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https://www.readbyqxmd.com/read/29751150/lipid-mediator-leukotriene-d-4-induces-airway-epithelial-cells-proliferation-through-egfr-erk1-2-pathway
#1
Neeraj Dholia, Umesh C S Yadav
BACKGROUND: Cysteinyl leukotrienes (CysLTs), the potent lipid inflammatory mediators, are elevated in many pathological conditions and implicated in various inflammatory diseases including asthma, however their role in airway epithelial cells modulation is not clearly understood. We have investigated the effects of a CysLT, Leukotriene D4 (LTD4 ) on human airway epithelial cells, and assessed its role and mode of action in these cells. METHODOLOGY: Human small airway epithelial cells (SAECs) and A549 cells were incubated with different concentrations of LTD4 for different time intervals...
May 8, 2018: Prostaglandins & Other Lipid Mediators
https://www.readbyqxmd.com/read/29743514/transcriptomic-integration-of-d-4-r-and-mor-signaling-in-the-rat-caudate-putamen
#2
Alejandra Valderrama-Carvajal, Haritz Irizar, Belén Gago, Haritz Jiménez-Urbieta, Kjell Fuxe, María C Rodríguez-Oroz, David Otaegui, Alicia Rivera
Morphine binding to opioid receptors, mainly to μ opioid receptor (MOR), induces alterations in intracellular pathways essential to the initial development of addiction. The activation of the dopamine D4 receptor (D4 R), which is expressed in the caudate putamen (CPu), mainly counteracts morphine-induced alterations in several molecular networks. These involve transcription factors, adaptive changes of MOR signaling, activation of the nigrostriatal dopamine pathway and behavioural effects, underlining functional D4 R/MOR interactions...
May 9, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29720711/in-vitro-and-in-vivo-characterization-of-pcc0104005-a-novel-modulator-of-serotonin-dopamine-activity-as-an-atypical-antipsychotic-drug
#3
Yanan Xu, Xiaoyin Zhu, Hongbo Wang, Shanyue Sun, Xin Yue, Jingwei Tian
PCC0104005 is a novel drug candidate for treating schizophrenia that displays high affinity for serotonin, dopamine, and noradrenaline receptors, including partial agonism at dopamine D2 , D3 , D4 , serotonin 5-HT1A , and 5-HT2A receptors and antagonism at 5-HT2B , 5-HT6 , and 5-HT7 receptors. PCC0104005 blocks MK-801-induced hyperactivity in rats, consistent with the reduction in dopamine D2 receptor stimulation and increased dopamine release in the medial prefrontal cortex. PCC0104005 inhibits 5-HTP-induced head twitches in rats, due to its moderate affinity for human 5-HT2A receptors (Ki = 5...
May 2, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29704613/regional-brain-volume-changes-following-chronic-antipsychotic-administration-are-mediated-by-the-dopamine-d2-receptor
#4
Elisa Guma, Jill Rocchetti, Gabriel A Devenyi, Arnaud Tanti, Axel Mathieu, Jason P Lerch, Guillaume Elgbeili, Blandine Courcot, Naguib Mechawar, M Mallar Chakravarty, Bruno Giros
BACKGROUND: Neuroanatomical alterations are well established in patients suffering from schizophrenia, however the extent to which these changes are attributable to illness, antipsychotic drugs (APDs), or their interaction is unclear. APDs have been extremely effective for treatment of positive symptoms in major psychotic disorders. Their therapeutic effects are mediated, in part, through blockade of D2-like dopamine (DA) receptors, i.e. the D2, D3 and D4 dopamine receptors. Furthermore, the dependency of neuroanatomical change on DA system function and D2-like receptors has yet to be explored...
April 25, 2018: NeuroImage
https://www.readbyqxmd.com/read/29686048/fear-memory-recall-potentiates-opiate-reward-sensitivity-through-dissociable-dopamine-d1-vs-d4-receptor-dependent-memory-mechanisms-in-the-prefrontal-cortex
#5
Jing Jing Li, Hanna Szkudlarek, Justine Renard, Roger Hudson, Walter Rushlow, Steven R Laviolette
Disturbances in prefrontal cortical (PFC) dopamine (DA) transmission are well-established features of psychiatric disorders involving pathological memory processing, such as post-traumatic stress disorder (PTSD) and opioid addiction. Transmission through PFC DA D4 receptors (D4R) has been shown to potentiate the emotional salience of normally non-salient emotional memories whereas transmission through PFC DA D1 receptors (D1R) has been demonstrated to selectively block recall of reward or aversion-related associative memories...
April 23, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29685001/cysteinyl-leukotrienes-c4-and-d4-downregulate-human-mast-cell-expression-of-toll-like-receptors-1-through-7
#6
V Karpov, R Ilarraza, A Catalli, M Kulka
Cysteinyl leukotrienes (CysLT) are potent inflammatory lipid molecules that mediate some of the pathophysiological responses associated with asthma such as bronchoconstriction, vasodilation and increased microvascular permeability. As a result, CysLT receptor antagonists (LRA), such as montelukast, have been used to effectively treat patients with asthma. We have recently shown that mast cells are necessary modulators of innate immune responses to bacterial infection and an important component of this innate immune response may involve the production of CysLT...
March 2018: Journal of Biological Regulators and Homeostatic Agents
https://www.readbyqxmd.com/read/29678723/modulatory-effect-of-dopamine-receptor-5-on-the-neurosecretory-dahlgren-cells-of-the-olive-flounder-paralichthys-olivaceus
#7
Zhaohui Lan, Wei Zhang, Jinling Xu, Mo Zhou, Yingxin Chen, Huafeng Zou, Weiqun Lu
A neuromodulatory role for dopamine has been reported for magnocellular neuroendocrine cells in the mammalian hypothalamus. We examined its potential role as a local intercellular messenger in the neuroendocrine Dahlgren cell population of the caudal neurosecretory system (CNSS) of the euryhaline flounder Paralichthys olivaceus. In vitro application of dopamine (DA) caused an increase in electrical activity (firing frequency, recorded extracellularly) of Dahlgren cells, recruitment of previously silent cells, together with a greater proportion of cells showing phasic (irregular) activity...
April 17, 2018: General and Comparative Endocrinology
https://www.readbyqxmd.com/read/29589445/1-3-4-butylpiperidin-1-yl-propyl-1-2-3-4-tetrahydroquinolin-2-one-77-lh-28-1-as-a-model-for-the-rational-design-of-a-novel-class-of-brain-penetrant-ligands-with-high-affinity-and-selectivity-for-dopamine-d4-receptor
#8
Fabio Del Bello, Alessandro Bonifazi, Gianfabio Giorgioni, Carlo Cifani, Maria Vittoria Micioni Di Bonaventura, Riccardo Petrelli, Alessandro Piergentili, Stefano Fontana, Valerio Mammoli, Hideaki Yano, Rosanna Matucci, Giulio Vistoli, Wilma Quaglia
In the present paper, the M1 mAChR bitopic agonist 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1, 1) has been demonstrated to show unexpected D4R selectivity over D2R and D3R and to behave as a D4R antagonist. To better understand the structural features required for the selective interaction with the D4R and obtain compounds unable to activate mAChRs, the aliphatic butyl chain and the piperidine nucleus of 1 were modified, affording compounds 2-14. The 4-benzylpiperidine 9 and the 4-phenylpiperazine 12 showed high D4R affinity and selectivity not only over the other D2-like subtypes, but also over M1-M5 mAChRs...
March 28, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29587204/leukotriene-d4-induces-cellular-senescence-in-osteoblasts
#9
Jinsong Wei, Siyuan Chen, Weixiong Guo, Bailin Feng, Shukai Yang, Chengshuo Huang, Jiaqi Chu
Aging is associated with the development of osteoporosis, in which cellular senescence in osteoblasts plays a key role. Leukotriene D4 (LTD4), an important cysteinyl leukotriene (cysLT), is a powerful pro-inflammatory mediator formed from arachidonic acid. However, little information regarding the effects of LTD4 on the pathogenesis of osteoporosis has been reported before. In the present study, we defined the physiological roles of LTD4 in cellular senescence in osteoblasts. Our results indicate that LTD4 treatment decreased the expression of SIRT1 in a dose-dependent manner in MC3T3-E1 osteoblastic cells...
March 24, 2018: International Immunopharmacology
https://www.readbyqxmd.com/read/29579709/the-novel-piperazine-containing-compound-lqfm018-necroptosis-cell-death-mechanisms-dopamine-d-4-receptor-binding-and-toxicological-assessment
#10
Fabiana Bettanin Costa, Alane P Cortez, Renato Ivan de Ávila, Flávio S de Carvalho, Wanessa M Andrade, Andrezza F da Cruz, Karinna B Reis, Ricardo Menegatti, Luciano M Lião, Luiz Antônio S Romeiro, François Noël, Carlos Alberto M Fraga, Eliezer J Barreiro, Germán Sanz, Marcella F Rodrigues, Boniek G Vaz, Marize Campos Valadares
Piperazine is a promising scaffold for drug development due to its broad spectrum of biological activities. Based on this, the new piperazine-containing compound LQFM018 (2) [ethyl 4-((1-(4-chlorophenyl)-1H-pyrazol-4-yl)methyl)piperazine-1-carboxylate] was synthetized and some biological activities investigated. In this work, we described its ability to bind aminergic receptors, antiproliferative effects as well as the LQFM018 (2)-triggered cell death mechanisms, in K562 leukemic cells, by flow cytometric analyses...
March 23, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29575277/association-study-of-functional-polymorphisms-of-dopaminergic-pathway-in-epilepsy-related-factors-of-temporal-lobe-epilepsy-in-brazilian-population
#11
Juliana A Alcantara, Silvia Vincentiisa, Daniel S Kerr, Bernardo Dos Santos, Ruda Alessi, Helio van der Linden, Tiffany Chaim, Maurício H Serpa, Geraldo Busatto, Wagner F Gattaz, Renata Demarque, Kette Dr Valente
BACKGROUND: There is scarce data about the role of neurotransmission modulated by dopamine (DA) in epilepsy, especially temporal lobe epilepsy. This is the first study that aimed to analyze the dopaminergic polymorphisms in an etiologically homogeneous group of patients with temporal lobe epilepsy determined by hippocampal sclerosis (TLE-HS). Selected polymorphisms were: (i) the most expressed receptors in the limbic system D2-like (DRD2/ANKK1 TAQ-1A, D4_VNTR, and D4_rs1800955); (ii) the dopamine transporter DAT - 3 'untranslated region (3'UTR) and Intron 8; (iii) two degrading enzymes regulating the synaptic activity - the main metabolizer of dopamine Catechol-O-methyltransferase (COMT) and monoamine oxidase A (MAOA)...
March 25, 2018: European Journal of Neurology: the Official Journal of the European Federation of Neurological Societies
https://www.readbyqxmd.com/read/29570875/adenosine-a-2a-receptors-modulate-the-dopamine-d-2-receptor-mediated-inhibition-of-synaptic-transmission-in-the-mouse-prefrontal-cortex
#12
Joana I Real, Ana Patrícia Simões, Rodrigo A Cunha, Samira G Ferreira, Daniel Rial
Prefrontal cortex (PFC) circuits are modulated by dopamine acting on D1 - and D2 -like receptors, which are pharmacologically exploited to manage neuropsychiatric conditions. Adenosine A2A receptors (A2 A R), also control PFC-related responses and A2 A R antagonists are potential anti-psychotic drugs. Since tight antagonistic A2 A R-D2 R and synergistic A2 A R-D1 R interactions occur in other brain regions, we now investigated the cross-talk between A2 A R and D1 /D2 R controlling synaptic transmission between layers II/III and V in mouse PFC coronal slices...
March 23, 2018: European Journal of Neuroscience
https://www.readbyqxmd.com/read/29564731/dopamine-d4-receptor-gene-associated-with-the-frontal-striatal-cerebellar-loop-in-children-with-adhd-a-resting-state-fmri-study
#13
Andan Qian, Xin Wang, Huiru Liu, Jiejie Tao, Jiejie Zhou, Qiong Ye, Jiance Li, Chuang Yang, Jingliang Cheng, Ke Zhao, Meihao Wang
Attention deficit hyperactivity disorder (ADHD) is a common childhood neuropsychiatric disorder that has been linked to the dopaminergic system. This study aimed to investigate the effects of regulation of the dopamine D4 receptor (DRD4) on functional brain activity during the resting state in ADHD children using the methods of regional homogeneity (ReHo) and functional connectivity (FC). Resting-state functional magnetic resonance imaging data were analyzed in 49 children with ADHD. All participants were classified as either carriers of the DRD4 4-repeat/4-repeat (4R/4R) allele (n = 30) or the DRD4 2-repeat (2R) allele (n = 19)...
March 21, 2018: Neuroscience Bulletin
https://www.readbyqxmd.com/read/29552726/%C3%AE-2a-and-%C3%AE-2c-adrenoceptors-as-potential-targets-for-dopamine-and-dopamine-receptor-ligands
#14
Marta Sánchez-Soto, Verònica Casadó-Anguera, Hideaki Yano, Brian Joseph Bender, Ning-Sheng Cai, Estefanía Moreno, Enric I Canela, Antoni Cortés, Jens Meiler, Vicent Casadó, Sergi Ferré
The poor norepinephrine innervation and high density of Gi/o-coupled α2A - and α2C -adrenoceptors in the striatum and the dense striatal dopamine innervation have prompted the possibility that dopamine could be an effective adrenoceptor ligand. Nevertheless, the reported adrenoceptor agonistic properties of dopamine are still inconclusive. In this study, we analyzed the binding of norepinephrine, dopamine, and several compounds reported as selective dopamine D2 -like receptor ligands, such as the D3 receptor agonist 7-OH-PIPAT and the D4 receptor agonist RO-105824, to α2 -adrenoceptors in cortical and striatal tissue, which express α2A -adrenoceptors and both α2A - and α2C -adrenoceptors, respectively...
March 18, 2018: Molecular Neurobiology
https://www.readbyqxmd.com/read/29551965/the-dopamine-receptor-d4-gene-drd4-and-financial-risk-taking-stimulating-and-instrumental-risk-taking-propensity-and-motivation-to-engage-in-investment-activity
#15
Rafał Muda, Mariusz Kicia, Małgorzata Michalak-Wojnowska, Michał Ginszt, Agata Filip, Piotr Gawda, Piotr Majcher
The Dopamine receptor D4 gene (DRD4) has been previously linked to financial risk-taking propensity. Past works demonstrated that individuals with a specific variant of the DRD4 gene (7R+) are more risk-seeking than people without it (7R-). The most prominent explanation for this effect is the fact that 7R+ individuals are less sensitive to dopamine and thus seek more stimulation to generate "normal" dopaminergic activity and feel pleasure. However, results about this relationship have not been conclusive, and some revealed a lack of the relationship...
2018: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/29502220/characterization-of-a-drug-targetable-allosteric-site-regulating-vascular-endothelial-growth-factor-signaling
#16
Katherine M Thieltges, Dragana Avramovic, Chayne L Piscitelli, Sandra Markovic-Mueller, Hans Kaspar Binz, Kurt Ballmer-Hofer
Vascular endothelial growth factors (VEGFs) regulate blood and lymph vessel development upon activation of three receptor tyrosine kinases (VEGFRs). The extracellular domain of VEGFRs consists of seven Ig-homology domains, of which D2-3 form the ligand-binding site, while the membrane proximal domains D4-7 are involved in homotypic interactions in ligand-bound receptor dimers. Based on low-resolution structures, we identified allosteric sites in D4-5 and D7 of vascular endothelial growth factor receptor 2 (VEGFR-2) accomplishing regulatory functions...
March 3, 2018: Angiogenesis
https://www.readbyqxmd.com/read/29490167/new-maresin-conjugates-in-tissue-regeneration-pathway-counters-leukotriene-d-4-stimulated-vascular-responses
#17
Nan Chiang, Ian R Riley, Jesmond Dalli, Ana R Rodriguez, Bernd W Spur, Charles N Serhan
Resolution of acute inflammation is governed, in part, by lipid mediator class switching from proinflammatory eicosanoids to specialized proresolving mediators, including a recently identified new pathway of mediators, termed maresin conjugates in tissue regeneration (MCTR), which includes MCTR1, MCTR2, and MCTR3. Here, we addressed whether each MCTR can impact the known vascular actions of cysteinyl leukotrienes. Leukotriene D4 (LTD4 ; 1.5 nmol/mouse) initiated vascular leakage in mouse cremaster vessels, which was reduced (>75%) by MCTR1 and MCTR2 (0...
February 28, 2018: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/29470989/redox-exchange-of-the-disulfides-of-human-two-domain-cd4-regulates-the-conformational-dynamics-of-each-domain-providing-insight-into-its-mechanisms-of-control
#18
Gavin R Owen, Doris Le, Stoyan Stoychev, Nichole M Cerutti, Maria Papathanasopoulos
CD4, a membrane glycoprotein expressed by specific leukocytes, plays a vital role in the human immune response and acts as a primary receptor for HIV entry. Of its four ecto-domains (D1-D4), D1, D2, and D4 each contain a distinctive disulfide bond. Whereas the disulfides of D1 and D4 are more traditional in nature, providing structural functions, that of D2 is referred to as an "allosteric" disulfide due to its high dihedral strain energy and relative ease of reduction that is thought to regulate CD4 structure and function by shuffling its redox state...
March 4, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29466428/hemagglutinin-specific-neutralization-of-subacute-sclerosing-panencephalitis-viruses
#19
Miguel Ángel Muñoz-Alía, Claude P Muller, Stephen J Russell
Subacute sclerosing panencephalitis (SSPE) is a progressive, lethal complication of measles caused by particular mutants of measles virus (MeV) that persist in the brain despite high levels of neutralizing antibodies. We addressed the hypothesis that antigenic drift is involved in the pathogenetic mechanism of SSPE by analyzing antigenic alterations in the MeV envelope hemagglutinin protein (MeV-H) found in patients with SSPE in relation to major circulating MeV genotypes. To this aim, we obtained cDNA for the MeV-H gene from tissue taken at brain autopsy from 3 deceased persons with SSPE who had short (3-4 months, SMa79), average (3...
2018: PloS One
https://www.readbyqxmd.com/read/29466326/structure-of-the-d2-dopamine-receptor-bound-to-the-atypical-antipsychotic-drug-risperidone
#20
Sheng Wang, Tao Che, Anat Levit, Brian K Shoichet, Daniel Wacker, Bryan L Roth
Dopamine is a neurotransmitter that has been implicated in processes as diverse as reward, addiction, control of coordinated movement, metabolism and hormonal secretion. Correspondingly, dysregulation of the dopaminergic system has been implicated in diseases such as schizophrenia, Parkinson's disease, depression, attention deficit hyperactivity disorder, and nausea and vomiting. The actions of dopamine are mediated by a family of five G-protein-coupled receptors. The D2 dopamine receptor (DRD2) is the primary target for both typical and atypical antipsychotic drugs, and for drugs used to treat Parkinson's disease...
March 8, 2018: Nature
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