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dopamine 2 receptor

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https://www.readbyqxmd.com/read/29691888/pharmacological-characterization-of-a-%C3%AE-adrenergic-like-octopamine-receptor-in-plutella-xylostella
#1
Qing-Ting Huang, Hai-Hao Ma, Xi-Le Deng, Hang Zhu, Jia Liu, Yong Zhou, Xiao-Mao Zhou
The β-adrenergic-like octopamine receptor (OA2B2) belongs to the class of G-protein coupled receptors. It regulates important physiological functions in insects, thus is potentially a good target for insecticides. In this study, the putative open reading frame sequence of the Pxoa2b2 gene in Plutella xylostella was cloned. Orthologous sequence alignment, phylogenetic tree analysis, and protein sequence analysis all showed that the cloned receptor belongs to the OA2B2 protein family. PxOA2B2 was transiently expressed in HEK-293 cells...
April 25, 2018: Archives of Insect Biochemistry and Physiology
https://www.readbyqxmd.com/read/29686613/essential-control-of-the-function-of-the-striatopallidal-neuron-by-pre-coupled-complexes-of-adenosine-a-2a-dopamine-d-2-receptor-heterotetramers-and-adenylyl-cyclase
#2
Sergi Ferré, Jordi Bonaventura, Wendy Zhu, Candice Hatcher-Solis, Jaume Taura, César Quiroz, Ning-Sheng Cai, Estefanía Moreno, Verónica Casadó-Anguera, Alexxai V Kravitz, Kimberly R Thompson, Dardo G Tomasi, Gemma Navarro, Arnau Cordomí, Leonardo Pardo, Carme Lluís, Carmen W Dessauer, Nora D Volkow, Vicent Casadó, Francisco Ciruela, Diomedes E Logothetis, Daniel Zwilling
The central adenosine system and adenosine receptors play a fundamental role in the modulation of dopaminergic neurotransmission. This is mostly achieved by the strategic co-localization of different adenosine and dopamine receptor subtypes in the two populations of striatal efferent neurons, striatonigral and striatopallidal, that give rise to the direct and indirect striatal efferent pathways, respectively. With optogenetic techniques it has been possible to dissect a differential role of the direct and indirect pathways in mediating "Go" responses upon exposure to reward-related stimuli and "NoGo" responses upon exposure to non-rewarded or aversive-related stimuli, respectively, which depends on their different connecting output structures and their differential expression of dopamine and adenosine receptor subtypes...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29686254/the-relationship-between-dopamine-receptor-blockade-and-cognitive-performance-in-schizophrenia-a-11-c-raclopride-pet-study-with-aripiprazole
#3
Sangho Shin, Seoyoung Kim, Seongho Seo, Jae Sung Lee, Oliver D Howes, Euitae Kim, Jun Soo Kwon
Aripiprazole's effects on cognitive function in patients with schizophrenia are unclear because of the difficulty in disentangling specific effects on cognitive function from secondary effects due to the improvement in other schizophrenic symptoms. One approach to address this is to use an intermediate biomarker to investigate the relationship between the drug's effect on the brain and change in cognitive function. This study aims to investigate aripiprazole's effect on working memory by determining the correlation between dopamine D2/3 (D2/3) receptor occupancy and working memory of patients with schizophrenia...
April 24, 2018: Translational Psychiatry
https://www.readbyqxmd.com/read/29686073/neuronal-activity-regulates-neurotransmitter-switching-in-the-adult-brain-following-light-induced-stress
#4
Da Meng, Hui-Quan Li, Karl Deisseroth, Stefan Leutgeb, Nicholas C Spitzer
Neurotransmitter switching in the adult mammalian brain occurs following photoperiod-induced stress, but the mechanism of regulation is unknown. Here, we demonstrate that elevated activity of dopaminergic neurons in the paraventricular nucleus of the hypothalamus (PaVN) in the adult rat is required for the loss of dopamine expression after long-day photoperiod exposure. The transmitter switch occurs exclusively in PaVN dopaminergic neurons that coexpress vesicular glutamate transporter 2 (VGLUT2), is accompanied by a loss of dopamine type 2 receptors (D2Rs) on corticotrophin-releasing factor (CRF) neurons, and can lead to increased release of CRF...
April 23, 2018: Proceedings of the National Academy of Sciences of the United States of America
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/29684475/orexin-a-in-the-ventral-tegmental-area-enhances-saccharin-induced-conditioned-flavor-preference-the-role-of-d1-receptors-in-central-nucleus-of-amygdala
#6
Severiano Risco, Cristina Mediavilla
In industrialized societies, food intake is largely determined by its hedonic characteristics, which can be modified by our experience via taste learning. In this learning, the hedonic value of a neutral flavor changes after its association with a motivationally significant stimulus. Experiment 1 analyzes the effect of orexin administration (53 and 107 ng) in the ventral tegmental area (VTA) on hedonic intake through acquisition of a flavor-taste preference and a flavor-taste aversion. Accordingly, animals underwent four one-bottle acquisition sessions with unilateral application of orexin-A or saline in the VTA at 10 min before a 15-min flavor intake period...
April 20, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29683325/a-thieno-2-3-d-pyrimidine-scaffold-is-a-novel-negative-allosteric-modulator-of-the-dopamine-d2-receptor
#7
Tim John Fyfe, Barbara Zarzycka, Herman D Lim, Barrie Kellam, Shailesh N Mistry, Vsevolod Katritch, Peter J Scammells, J Robert Lane, Ben Capuano
Recently, a novel negative allosteric modulator (NAM) of the D2 -like dopamine receptors 1 was identified through virtual ligand screening. This ligand comprises a thieno[2,3- d]pyrimidine scaffold that does not feature in known dopaminergic ligands. Herein, we provide pharmacological validation of an allosteric mode of action for 1, revealing that it is a NAM of dopamine efficacy and identify the structural determinants of this allostery. We find that key structural moieties are important for functional affinity and negative cooperativity, whilst functionalization of the thienopyrimidine at the 5- and 6-positions results in analogues with divergent cooperativity profiles...
April 23, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29680151/vmat2-inhibitors-and-the-path-to-ingrezza-valbenazine
#8
Nicole D Harriott, John P Williams, Evan B Smith, Haig P Bozigian, Dimitri E Grigoriadis
The dopaminergic system plays a key role in the central nervous system, regulating executive function, arousal, reward, and motor control. Dysregulation of this critical monoaminergic system has been associated with diseases of the central nervous system including schizophrenia, Parkinson's disease, and disorders such as attention deficit hyperactivity disorders and addiction. Drugs that modify the dopaminergic system by modulating the activity of dopamine have been successful in demonstrating clinical efficacy by providing treatments for these diseases...
2018: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/29679989/d1-but-not-d2-dopamine-receptor-regulates-steroid-levels-during-the-final-stages-of-pikeperch-gametogenesis
#9
J Roche, D Żarski, A Khendek, I Ben Ammar, C Broquard, A Depp, Y Ledoré, T Policar, P Fontaine, S Milla
In pikeperch, Sander lucioperca, aquaculture hormonal treatment is usually applied to synchronize ovulation. However, the effect of dopamine (DA) receptor antagonists, in particular those blocking the D1 DA receptors, remains unknown. Thus, the aim of the present study was to investigate and compare the effects of D1 and D2 DA receptor antagonists on the sex-steroid production and reproductive performance of the species. Two experiments were performed during which mature pikeperch females were injected with different molecules: NaCl 0...
April 22, 2018: Animal: An International Journal of Animal Bioscience
https://www.readbyqxmd.com/read/29671013/ontogeny-of-cocaine-induced-behaviors-and-cocaine-pharmacokinetics-in-male-and-female-neonatal-preweanling-and-adult-rats
#10
Sanders A McDougall, Matthew G Apodaca, Alena Mohd-Yusof, Adrian D Mendez, Caitlin G Katz, Angie Teran, Israel Garcia-Carachure, Anthony T Quiroz, Cynthia A Crawford
RATIONALE: Ontogenetic differences in the behavioral responsiveness to cocaine have often been attributed to the maturation of dopaminergic elements (e.g., dopamine transporters, D2High receptors, receptor coupling, etc.). OBJECTIVE: The purpose of this study was to determine whether ontogenetic changes in cocaine pharmacokinetics might contribute to age-dependent differences in behavioral responsiveness. METHODS: Male and female neonatal (PD 5), preweanling (PD 10 and PD 20), and adult (PD 70) rats were injected (IP) with cocaine or saline and various behaviors (e...
April 18, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29670116/association-between-radiological-parameters-and-clinical-and-molecular-characteristics-in-human-somatotropinomas
#11
María R Alhambra-Expósito, Alejandro Ibáñez-Costa, Paloma Moreno-Moreno, Esther Rivero-Cortés, Mari C Vázquez-Borrego, Cristóbal Blanco-Acevedo, Álvaro Toledano-Delgado, María S Lombardo-Galera, Juan A Vallejo-Casas, Manuel D Gahete, Justo P Castaño, María A Gálvez, Raúl M Luque
Acromegaly is a rare but severe disease, originated in 95% of cases by a growth hormone-secreting adenoma (somatotropinoma) in the pituitary. Magnetic resonance imaging (MRI) is a non-invasive technique used for the diagnosis and prognosis of pituitary tumours. The aim of this study was to determine whether the use of T2-weighted signal intensity at MRI could help to improve the characterisation of somatotropinomas, by analysing its relationship with clinical/molecular features. An observational study was implemented in a cohort of 22 patients (mean age = 42...
April 18, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29669297/effects-of-apomorphine-a-dopamine-agonist-on-daphnia-magna-imaging-of-swimming-track-density-as-a-novel-tool-in-the-assessment-of-swimming-activity
#12
Adam Bownik, Natalia Sokołowska, Brygida Ślaska
Apomorphine (APO) is a non-selective agonist of dopamine receptor activating D2-like receptors. Although Daphnia has been used in neurotoxicology in toxicity testing, little is known on its behavioural and physiological responses to dopamine receptors ligands. Therefore, the aim of our study was to determine swimming behaviour (swimming track density, speed, turning activity) and physiological parameters such as heart rate, thoracic limb activity and post-abdominal claw movement frequency in daphnids exposed for 1, 2 and 4h to concentrations of 0...
April 15, 2018: Science of the Total Environment
https://www.readbyqxmd.com/read/29669266/the-strength-of-reward-related-learning-depends-on-the-degree-of-activation-of-ventral-tegmental-area-dopamine-neurons
#13
E Galaj, R Ranaldi
We tested whether (1) the capacity of a reward-associated conditioned stimulus (CS) to cause conditioned activation of ventral tegmental area (VTA) dopamine (DA) neurons is associated with its capacity to elicit conditioned approach responses and (2) whether the acquisition of these capacities by a CS requires N-methyl-D-aspartate (NMDA) and muscarinic acetylcholine (mACh) receptor stimulation. Rats were trained to emit a conditioned approach response to a light CS that was previously paired with food and were treated systemically with scopolamine (a mACh receptor antagonist) or MK-801 a (NMDA receptor antagonist) either prior to each conditioning session (during which animals experienced paired CS and food presentations) or prior to the conditioned approach (CS-only)...
April 15, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29666757/evolution-of-dopamine-receptors-phylogenetic-evidence-suggests-a-later-origin-of-the-drd-2l-and-drd-4rs-dopamine-receptor-gene-lineages
#14
Juan C Opazo, Kattina Zavala, Soledad Miranda-Rottmann, Roberto Araya
Dopamine receptors are integral membrane proteins whose endogenous ligand is dopamine. They play a fundamental role in the central nervous system and dysfunction of dopaminergic neurotransmission is responsible for the generation of a variety of neuropsychiatric disorders. From an evolutionary standpoint, phylogenetic relationships among the DRD1 class of dopamine receptors are still a matter of debate as in the literature different tree topologies have been proposed. In contrast, phylogenetic relationships among the DRD 2 group of receptors are well understood...
2018: PeerJ
https://www.readbyqxmd.com/read/29660611/effect-of-in-vivo-exposure-to-ambient-fine-particles-pm-2-5-on-the-density-of-dopamine-d-2-like-receptors-and-dopamine-induced-35-s-gtp%C3%AE-s-binding-in-rat-prefrontal-cortex-and-striatum-membranes
#15
María-de-Los-Angeles Andrade-Oliva, Octavio-Gamaliel Aztatzi-Aguilar, Francisco García-Sierra, Andrea De Vizcaya-Ruiz, José-Antonio Arias-Montaño
Male Sprague-Dawley rats (8-9 weeks-old) were exposed for three days (acute exposure) or eight weeks (subchronic exposure) to purified air or concentrated ambient fine particles, PM2.5 (≤2.5 μm; 15 to 18-fold of ambient air; 370-445 μg/m3 ). In membranes from rat prefrontal cortex (PFC) or striatum, the density and function of dopamine D2 -like receptors (D2 Rs) were assessed by [3 H]-spiperone binding and dopamine-stimulated [35 S]-GTPγS binding, respectively. Glial activation was evaluated by immunoperoxidase labeling of the glial fibrillary acidic protein (GFAP)...
April 10, 2018: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/29656800/dopaminergic-disturbances-in-tourette-syndrome-an-integrative-account
#16
REVIEW
Tiago V Maia, Vasco A Conceição
Tourette syndrome (TS) is thought to involve dopaminergic disturbances, but the nature of those disturbances remains controversial. Existing hypotheses suggest that TS involves 1) supersensitive dopamine receptors, 2) overactive dopamine transporters that cause low tonic but high phasic dopamine, 3) presynaptic dysfunction in dopamine neurons, or 4) dopaminergic hyperinnervation. We review evidence that contradicts the first two hypotheses; we also note that the last two hypotheses have traditionally been considered too narrowly, explaining only small subsets of findings...
March 9, 2018: Biological Psychiatry
https://www.readbyqxmd.com/read/29644470/ruthenium-ii-n-alkyl-phenothiazine-complexes-as-potential-anticancer-agents
#17
Andreja Leskovac, Sandra Petrovic, Tamara Lazarevic-Pasti, Milena Krstic, Vesna Vasic
In recent years, the search for effective anticancer compounds based on transition metal complexes has been the focus of medical investigations. The synergy between the ruthenium(II) and N-alkylphenothiazine counter-ions (chlorpromazine hydrochloride, thioridazine hydrochloride and trifluoperazine dihydrochloride, respectively) through the formation of three different complexes (1-3) was investigated. We explored whether the selected counter-ions and complexes might affect redox homeostasis and genome integrity of normal human blood cells, and induce an inhibition of Na+ /K+ -ATPase and AChE at pharmacologically relevant doses...
April 11, 2018: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/29626009/the-nurr1-ligand-1-1-bis-3-indolyl-1-p-chlorophenyl-methane-modulates-glial-reactivity-and-is-neuroprotective-in-mptp-induced-parkinsonism
#18
Sean L Hammond, Katriana A Popichak, Xi Li, Lindsay G Hunt, Evan H Richman, Pranav Damale, Edwin Chong, Donald S Backos, Stephen Safe, Ronald B Tjalkens
The orphan nuclear receptor, Nurr1 (NR4A2), regulates inflammatory gene expression in glial cells, as well as genes associated with homeostatic and trophic function in dopaminergic neurons. Despite these known functions of Nurr1, an endogenous ligand has not been discovered. We postulated that activation of Nurr1 would suppress activation of glia and thereby protect against loss of dopamine (DA) neurons following subacute lesioning with 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP). Our previous studies have shown that a synthetic Nurr1 ligand, 1,1-bis(3'-indolyl)-1-(p-chlorophenyl)methane (C-DIM12), suppresses inflammatory gene expression in primary astrocytes and induces a dopaminergic phenotype in neurons...
April 6, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29625570/the-inhibition-of-human-lung-fibroblast-proliferation-and-differentiation-by-gs-coupled-receptors-is-not-predicted-by-the-magnitude-of-camp-response
#19
Maxine J Roberts, Rebecca E Broome, Toby C Kent, Steven J Charlton, Elizabeth M Rosethorne
BACKGROUND: Idiopathic pulmonary fibrosis (IPF) is a chronic and progressive fibrotic lung disease for which there is no cure. Current therapeutics are only able to slow disease progression, therefore there is a need to explore alternative, novel treatment options. There is increasing evidence that the 3', 5' cyclic adenosine monophosphate (cAMP) pathway is an important modulator in the development of fibrosis, with increasing levels of cAMP able to inhibit cellular processes associated with IPF...
April 7, 2018: Respiratory Research
https://www.readbyqxmd.com/read/29618432/effects-of-single-administration-of-apomorphine-on-memory-and-monoamine-metabolism-a-dose-related-study
#20
Huma Ikram, Rumaisa Zakir, Darakhshan Jabeen Haleem
In the present study, we have monitored dose dependent effects of apomorphine on learning and memory. Behavioral sensitization and craving, which develop upon repeated treatment with dopamine receptor agonist apomorphine, are major limitations of the therapeutic use of apomorphine in Parkinson's patients. Effects of single (intraperitoneal) injection of apomorphine at different doses (i.e., 0.5, 1.0, & 2.0 mg/ml/kg) on locomotion in a familiar environment (Skinner's box) and memory in Morris water maze were investigated...
March 2018: Pakistan Journal of Pharmaceutical Sciences
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