroreport
https://www.readbyqxmd.com/read/28427048/1-25-dihydroxyvitamin-d3-attenuates-the-effects-of-lipopolysaccharide-by-causing-adam10-dependent-ectodomain-shedding-of-toll-like-receptor-4
#4
Won Seok Yang, Jin Ju Kim, Nam Jeong Han, Eun Kyoung Lee, Su-Kil Park
BACKGROUND/AIMS: We investigated how 1,25-dihydroxyvitamin D3 (1,25D3) inhibits the effects of lipopolysaccharide (LPS) in human aortic endothelial cells. METHODS: Cellular signaling was explored by determination of protein abundance with Western blot, measurement of cytosolic Ca2+ concentration and immunofluorescence staining for a disintegrin and metalloprotease 10 (ADAM10). RESULTS: LPS stimulated the expression of intercellular adhesion molecule 1 (ICAM-1) through toll-like receptor 4 (TLR4) and subsequent activation of p38 mitogen-activated protein kinase (p38 MAPK)...
April 17, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28426179/novel-selective-and-developable-dopamine-d3-antagonists-with-modified-amino-region
#5
Fabrizio Micheli
This minireview describes the presentation made at the XXIV National Meeting in Medicinal Chemistry held in Perugia (Italy) in 2016, September 11-14. It relates to the discovery of novel templates of the so called "amino" region of the Dopamine D3 antagonists. Moving from the early scaffolds which were modified in the amine portion, the review describes the variations which led to the discovery of new systems which were published in 2016 allowing the identification of molecules endowed of great selectivity over DA D2 receptor and hERG channel...
April 20, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28421623/a-preliminary-investigation-of-the-effect-of-acute-alcohol-on-dopamine-transmission-as-assessed-by-11-c-phno
#6
Thulasi Thiruchselvam, Alan A Wilson, Isabelle Boileau, Bernard Le Foll
BACKGROUND: Previous positron emission tomography (PET) studies exploring the effect of acute alcohol on dopamine (DA) levels have yielded inconsistent results, with only some studies suggesting increased synaptic DA levels after an alcohol challenge. The D2 /D3 agonist radiotracer, [(11) C]-(+)-propyl-hexahydro-naphtho-oxazin ([(11) C]-(+)-PHNO), has greater sensitivity to synaptic DA fluctuation than previously used antagonist radiotracers and is in principle more suitable for imaging alcohol-induced changes in DA...
April 19, 2017: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/28416594/new-repeat-polymorphism-in-the-akt1-gene-predicts-striatal-dopamine-d2-d3-receptor-availability-and-stimulant-induced-dopamine-release-in-the-healthy-human-brain
#7
Elena Shumay, Corinde E Wiers, Ehsan Shokri-Kojori, Sung Won Kim, Colin A Hodgkinson, Hui Sun, Dardo Tomasi, Christopher T Wong, Daniel R Weinberger, Gene-Jack Wang, Joanna S Fowler, Nora D Volkow
The role of the protein kinase Akt1 in dopamine neurotransmission is well recognized and has been implicated in schizophrenia and psychosis. However, the extent to which variants in the AKT1 gene influence dopamine neurotransmission is not well understood.Here we investigated the effect of a newly characterized variant number tandem repeat (VNTR) polymorphism in AKT1 (major alleles: L- (8 repeats) and H- (9 repeats)) on striatal dopamine D2/D3 receptor (DRD2) availability and on dopamine release in healthy volunteers...
April 17, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28412753/vitamin-d-increases-programmed-death-receptor-1-expression-in-crohn-s-disease
#8
Mia Bendix, Stinne Greisen, Anders Dige, Christian L Hvas, Nina Bak, Søren P Jørgensen, Jens F Dahlerup, Bent Deleuran, Jørgen Agnholt
BACKGROUND: Vitamin D modulates inflammation in Crohn's disease (CD). Programmed death (PD)-1 receptor contributes to the maintenance of immune tolerance. Vitamin D might modulate PD-1 signalling in CD. AIM: To investigate PD-1 expression on T cell subsets in CD patients treated with vitamin D or placebo. METHODS: We included 40 CD patients who received 1200 IU vitamin D3 for 26 weeks or placebo and eight healthy controls. Peripheral blood mononuclear cells (PBMCs) and plasma were isolated at baseline and week 26...
April 11, 2017: Oncotarget
https://www.readbyqxmd.com/read/28408985/new-drugs-in-psychiatry-focus-on-new-pharmacological-targets
#9
REVIEW
Filippo Caraci, Gian Marco Leggio, Salvatore Salomone, Filippo Drago
The approval of psychotropic drugs with novel mechanisms of action has been rare in recent years. To address this issue, further analysis of the pathophysiology of neuropsychiatric disorders is essential for identifying new pharmacological targets for psychotropic medications. In this report, we detail drug candidates being examined as treatments for psychiatric disorders. Particular emphasis is placed on agents with novel mechanisms of action that are being tested as therapies for depression, schizophrenia, or Alzheimer's disease...
2017: F1000Research
https://www.readbyqxmd.com/read/28408289/dopaminergic-control-of-anxiety-in-young-and-aged-zebrafish
#10
Victoria Kacprzak, Neil A Patel, Elizabeth Riley, Lili Yu, Jing-Ruey J Yeh, Irina V Zhdanova
Changes in the expression of the dopamine transporter (DAT), or the sensitivity of dopamine receptors, are associated with aging and substance abuse and may underlie some of the symptoms common to both conditions. In this study, we explored the role of the dopaminergic system in the anxiogenic effects of aging and acute cocaine exposure by comparing the behavioral phenotypes of wild type (WT) and DAT knockout zebrafish (DAT-KO) of different ages. To determine the involvement of specific dopamine receptors in anxiety states, antagonists to D1 (SCH23390) and D2/D3 (sulpiride) were employed...
April 10, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28402705/interaction-of-factor-h-binding-protein-of-streptococcus-suis-with-globotriaosylceramide-promotes-the-development-of-meningitis
#11
Decong Kong, Zhe Chen, Junping Wang, Qingyu Lv, Hua Jiang, Yuling Zheng, Maokai Xu, Xuyu Zhou, Huaijie Hao, Yongqiang Jiang
Streptococcus suis is an important emerging zoonotic agent that causes acute bacterial meningitis in humans with high mortality and morbidity. Our previous work showed that factor H-binding protein (Fhb) contributed to virulence of S. suis, but the role of Fhb in the development of S. suis meningitis remained unclear. In this study, we demonstrated for the first time that Fhb contributed to the traversal of S. suis across the human blood-brain barrier by allelic-exchange mutagenesis, complementation and specific antibody blocking studies...
April 12, 2017: Virulence
https://www.readbyqxmd.com/read/28399453/structure-activity-relationship-study-of-vitamin-d-analogs-with-oxolane-group-in-their-side-chain
#12
Anna Y Belorusova, Andrea Martínez, Zoila Gándara, Generosa Gómez, Yagamare Fall, Natacha Rochel
Synthetic analogs of 1α,25-dihydroxyvitamin D3 (1,25(OH)2D3) have been developed with the goal of improving the biological profile of the natural hormone for therapeutic applications. Derivatives of 1,25(OH)2D3 with the oxolane moiety branched in the side chain at carbon C20, act as Vitamin D nuclear Receptor (VDR) superagonists being several orders of magnitude more active than the natural ligand. Here, we describe the synthesis and biological evaluation of three diastereoisomers of (1S, 3R)-Dihydroxy-(20S)-[(2″-hydroxy-2″-propyl)-tetrahydrofuryl]-22,23,24,25,26,27-hexanor-1α-hydroxyvitamin D3, with different stereochemistry at positions C2 and C5 of the oxolane ring branched at carbon C22 (1, C2RC5S; 2, C2SC5R; 3, C2SC5S)...
April 2, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28393228/microarray%C3%A2-based-screening-of-differentially-expressed-genes-in-glucocorticoid%C3%A2-induced-avascular-necrosis
#13
Gangyong Huang, Yibing Wei, Guanglei Zhao, Jun Xia, Siqun Wang, Jianguo Wu, Feiyan Chen, Jie Chen, Jingshen Shi
The underlying mechanisms of glucocorticoid (GC)‑induced avascular necrosis of the femoral head (ANFH) have yet to be fully understood, in particular the mechanisms associated with the change of gene expression pattern. The present study aimed to identify key genes with a differential expression pattern in GC‑induced ANFH. E‑MEXP‑2751 microarray data were downloaded from the ArrayExpress database. Differentially expressed genes (DEGs) were identified in 5 femoral head samples of steroid‑induced ANFH rats compared with 5 placebo‑treated rat samples...
April 5, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28389358/microrna-125b-inhibits-aml-cells-differentiation-by-directly-targeting-fes
#14
Jinhang Hu, Lufeng Zheng, Xiao Shen, Yan Zhang, Cheng Li, Tao Xi
MicroRNA-125b (miR-125b) has been reported to be upregulated in several kinds of leukemia, suggesting that miR-125b plays a role in Leukemia development. In this study, it was shown that miR-125b expression level decreased in response to 1α, 25-dihydroxy-vitamin D3 (1,25D3) in a dose- and time-dependent manner and miR-125b blocked 1,25D3-induced monocytic differentiation of U937 cells. In addition, miR-125b decreased mRNA expression of myelomonocytic differentiation markers, including CD11c, CD18 and CD64 and arrested the cell cycle at the S phase in U937 and HL60 cells...
April 4, 2017: Gene
https://www.readbyqxmd.com/read/28381354/1-25-dihydroxyvitamin-d3-prevents-deleterious-effects-of-homocysteine-on-mitochondrial-function-and-redox-status-in-heart-slices
#15
Aline Longoni, Janaina Kolling, Cassiana Siebert, João Paulo Dos Santos, Jussemara Souza da Silva, Letícia F Pettenuzzo, Leo Anderson Meira-Martins, Carlos-Alberto Gonçalves, Adriano M de Assis, Angela T S Wyse
Because homocysteine (Hcy) is a risk factor for cardiovascular disease, and vitamin D deficiency can contribute to cardiovascular pathologies. In the present study, we tested the hypothesis that Hcy could impair energy metabolism, mitochondrial function, and redox status in heart slices of Wistar rats and that 1,25-dihydroxivitamin D3 (calcitriol) treatment could prevent such effects. Heart slices were first pretreated with 3 different concentrations of calcitriol (50, 100, and 250nmol/L) for 30minutes at 37°C, after which Hcy was added to promote deleterious effects on metabolism...
February 2017: Nutrition Research
https://www.readbyqxmd.com/read/28373650/vitamin-d3-inhibits-micro-rna-17-92-to-promote-specific-immunotherapy-in-allergic-rhinitis
#16
Zhi-Jian Yu, Lu Zeng, Xiang-Qian Luo, Xiao-Rui Geng, Rui Xu, Kun Chen, Gui Yang, Xi Luo, Zhi-Qiang Liu, Zhi-Gang Liu, Da-Bo Liu, Ping-Chang Yang, Hua-Bin Li
It is recognized that T helper 2 (Th2) polarization plays a critical role in a large number of immune disorders. Yet, the remedies for reconciling the established Th2 polarization are still limited currently. Published data indicate that micro RNA-17-92 cluster is associated with the skewed immune response; 25 vitamin D3 (VD3) can regulate multiple bioactivities in the body. This study tests a hypothesis that VD3 facilitates the effect of specific immunotherapy (SIT) on Th2 response. We observed that treatment with either SIT or VD3 alleviated AR symptoms as well as reduced serum levels of specific IgE and T helper (Th) 2 cytokines, suppressed miR-19a (one of the members of the miR-17-92 cluster) and increased IL-10 in peripheral B cells, which was further improved in those AR patients treated with both SIT and VD3...
April 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28373127/rp5063-an-atypical-antipsychotic-drug-with-a-unique-pharmacologic-profile-improves-declarative-memory-and-psychosis-in-mouse-models-of-schizophrenia
#17
Lakshmi Rajagopal, Sunoh Kwon, Mei Huang, Eric Michael, Laxminarayan Bhat, Marc Cantillon, Herbert Y Meltzer
Various types of atypical antipsychotic drugs (AAPDs) modestly improve the cognitive impairment associated with schizophrenia (CIAS). RP5063 is an AAPD with a diverse and unique pharmacology, including partial agonism at dopamine (DA) D2, D3, D4, serotonin (5-HT)1A, and 5-HT2A receptors (Rs), full agonism at α4β2 nicotinic acetylcholine (ACh)R (nAChR), and antagonism at 5-HT2B, 5-HT6, and 5-HT7Rs. Most atypical APDs are 5-HT2A inverse agonists. The efficacy of RP5063 in mouse models of psychosis and episodic memory were studied...
March 31, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28372324/apolipoprotein-e-isoforms-differentially-regulate-alzheimer-s-disease-and-amyloid-%C3%AE-induced-inflammatory-response-in-vivo-and-in-vitro
#18
Evan Dorey, Michelle Bamji-Mirza, Dema Najem, Yan Li, Hong Liu, Debbie Callaghan, Douglas Walker, Lih-Fen Lue, Danica Stanimirovic, Wandong Zhang
Neuroinflammation plays a critical role in neuronal dysfunction and death of Alzheimer's disease (AD). ApoE4 is a major risk factor of AD, while ApoE2 is neuroprotective. Little is known about the roles of ApoE isoforms in the neuroinflammation seen in AD. Their roles and mechanisms in Aβ-induced/neuroinflammation were investigated in this study using in vivo and in vitro models. Rat astrocytes were treated with lipid-poor recombinant hApoE and/or Aβ42. Mouse astrocyte lines-expressing lipidated hApoE were treated with Aβ42 and/or vitamin D receptor (VDR) agonist, 1α,25-dihydroxyvitamin D3...
2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28368577/classics-in-chemical-neuroscience-aripiprazole
#19
Austen B Casey, Clinton E Canal
Aripiprazole was the first antipsychotic developed to possess agonist properties at dopamine D2 autoreceptors, a groundbreaking strategy that presented a new vista for schizophrenia drug discovery. The dopamine D2 receptor is the crucial target of all extant antipsychotics, and all developed prior to aripiprazole were D2 receptor antagonists. Extensive blockade of these receptors, however, typically produces extrapyramidal (movement) side effects, which plagued first-generation antipsychotics, such as haloperidol...
April 13, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28361444/functional-roles-of-t3-37-and-s5-46-in-the-activation-mechanism-of-the-dopamine-d1-receptor
#20
Estefanía A Hugo, Bruce K Cassels, Angélica Fierro
The activation mechanism of dopamine receptors is unknown. The amino acids S5.42, S5.43, and S5.46 located in helix 5 appear to be crucial, but their specific roles in receptor activation have not been studied. We modeled the D1 dopamine receptor using the crystal structures of the D3 dopamine and β2 adrenergic receptors. Molecular dynamics simulations show that the interaction of dopamine with the D1 receptor leads to the formation of a hydrogen-bond network with its catechol group and helices 3, 5, and 6, including water molecules...
April 2017: Journal of Molecular Modeling
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