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D3 receptor

SeungHwan Lee, Xiang Qun Shi, Anni Fan, Brian West, Ji Zhang
Introduction Neuropathic pain is a debilitating condition. The importance of neuroimmune interactions in neuropathic pain has been evidenced by the involvement of different immune cells in peripheral and central sensitization of pathological pain. Macrophages and microglia are the most abundant immune cells activated in injured nerves and spinal cord, respectively. Several lines of evidence showed that macrophage/microglia survival, activation, proliferation, and differentiation require the involvement of macrophage-colony stimulating factor...
January 2018: Molecular Pain
Z Merhi, E Buyuk, M J Cipolla
STUDY QUESTION: Does vitamin D attenuate the adverse effects of advanced glycation end products (AGEs) on steroidogenesis by human granulosa cells (GCs)? SUMMARY ANSWER: AGEs alter the expression of genes important in steroidogenesis while 1,25-dihydroxyvitamin D3 (vit D3) in vitro attenuates some of the actions of AGEs on steroidogenic gene expression, possibly by downregulating the expression of the pro-inflammatory cell membrane receptor for AGEs (RAGE). WHAT IS KNOWN ALREADY: Vitamin D attenuates the pro-inflammatory effects of AGEs in non-ovarian tissues...
March 12, 2018: Molecular Human Reproduction
Mariusz Papp, Piotr Gruca, Magdalena Lason-Tyburkiewicz, Ewa Litwa, Monika Niemczyk, Katarzyna Tota-Glowczyk, Agata Faron-Gorecka, Maciej Kusmider, Joanna Solich, Marta Szlachta, Paul Willner
We have previously reported the effects of intracranial injections of dopamine D1, D2 and D3 ligands in animals subjected to the Novel Object Recognition (NOR) test following exposure to chronic mild stress (CMS) and chronic treatment with risperidone (RSP). Here, we present some molecular biological data from the same animals. It was predicted that brain-derived neurotrophic factor (BDNF) signalling in the prefrontal cortex (PFC) would reflect behavioural performance, implying an increase following acute administration of a D2 agonist or a D3 antagonist, blockade of this effect by CMS and its restoration by chronic RSP...
March 13, 2018: Behavioural Pharmacology
Hyun-Soo Kim, Mingzhen Zheng, Do-Kyung Kim, Won-Pyo Lee, Sang-Joun Yu, Byung-Ock Kim
Purpose: The purpose of this study was to evaluate the effects of 1,25-dihydroxyvitamin D3 on the proliferation, differentiation, and matrix mineralization of MC3T3-E1 osteoblast-like cells in vitro. Methods: MC3T3-E1 osteoblastic cells and 1,25-dihydroxyvitamin D3 were prepared. Cytotoxic effects and osteogenic differentiation were evaluated using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, alkaline phosphatase (ALP) activity assay, ALP staining, alizarin red S staining, and reverse transcription-polymerase chain reaction (RT-PCR) for osteogenic differentiation markers such as ALP, collagen type I (Col-I), osteocalcin (OCN), vitamin D receptor (VDR), and glyceraldehyde 3-phosphate dehydrogenase...
February 2018: Journal of Periodontal & Implant Science
Ginetta Collo, Laura Cavalleri, Federica Bono, Cristina Mora, Stefania Fedele, Roberto William Invernizzi, Massimo Gennarelli, Giovanna Piovani, Tilo Kunath, Mark J Millan, Emilio Merlo Pich, PierFranco Spano
The antiparkinsonian ropinirole and pramipexole are D3 receptor- (D3R-) preferring dopaminergic (DA) agonists used as adjunctive therapeutics for the treatment resistant depression (TRD). While the exact antidepressant mechanism of action remains uncertain, a role for D3R in the restoration of impaired neuroplasticity occurring in TRD has been proposed. Since D3R agonists are highly expressed on DA neurons in humans, we studied the effect of ropinirole and pramipexole on structural plasticity using a translational model of human-inducible pluripotent stem cells (hiPSCs)...
2018: Neural Plasticity
M Herian, M R Luck, M Grzesiak
Recently it has been shown that vitamin D(3) acting via its cognate receptor (VDR) regulates the growth, differentiation and function of female reproductive tissues including ovary. The aim of the study was to examine the effect of testosterone (T) and its antagonist 2-hydroxyflutamide (HF) on VDR protein expression and function in porcine ovarian follicles. Medium size antral follicles expressing great amount of androgen receptors and represent high steroidogenic activity were used in this research. After 6 h incubation of whole follicles with T, HF or T+HF, immunohistochemical analysis of VDR revealed its nuclear localization in granulosa and theca interna cells in control and experimental groups...
March 12, 2018: Physiological Research
Ho Pan Sham, Katherine H Walker, Raja-Elie E Abdulnour, Nandini Krishnamoorthy, David N Douda, Paul C Norris, Ioanna Barkas, Sarah Benito-Figueroa, Jennifer K Colby, Charles N Serhan, Bruce D Levy
Specialized proresolving mediators (SPMs) decrease NF-κB activity to prevent excessive tissue damage and promote the resolution of acute inflammation. Mechanisms for NF-κB regulation by SPMs remain to be determined. In this study, after LPS challenge, the SPMs 15-epi-lipoxin A4 (15-epi-LXA4 ), resolvin D1, resolvin D2, resolvin D3, and 17-epi-resolvin D1 were produced in vivo in murine lungs. In LPS-activated human bronchial epithelial cells, select SPMs increased expression of the NF-κB regulators A20 and single Ig IL-1R-related molecule (SIGIRR)...
March 9, 2018: Journal of Immunology: Official Journal of the American Association of Immunologists
Vida Sheikh, Pinar Kasapoglu, Alireza Zamani, Zahra Basiri, Ahmad Tahamoli-Roudsari, Mahdi Alahgholi-Hajibehzad
1 α, 25-dihydroxyvitamin D3 (VitD3) has been suggested to have strong modulatory properties in the immune system. Researchers in the present study primarily aimed to understand the effect of VitD3 on human CD4+ T cell proliferation in antigen presenting cells (APCs) free condition in vitro. The effect of VitD3 on intracellular cytokine responses trend to Th1, Th2, Th17 and Th22 was evaluated using the flow cytometry. Moreover the effect of VitD3 on the expression of inhibitory markers such as PD1, PD-L1, and CTLA4 which are induced upon polyclonal T cell receptor (TCR) activation on CD4+ T cells, was assessed...
March 6, 2018: Human Immunology
Zhanyi Gao, Kaining Liu, Huanxin Meng
BACKGROUND: The vitamin D pathway, from toll-like receptor activation to human cationic antimicrobial protein (hCAP-18/LL-37) generation, has been identified in monocytes and keratinocytes. This study aimed to investigate the vitamin D pathway in human gingival fibroblasts (hGFs) and periodontal ligament cells (hPDLCs) and to provide preliminary evidence of its role in periodontal immune defense. METHODS: Primary cultures of hGFs and hPDLCs were stimulated with 1,25-dihydroxy vitamin D3 and 25-hydroxy vitamin D3 , with or without Porphyromonas gingivalis lipopolysaccharide...
February 18, 2018: Journal of Periodontology
Ji-Kyung Choi, Grewo Lim, Iris Y Chen, Bruce G Jenkins
Methamphetamine (meth), and other psychostimulants such as cocaine, present a persistent problem for society with chronic users being highly prone to relapse. We show, in a chronic methamphetamine administration model, that discontinuation of drug for more than a week produces much larger changes in overall meth-induced brain connectivity and cerebral blood volume (CBV) response than changes that occur immediately following meth administration. Areas showing the largest changes were hippocampal, limbic striatum and sensorimotor cortical regions as well as brain stem areas including the pedunculopontine tegmentum (PPTg) and pontine nuclei - regions known to be important in mediating reinstatement of drug-taking after abstinence...
March 5, 2018: NeuroImage
Simon Cervenka
The dopamine (DA) system is considered to be centrally involved in the pathophysiology of several major psychiatric disorders. Using positron emission tomography (PET), aberrations in dopamine D2/D3-receptors (D2-R) levels and uptake of the DA precursor FDOPA have been shown for schizophrenia, substance abuse and depression. Radioligands for the dopamine D1-receptor (D1-R) have been available for more than three decades, however this receptor subtype has received much less attention in psychiatry research. Here, studies investigating D1-R in psychiatric patients in comparison to healthy control subjects are summarized...
March 5, 2018: Neuroscience Letters
Robert K Doot, Jacob G Dubroff, Kyle J Labban, Robert H Mach
Dopamine D3 receptors have key roles in behavioral reward, addiction, Parkinson's disease, and schizophrenia, and there is interest in studying their role in these disorders using PET. However, current PET radiotracers for studying D3 receptors in humans all bind to both D2 and D3 due to similarities between the two receptors. Selective D2 and D3 radioligands would aid investigation of the differences between D2 and D3 circuitry in the central nervous system. While there are currently in vitro measures of ligand D3/D2 selectivity, there is a need for an in vivo PET measure of D3/D2 selectivity...
March 5, 2018: Neuroscience Letters
Meixi Hao, Siyuan Hou, Lingjing Xue, Haoliang Yuan, Lulu Zhu, Cong Wang, Bin Wang, Chunming Tang, Can Zhang
Vitamin D3 receptor (VDR), belonging to the nuclear receptor superfamily, is a potential molecular target for anticancer drug discovery. In this study, a series of non-steroidal vitamin D analogs with phenyl-pyrrolyl pentane skeleton were synthesized with therapeutic potential for cancer treatment. Among them, 11b and 11g were identified as the most effective agents in reducing the viability of four cancer cell lines, particularly breast cancer cells, with IC50 values in the submicromolar concentration range...
March 8, 2018: Journal of Medicinal Chemistry
Hidekazu Sugiura, Ai Matsushita, Mayuko Futaya, Atsuko Teraoka, Ken-Ichi Akiyama, Noriyoshi Usui, Nobuo Nagano, Kosaku Nitta, Ken Tsuchiya
The hormone fibroblast growth factor 23 (FGF23) is secreted from bone and is involved in phosphorus (P) metabolism. FGF23 mainly binds the FGF receptor, which interacts with αKlotho in the kidney or parathyroid and regulates Na-dependent phosphate co-transporter type IIa (NaPi-IIa) and type IIc (NaPi-IIc) expression, 1,25-dihydroxyvitamin D3 (1,25(OH)2D3) activity, and parathyroid hormone (PTH) secretion. In this study, we utilized hemi-nephrectomized rats fed a high-P diet (HP Nx), rats subjected to a partial nephrectomy (PN) and rats with doxorubicin-induced renal failure (DXR) as chronic kidney disease (CKD) animal models and analyzed the P metabolism and FGF23 expression in the kidneys in each CKD model...
2018: PloS One
P Zhang, W Zhang, D Zhang, M Wang, R Aprecio, N Ji, O Mohamed, Y Li, Y Ding, Q Wang
BACKGROUND AND OBJECTIVE: Periodontitis is an increasingly prevalent complication of diabetes mellitus (known as diabetes mellitus-associated periodontitis), and 25-hydroxyvitamin D3 (25VD3 ) was recently found to be a critical regulator of innate immunity in this disease, but the underlying mechanisms remain poorly understood. T-cell protein tyrosine phosphatase non-receptor type 2 (PTPN2) is a potential downstream protein of the 25VD3 /vitamin D receptor pathway. The aim of this study was to investigate the regulation of PTPN2 in periodontal inflammation in diabetes mellitus-associated periodontitis...
March 8, 2018: Journal of Periodontal Research
Dake Song, Yaping Ge, Zhaodi Chen, Chao Shang, Ying Guo, Taiyun Zhao, Yunfeng Li, Ning Wu, Rui Song, Jin Li
Post-traumatic stress disorder (PTSD) is a complicated psychiatric disorder, which occurs after exposure to a traumatic event. The main clinical manifestation of PTSD includes fear and stress dysregulation. In both animals and humans, dysregulation of dopamine function appears to be related to conditioned fear responses. Previous studies show that the dopamine D3 receptor (D3R) is involved in schizophrenia, autism, and substance use disorders and is related to emotional disorders. However, few studies have investigated the role of the D3R in the pathogenesis and aetiology of PTSD...
March 3, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
Sophie Gong, Yuan Li, Wenji Su, Yu Ding, Jiaqi Lu, Kelly Dong, Steve Hood, Wandong Zhang, Georg C Terstappen
Antibody-triggered endocytosis (ATE) is a biological mechanism on which many therapeutic strategies are grounded, such as delivery of antibody-drug conjugates (ADCs). Current methods monitoring ATE include confocal Z-stack analysis, acid wash, antibody quenching, and pH-sensitive dye labeling. However, those generate less quantifiable results with low throughput. Here we report a new method referred to as "paired imaging measurement" to analyze ATE using a quantitative algorithm in conjunction with high-content imaging...
March 1, 2018: SLAS Discovery
Landon M Klein, Nicholas V Cozzi, Paul F Daley, Simon D Brandt, Adam L Halberstadt
Substantial effort has been devoted toward understanding the psychopharmacological effects of tryptamine hallucinogens, which are thought to be mediated by activation of 5-HT2A and 5-HT1A receptors. Recently, several psychoactive tryptamines based on the N,N-diallyltryptamine (DALT) scaffold have been encountered as recreational drugs. Despite the apparent widespread use of DALT derivatives in humans, little is known about their pharmacological properties. We compared the binding affinities of DALT and its 2-phenyl-, 4-acetoxy-, 4-hydroxy-, 5-methoxy-, 5-methoxy-2-methyl-, 5-fluoro-, 5-fluoro-2-methyl-, 5-bromo-, and 7-ethyl-derivatives at 45 receptor and transporter binding sites...
February 27, 2018: Neuropharmacology
Wenfeng Gao, Rui Wang, Xiaojun Wang, Hao Wu, Yang Wang, Xiaofan Lu, Li Li, Jiasheng Zheng, Wei Li
AIM: Vitamin D is involved in antiviral/antitumor activities. Its associations to hepatitis B virus (HBV), HIV and hepatocellular carcinoma (HCC) are unclear. MATERIALS & METHODS: A retrospective study was conducted on 232 chronic hepatitis B (CHB) patients and 72 HIV-infected patients. The correlation between serum 25(OH)D3 and 25 vitamin D receptor single nucleotide polymorphisms to disease progression and interferons were evaluated. RESULTS: The 25(OH)D3 was associated with HBV infection and progression...
September 2017: Biomarkers in Medicine
Holly P Quach, Tamara Dzekic, Paola Bukuroshi, K Sandy Pang
Vitamin D3 and the synthetic vitamin D analogs, 1α-hydroxyvitamin D3 [1α(OH)D3 ] and 1α-hydroxyvitamin D2 [1α(OH)D2 ], and 25-hydroxyvitamin D3 [25(OH)D3 ] were appraised for their vitamin D receptor (VDR) associated-potencies as cholesterol lowering agents in mice in vivo. These precursors require activation in vivo: 1α(OH)D3 and 1α(OH)D2 are activated by liver Cyp2r1 and Cyp27a1 to active VDR ligands, 1α,25-dihydroxyvitamin D3 [1,25(OH)2 D3 ] and 1α,25-dihydroxyvitamin D2 [1,25(OH)2 D2 ], respectively...
February 27, 2018: Biopharmaceutics & Drug Disposition
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