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D1 D2 D3 D4 D5

Irene Sebastianutto, Natallia Maslava, Corey R Hopkins, M Angela Cenci
Rodent models of l-DOPA-induced dyskinesia (LID) are essential to investigate pathophysiological mechanisms and treatment options. Ratings of abnormal involuntary movements (AIMs) are used to capture both qualitative and quantitative features of dyskinetic behaviors. Thus far, validated rating scales for the mouse have anchored the definition of severity to the time during which AIMs are present. Here we have asked whether the severity of axial, limb, and orolingual AIMs can be objectively assessed with scores based on movement amplitude...
September 2, 2016: Neurobiology of Disease
Ahmed Nasri, Soufiane Jouili, Fehmi Boufahja, Amor Hedfi, Ibtihel Saidi, Ezzeddine Mahmoudi, Patricia Aïssa, Naceur Essid, Beyrem Hamouda
Trophic structure of free living nematode from Bizerte lagoon was tested by a microcosmic study after 30 days of exposure with 5 increasing doses of pharmaceutical penicillin G (D1: 3 mg L(-1), D2: 30 mg L(-1), D3: 300 mg L(-1), D4: 600 mg L(-1), D5: 700 mg L(-1)). Results showed significant differences between nematode assemblages from undisturbed controls and those from penicillin G treatments. Selective deposit-feeders (1A) or nonselective deposit-feeders (1B), very abundant in the control microcosm, were significantly affected and their dominance declined significantly...
August 2016: Ecotoxicology
Eugenia V Gurevich, Raul R Gainetdinov, Vsevolod V Gurevich
Actions of the neurotransmitter dopamine in the brain are mediated by dopamine receptors that belong to the superfamily of G protein-coupled receptors (GPCRs). Mammals have five dopamine receptor subtypes, D1 through D5. D1 and D5 couple to Gs/olf and activate adenylyl cyclase, whereas D2, D3, and D4 couple to Gi/o and inhibit it. Most GPCRs upon activation by an agonist are phosphorylated by GPCR kinases (GRKs). The GRK phosphorylation makes receptors high-affinity binding partners for arrestin proteins. Arrestin binding to active phosphorylated receptors stops further G protein activation and promotes receptor internalization, recycling or degradation, thereby regulating their signaling and trafficking...
September 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Antoni Cortés, Estefanía Moreno, Mar Rodríguez-Ruiz, Enric I Canela, Vicent Casadó
INTRODUCTION: Dopamine is a neurotransmitter widely distributed in both the periphery and the central nervous system (CNS). Its physiological effects are mediated by five closely related G protein-coupled receptors (GPCRs) that are divided into two major subclasses: the D1-like (D1, D5) and the D2-like (D2, D3, D4) receptors. D3 receptors (D3Rs) have the highest density in the limbic areas of the brain, which are associated with cognitive and emotional functions. These receptors are therefore attractive targets for therapeutic management...
July 2016: Expert Opinion on Drug Discovery
Matthew F Lazenka, Luke P Legakis, S Stevens Negus
Dopamine acts through dopamine Type I receptors (comprising D1 and D5 subtypes) and dopamine Type II receptors (comprising D2, D3, and D4 subtypes). Intracranial self-stimulation (ICSS) is 1 experimental procedure that can be used to evaluate abuse-related effects of drugs targeting dopamine receptors. This study evaluated effects of dopamine receptor ligands on ICSS in rats using experimental procedures that have been used previously to examine abused indirect dopamine agonists such as cocaine and amphetamine...
June 2016: Experimental and Clinical Psychopharmacology
Malte Heykants, Esther Mahabir
The goal was to increase pseudopregnant mice production by estrous cycle staging by visual examination before pairing and to determine the effect of such pseudopregnant recipients on embryo transfer. To compare methods of estrous cycle staging over 14 days, groups consisted of 10 females in proestrus-estrus and 10 vasectomized males; group 1: only daily visual observation; group 2: daily visual observation and cytological examination on day 1; group 3: daily visual observation and daily cytological examination...
March 15, 2016: Theriogenology
Kei Yamamoto, Romain Fontaine, Catherine Pasqualini, Philippe Vernier
Dopamine neurotransmission regulates various brain functions, and its regulatory roles are mediated by two families of G protein-coupled receptors: the D1 and D2 receptor families. In mammals, the D1 family comprises two receptor subtypes (D1 and D5), while the D2 family comprises three receptor subtypes (D2, D3 and D4). Phylogenetic analyses of dopamine receptor genes strongly suggest that the common ancestor of Osteichthyes (bony jawed vertebrates) possessed four subtypes in the D1 family and five subtypes in the D2 family...
2015: Brain, Behavior and Evolution
Dong Joon Lee, Henry C Tseng, Sing Wai Wong, Zhengyan Wang, Meng Deng, Ching-Chang Ko
Multiple growth factors (e.g., BMP2, TGF-β1, FGF2) and isolated genes have been shown to improve osteoblastic proliferation and mineralization, advancing bone tissue engineering. Among these factors, both polydopamine (PDA) and dopamine (DA) monomer have recently been reported to increase osteoblast proliferation and mineralization in vitro. Although a well-characterized neurotransmitter, DA's role in the bone is unknown. We hypothesize that DA can directly act on osteoblasts, and examined whether osteoblasts express DA receptors that respond to exogenous DA...
2015: Bone Research
Fang-Fang Zhang, Jing Li
Alzheimer's disease is the common cause of dementia characterized by the accumulation of amyloid-β produced by breakage of amyloid-β precursor protein (APP). The present study was designed to synthesize and investigate the effect of chloroquine derivatives on the expression of presenilin. Among the five chloroquine derivatives (D1, D2, D3, D4 and D5) synthesized, D5 with diisopropyl substitution was found to be most effect. The results from western blot analysis showed the inhibition of presenilin 1 protein expression on treatment with chloroquine derivative D5 in Daudi cells...
2015: International Journal of Clinical and Experimental Pathology
Marco Antonio Góngora-Meléndez, Armando Magaña-Cobos, Juan Manuel Montiel-Herrera, Cinthya Lorena Pantoja-Minguela, Mario Luis Pineda-Maldonado, Eduardo Enrique Piñeyro-Beltrán
Food allergy prevalence has increased during the last years, affecting 15-20% of children, in this case, egg allergy affects from 0.5-2.5%. Most of the egg allergic reactions are type I or IgE mediated antibodies against egg proteins. Five major proteins have been identified: ovomucoid (Gal d1), ovoalbumin (Gal d2), ovotransferrin (Gal d3), lysozyme (Gal d4) and albumin (Gal d5). Ovomucoid protein, which is found in the egg white, is heat resistant and enzyme resistant. This protein is the most allergenic and the most common in egg composition...
July 2015: Revista Alergia Mexico: Organo Oficial de la Sociedad Mexicana de Alergia e Inmunología, A.C
Valentina Bruno, Alicia Valiente-Gómez, Oscar Alcoverro
Clozapine is a major atypical antipsychotic drug used in treatment-resistant schizophrenia (Patel and Allin. Ther Adv Psychopharmacol 2011;1:25-29). It interferes with dopamine binding to D1, D2, D3, and D5 receptors but has high affinity to D4. It also has an anticholinergic effect and antagonizes α-adrenergic, histaminergic, and serotoninergic receptors (Oerther and Ahlenius. J Pharmacol Exp Ther 2000;292:731-736). Clozapine has proved effective in treating positive and negative symptoms in patients with refractory schizophrenia, thus accounting for its frequent use...
July 2015: Clinical Neuropharmacology
Karen Pintado-Palomino, Oscar Peitl Filho, Edgar Dutra Zanotto, Camila Tirapelli
OBJECTIVES: To evaluate the efficacy of experimental proposals of desensitizing agents during tooth bleaching. METHODS: 140 participants without tooth sensitivity (TS) received 16% carbamide peroxide (14 days-04 h each) (T1) or 35% hydrogen peroxide (single session-45 min) (T2). Participants used concomitantly (10 per group): desensitizing dentifrices (D1-experimental bioactive glass-ceramic; D2-commercial potassium nitrate; D3-commercial calcium and sodium phosphosilicate) in-home, daily and, desensitizing pastes (D4-experimental bioactive glass-ceramic; D5-experimental Bioglass type 45S5; D6-commercial calcium phosphate), in-office, immediately after the treatment and more 4 times...
September 2015: Journal of Dentistry
Ahmed Nasri, Soufiane Jouili, Fehmi Boufahja, Amor Hedfi, Ezzeddine Mahmoudi, Patricia Aïssa, Naceur Essid, Hamouda Beyrem
A microcosm experiment was conducted to examine the effects of the pharmaceutical (penicillin G) on free living nematode communities of a Tunisian coastal zone (South-Western Mediterranean Sea). Sediments were contaminated with five penicillin G dose [D1 (3 mgL(-1)), D2 (30 mgL(-1)), D3 (300 mgL(-1)), D4 (600 mgL(-1)), D5 (700 mgL(-1))], and effects were examined after 30 days. Results showed significant differences between nematode assemblages from undisturbed controls and those from penicillin G treatments...
July 2015: Environmental Toxicology and Pharmacology
Jojanneke H J Huck, Dorette Freyer, Chotima Böttcher, Mihovil Mladinov, Claudia Muselmann-Genschow, Mareike Thielke, Nadine Gladow, Dana Bloomquist, Philipp Mergenthaler, Josef Priller
Dopamine is the predominant catecholamine in the brain and functions as a neurotransmitter. Dopamine is also a potent immune modulator. In this study, we have characterized the expression of dopamine receptors on murine microglia. We found that cultured primary microglia express dopamine D1, D2, D3, D4, and D5 receptors. We specifically focused on the D2 receptor (D2R), a major target of antipsychotic drugs. Whereas D2Rs were strongly expressed on striatal neurons in vivo, we did not detect any D2R expression on resident microglia in the healthy brains of wild-type mice or transgenic mice expressing the green fluorescent protein (GFP) under the control of the Drd2 promoter...
November 2015: Journal of Cerebral Blood Flow and Metabolism
Ying Zhang, Ruipan Zheng, Xiangzhi Meng, Lulu Wang, Li Liu, Yan Gao
OBJECTIVE: To date, there are no reports on the cellular localization of dopamine receptors in the human pancreas. In our study, we determined the localization and expression of 5 dopamine receptors (D(1), D(2), D(3), D(4), and D(5)) in normal human pancreas tissue. METHODS: Human nonpathological pancreas tissues were fixed with 4% paraformaldehyde, paraffin-embedded, and processed for immunohistochemical analysis to detect dopamine receptors in the human pancreas tissue by using double immunofluorescent labeling and confocal microscopy...
August 2015: Pancreas
F J B Mendonça Júnior, L Scotti, H Ishiki, S P S Botelho, M S Da Silva, M T Scotti
Benzodiazepines (BZ or BZD) are a class of gabaminergic psychoactive chemicals used in hypnotics, sedation, in the treatment of anxiety, and in other CNS disorders. These drugs include alprazolam (Xanax), diazepam (Valium), clonazepam (Klonopin), and others. There are two distinct types of pharmacological binding sites for benzodiazepines in the brain (BZ1 and BZ2), these sites are on GABA-A receptors, and are classified as short, intermediate, or long-acting. From the thienobenzodiazepine class (TBZ), Olanzapine (2-methyl-4-(4-methyl-l-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine) (Zyprexa) was used as an example to demonstrate the antagonism of this class of compounds for multiples receptors including: dopamine D1-D5, α-adrenoreceptor, histamine H1, muscarinic M1-M5 and 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3 and 5-HT6 receptors...
2015: Mini Reviews in Medicinal Chemistry
Jean-Martin Beaulieu, Stefano Espinoza, Raul R Gainetdinov
The variety of physiological functions controlled by dopamine in the brain and periphery is mediated by the D1, D2, D3, D4 and D5 dopamine GPCRs. Drugs acting on dopamine receptors are significant tools for the management of several neuropsychiatric disorders including schizophrenia, bipolar disorder, depression and Parkinson's disease. Recent investigations of dopamine receptor signalling have shown that dopamine receptors, apart from their canonical action on cAMP-mediated signalling, can regulate a myriad of cellular responses to fine-tune the expression of dopamine-associated behaviours and functions...
January 2015: British Journal of Pharmacology
Andres D Ramirez, Sean M Smith
Abnormal dopamine neurotransmission has been linked to a wide array of motor, cognitive, and psychiatric disorders. Dopamine binds and regulates intracellular signals through D1-like (D1 and D5) and D2-like (D2, D3, and D4) G-protein coupled receptors. Activation of D1- like receptors stimulates cAMP/PKA signaling via Gs mediated activation of adenylyl cyclase. In contrast, activation of D2-like receptors inhibits cAMP/PKA signaling by Gi inhibition of adenylyl cyclase. In the brain, dopamine signaling is tightly regulated by cyclic nucleotide phosphodiesterases (PDEs)...
2014: Central Nervous System Agents in Medicinal Chemistry
Abhed Pandey, Shuichi Satoh
The present study aimed to investigate the effect of phosphorus and various organic acids supplementation on growth, nutrient retention and loading in rainbow trout fed on low fishmeal based diets. Five experimental diets were formulated, Diet D1 (0.5P) was positive control with 0.5% inorganic phosphorus addition and D2 (0P, negative control) without addition of inorganic phosphorus. D3, D4 and D5 were supplemented with 1% fumaric (FuA), formic (FoA) and acetic (AA) acids, respectively. All the diets were fed until satiation to duplicate groups of 25 fish for 12 weeks...
November 2014: Journal of Environmental Biology
Fabian G Mueck, Sebastian Roesch, Michael Scherr, Florian Fischer, Lucas Geyer, Oliver Peschel, Daniel Maxien, Silke Grabherr, Stefan Wirth
RATIONALE AND OBJECTIVES: Dose reduction may compromise patients because of a decrease of image quality. Therefore, the amount of dose savings in new dose-reduction techniques needs to be thoroughly assessed. To avoid repeated studies in one patient, chest computed tomography (CT) scans with different dose levels were performed in corpses comparing model-based iterative reconstruction (MBIR) as a tool to enhance image quality with current standard full-dose imaging. MATERIALS AND METHODS: Twenty-five human cadavers were scanned (CT HD750) after contrast medium injection at different, decreasing dose levels D0-D5 and respectively reconstructed with MBIR...
March 2015: Academic Radiology
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