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Dopamine D2

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https://www.readbyqxmd.com/read/28429261/localization-of-the-dopamine-receptors-of-types-1-and-2-on-the-bodies-of-pomc-expressing-neurons-of-the-arcuate-nucleus-of-the-hypothalamus-in-mice-and-rats
#1
I V Romanova, A L Mikhrina, A O Shpakov
Using immunofluorescent techniques, we have demonstrated the presence of two main types of dopamine receptors, D1 and D2, on the bodies of neurons of the arcuate nucleus of the hypothalamus expressing the precursor of peptides of the melanocortin family proopiomelanocortin in C57Bl/6J mice and Wistar rats. These data show close functional relationship between the dopamine and melanocortin systems of the brain and involvement of dopamine in the control of synthesis and secretion of peptides of the melanocortin family...
January 2017: Doklady Biological Sciences: Proceedings of the Academy of Sciences of the USSR, Biological Sciences Sections
https://www.readbyqxmd.com/read/28426179/novel-selective-and-developable-dopamine-d3-antagonists-with-modified-amino-region
#2
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/28424607/multivariate-analysis-of-18-f-dmfp-pet-data-to-assist-the-diagnosis-of-parkinsonism
#3
Fermín Segovia, Juan M Górriz, Javier Ramírez, Francisco J Martínez-Murcia, Johannes Levin, Madeleine Schuberth, Matthias Brendel, Axel Rominger, Kai Bötzel, Gaëtan Garraux, Christophe Phillips
An early and differential diagnosis of parkinsonian syndromes still remains a challenge mainly due to the similarity of their symptoms during the onset of the disease. Recently, (18)F-Desmethoxyfallypride (DMFP) has been suggested to increase the diagnostic precision as it is an effective radioligand that allows us to analyze post-synaptic dopamine D2/3 receptors. Nevertheless, the analysis of these data is still poorly covered and its use limited. In order to address this challenge, this paper shows a novel model to automatically distinguish idiopathic parkinsonism from non-idiopathic variants using DMFP data...
2017: Frontiers in Neuroinformatics
https://www.readbyqxmd.com/read/28421623/a-preliminary-investigation-of-the-effect-of-acute-alcohol-on-dopamine-transmission-as-assessed-by-11-c-phno
#4
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/28421257/histone-deacetylase-inhibitors-reverse-age-related-increases-in-side-effects-of-haloperidol-in-mice
#5
Janitza L Montalvo-Ortiz, Daniel W Fisher, Guadalupe Rodríguez, Deyu Fang, John G Csernansky, Hongxin Dong
BACKGROUND: Older patients can be especially susceptible to antipsychotic-induced side effects, and the pharmacodynamic mechanism underlying this phenomenon remains unclear. We hypothesized that age-related epigenetic alterations lead to decreased expression and functionality of the dopamine D2 receptor (D2R), contributing to this susceptibility. METHODS: In this study, we treated young (2-3 months old) and aged (22-24 months old) C57BL/6 mice with the D2R antagonist haloperidol (HAL) once a day for 14 days to evaluate HAL-induced motor side effects...
April 18, 2017: Psychopharmacology
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
#6
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/28416380/spinal-dopaminergic-involvement-in-the-antihyperalgesic-effect-of-antidepressants-in-a-rat-model-of-neuropathic-pain
#7
Mi Chen, Hajime Hoshino, Shigeru Saito, Yang Yang, Hideaki Obata
Antidepressants such as tricyclic antidepressants, and serotonin noradrenaline reuptake inhibitors are a first-line treatment for neuropathic pain. Here, we aimed to determine the involvement of the spinal dopaminergic system in the antihyperalgesic effects of antidepressants in a rat model of neuropathic pain induced by spinal nerve ligation (SNL). The right L5 spinal nerve of male Sprague-Dawley rats was ligated under inhalation anesthesia to induce hyperalgesia. Behavioral testing was performed by measuring ipsilateral hindpaw withdrawal thresholds after intraperitoneal injection of amitriptyline, duloxetine, milnacipran, and fluoxetine...
April 14, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28412910/aripiprazole-a-drug-that-displays-partial-agonism-and-functional-selectivity
#8
Erin W Tuplin, Matthew R Holahan
The treatment of schizophrenia is challenging due to the wide range of symptoms (positive, negative, cognitive) associated with the disease. Typical antipsychotics that antagonize D2 receptors are effective in treating positive symptoms, but extrapyramidal side-effects (EPS) are a common occurrence. Atypical antipsychotics targeting 5-TH2A and D2 receptors are more effective at treating cognitive and negative symptoms compared to typical antipsychotics, but these drugs also result in side-effects such as metabolic syndromes...
April 13, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28411401/expression-of-stem-cell-markers-and-dopamine-d2-receptors-in-human-and-rat-prolactinomas
#9
Zhichao Gao, Lin Cai, Jianglong Lu, Chengde Wang, Qun Li, Jian Chen, Xiaoxiao Song, Xianbin Chen, Linlin Zhang, Weiming Zheng, Zhipeng Su
BACKGROUND Dopamine agonists (DAs) are the first-line treatment for prolactinomas. DAs primarily target the dopamine D2 receptor (D2R). Tumor stem-like cells (TSLCs) are associated with the tolerance to radiotherapy and chemotherapy. TSLCs have also been identified in pituitary adenomas. We aimed to characterize the expression pattern of stem cell markers and D2R in human and rat prolactinomas. MATERIAL AND METHODS Human prolactinoma specimens (n=14) were obtained from patients with surgical resection. The xenograft model of rat prolactinomas was generated by endermically injecting MMQ cells, HE and PRL were confirmed by immunohistochemical staining of tumor sections, and the expression of serum PRL was measured by ELISA...
April 15, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28411257/relief-of-pain-depressed-behavior-in-rats-by-activation-of-d1-like-dopamine-receptors
#10
Matthew F Lazenka, Kelen C Freitas, Sydney Henck, S Stevens Negus
Clinically significant pain often includes depression of both behavior and mesolimbic dopamine signaling. Indirect and/or direct dopamine receptor agonists may alleviate pain-related behavioral depression. To test this hypothesis, the present study compared effects of indirect and direct dopamine agonists in a preclinical assay of pain-depressed operant responding. Male Sprague-Dawley rats with chronic indwelling microelectrodes in the medial forebrain bundle were trained in an intracranial self-stimulation (ICSS) procedure to press a lever for pulses of electrical brain stimulation...
April 14, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28409407/associations-between-dopamine-d2-receptor-drd2-gene-maternal-positive-parenting-and-trajectories-of-depressive-symptoms-from-early-to-mid-adolescence
#11
Cong Cao, Jolien Rijlaarsdam, Anja van der Voort, Linqin Ji, Wenxin Zhang, Marian J Bakermans-Kranenburg
Using data from the Longitudinal Study of Chinese Children and Adolescents (LSCCA), this study is the first to examine the roles of the dopamine D2 receptor (DRD2) gene polymorphisms (i.e., TaqIA and A241G) and maternal positive parenting at ages 10 and 11 years in the trajectories of depressive symptoms from early to mid-adolescence (ages 11 to 16 years). In a sample of 1090 Chinese adolescents (50% girls), three trajectories of depressive symptoms were identified: (i) low-stable (36.1%), (ii) moderate-increasing (44...
April 13, 2017: Journal of Abnormal Child Psychology
https://www.readbyqxmd.com/read/28408289/dopaminergic-control-of-anxiety-in-young-and-aged-zebrafish
#12
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 wildtype (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/28407307/adenosine-a1-receptors-measured-with-11-c-mpdx-pet-in-early-parkinson-s-disease
#13
Masahiro Mishina, Kenji Ishii, Yuichi Kimura, Masahiko Suzuki, Shin Kitamura, Kenji Ishibashi, Muneyuki Sakata, Keiichi Oda, Shiro Kobayashi, Kazumi Kimura, Kiichi Ishiwata
Adenosine A1 receptors (A1 Rs) interact negatively with dopamine D1 receptors (D1 Rs) in neurons of the basal ganglia's direct pathway, while adenosine A2A receptors (A2A Rs) negatively interact with dopamine D2 receptors (D2 Rs) in indirect-pathway neurons. The aim of this study was to investigate the cerebral density of A1 Rs in Parkinson's disease (PD) in its early stages, using PET scans with the radioligand 8-dicyclopropylmethyl-1-(11) C-methyl-3-propylxanthine ((11) C-MPDX). We studied 10 drug-naïve patients with early PD...
April 13, 2017: Synapse
https://www.readbyqxmd.com/read/28406384/lack-of-increase-in-sexual-drive-and-function-after-dopaminergic-stimulation-in-women
#14
Tillmann H C Krüger, Lydia Keil, Stefanie Jung, Kai G Kahl, Matthias Wittfoth, Brigitte Leeners, Uwe Hartmann
Human and animal data indicate that the dopaminergic system plays a crucial role in sexual drive and function. Using a double-blind, placebo-controlled crossover design this prototype-study investigated the effect of the D2-dopamine agonist cabergoline on sexual parameters in thirteen healthy women. Cardiovascular and genital parameters were monitored continuously. Sexual drive and function were measured using self-report sexual experience scales. In contrast to previous theories and assumptions we found that cabergoline did not alter objective and subjective sexual parameters in healthy women...
April 13, 2017: Journal of Sex & Marital Therapy
https://www.readbyqxmd.com/read/28404690/pharmacologic-characterization-of-valbenazine-nbi-98854-and-its-metabolites
#15
Dimitri E Grigoriadis, Evan Smith, Sam R J Hoare, Ajay Madan, Haig Bozigian
The vesicular monoamine transporter 2 (VMAT2) is an integral presynaptic protein that regulates the packaging and subsequent release of dopamine and other monoamines from neuronal vesicles into the synapse. Valbenazine (NBI-98854), a novel compound that selectively inhibits VMAT2, is being developed for the treatment of tardive dyskinesia. Valbenazine is converted to two significant circulating metabolites in vivo, namely, (+)-α-dihydrotetrabenazine (R,R,R-DHTBZ) and a mono-oxy metabolite, NBI-136110. Radioligand binding studies were conducted to assess and compare valbenazine, tetrabenazine and their respective metabolites in their abilities to selectively and potently inhibit [(3)H]-DHTBZ binding to VMAT2 in rat striatal, rat forebrain, and human platelet homogenates...
April 12, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28398340/the-impact-of-common-dopamine-d2-receptor-gene-polymorphisms-on-d2-3-receptor-availability-c957t-as-a-key-determinant-in-putamen-and-ventral-striatum
#16
C T Smith, L C Dang, J W Buckholtz, A M Tetreault, R L Cowan, R M Kessler, D H Zald
Dopamine function is broadly implicated in multiple neuropsychiatric conditions believed to have a genetic basis. Although a few positron emission tomography (PET) studies have investigated the impact of single-nucleotide polymorphisms (SNPs) in the dopamine D2 receptor gene (DRD2) on D2/3 receptor availability (binding potential, BPND), these studies have often been limited by small sample size. Furthermore, the most commonly studied SNP in D2/3 BPND (Taq1A) is not located in the DRD2 gene itself, suggesting that its linkage with other DRD2 SNPs may explain previous PET findings...
April 11, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28396166/paeoniflorin-and-liquiritin-two-major-constituents-in-chinese-herbal-formulas-used-to-treat-hyperprolactinemia-associated-disorders-inhibits-prolactin-secretion-in-prolactinoma-cells-by-different-mechanisms
#17
Yuanyi Wei, Lei La, Lili Wang, Robert Batey, Yuhao Li, Chunxia Wang
ETHNOPHARMACOLOGICAL RELEVANCE: Paeoniflorin and liquiritin are major constituents in some Chinese herbal formulas, such as Yiru Tiaojing (YRTJ) Granule (a hospitalized preparation) and Peony-Glycyrrhiza Decoction, used for hyperprolactinemia-associated disorders. AIM OF THE STUDY: To investigate the effect of paeoniflorin and liquiritin on prolactin secretion. MATERIALS AND METHODS: The effect of YRTJ Granule on metoclopramide-induced hyperprolactinemia was tested in rats...
April 7, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28395208/increased-dopamine-receptor-expression-and-anti-depressant-response-following-deep-brain-stimulation-of-the-medial-forebrain-bundle
#18
Manoj P Dandekar, Dustin Luse, Carson Hoffmann, Patrick Cotton, Travis Peery, Christian Ruiz, Caroline Hussey, Vijayasree V Giridharan, Jair C Soares, Joao Quevedo, Albert J Fenoy
BACKGROUND: Among several potential neuroanatomical targets pursued for deep brain stimulation (DBS) for treating those with treatment-resistant depression (TRD), the superolateral-branch of the medial forebrain bundle (MFB) is emerging as a privileged location. We investigated the antidepressant-like phenotypic and chemical changes associated with reward-processing dopaminergic systems in rat brains after MFB-DBS. METHODS: Male Wistar rats were divided into three groups: sham-operated, DBS-Off, and DBS-On...
April 5, 2017: Journal of Affective Disorders
https://www.readbyqxmd.com/read/28393838/functional-polymorphisms-in-dopaminergic-genes-modulate-neurobehavioral-and-neurophysiological-consequences-of-sleep-deprivation
#19
Sebastian C Holst, Thomas Müller, Amandine Valomon, Britta Seebauer, Wolfgang Berger, Hans-Peter Landolt
Sleep deprivation impairs cognitive performance and reliably alters brain activation in wakefulness and sleep. Nevertheless, the molecular regulators of prolonged wakefulness remain poorly understood. Evidence from genetic, behavioral, pharmacologic and imaging studies suggest that dopaminergic signaling contributes to the behavioral and electroencephalographic (EEG) consequences of sleep loss, although direct human evidence thereof is missing. We tested whether dopamine neurotransmission regulate sustained attention and evolution of EEG power during prolonged wakefulness...
April 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28392487/variation-on-the-dopamine-d2-receptor-gene-drd2-is-associated-with-basal-ganglia-to-frontal-structural-connectivity
#20
Sebastian Markett, Marcel A de Reus, Martin Reuter, Christian Montag, Bernd Weber, Jan-Christoph Schoene-Bake, Martijn P van den Heuvel
Dopaminergic neurotransmission in the mesocortical system is crucial for higher order cognition. Common variation on the dopamine D2 receptor (DRD2) gene has been linked to individual differences in dopaminergic signaling and was also repeatedly associated to cognitive markers. The relationship between dopaminergic genetic variants and neurostructural properties of the mesocortical system, however, has received little attention so far. Recently, the direction of a dopaminergic manipulation was predicted from the integrity of fiber tracts between subcortical areas and the frontal lobes...
April 6, 2017: NeuroImage
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