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Dopamine D2

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https://www.readbyqxmd.com/read/28223337/functional-expression-of-dopamine-d2-receptor-is-regulated-by-tetraspanin-7-mediated-postendocytic-trafficking
#1
Seol-Ae Lee, Yeongjun Suh, Saebom Lee, Jaehoon Jeong, Soo Jeong Kim, So Jung Kim, Sang Ki Park
The dopaminergic system plays an essential role in various functions of the brain, including locomotion, memory, and reward, and the deregulation of dopaminergic signaling as a result of altered functionality of dopamine D2 receptor (DRD2) is implicated in multiple neurologic and psychiatric disorders. Tetraspanin-7 (TSPAN7) is expressed to variable degrees in different tissues, with the highest level in the brain, and multiple mutations in TSPAN7 have been implicated in intellectual disability. Here, we tested the hypothesis that TSPAN7 may be a binding partner of DRD2 that is involved in the regulation of its functional activity...
February 21, 2017: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/28218041/guibourtia-tessmannii-induced-fictive-ejaculation-in-spinal-male-rat-involvement-of-d1-d2-like-receptors
#2
Patrick Brice Deeh Defo, Elvis Asongu, Modeste Nya Wankeu, Esther Ngadjui, Georges Romeo Bonsou Fazin, François Xavier Kemka, Miguel Carro-Juarez, Albert Kamanyi, Pierre Kamtchouing, Pierre Watcho
CONTEXT: Guibourtia tessmannii (Caesalpiniaceae) is a plant traditionally used as aphrodisiac. We previously reported the pro-ejaculatory effects of the aqueous and methanol extracts of G. tesmannii in spinal male rat. However, the mechanism underlying such effects has not been elucidated. OBJECTIVE: This study characterizes the dopaminergic sub-type receptors involved in G. tesmannii-induced ejaculation in male Wistar rat. MATERIALS AND METHODS: Urethane-anesthetized spinal male rats were intravenously treated with saline solution (1 mL/kg, control); dopamine (0...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28216334/crocins-the-active-constituents-of-crocus-sativus-l-counteracted-apomorphine-induced-performance-deficits-in-the-novel-object-recognition-task-but-not-novel-object-location-task-in-rats
#3
Nikolaos Pitsikas, Petros A Tarantilis
Schizophrenia is a chronic mental disease that affects nearly 1% of the population worldwide. Several lines of evidence suggest that the dopaminergic (DAergic) system might be compromised in schizophrenia. Specifically, the mixed dopamine (DA) D1/D2 receptor agonist apomorphine induces schizophrenia-like symptoms in rodents, including disruption of memory abilities. Crocins are among the active components of saffron (dried stigmas of Crocus sativus L. plant) and their implication in cognition is well documented...
February 16, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28216123/ablation-of-the-auditory-cortex-results-in-changes-in-the-expression-of-neurotransmission-related-mrnas-in-the-cochlea
#4
Verónica Lamas, José M Juiz, Miguel A Merchán
The auditory cortex (AC) dynamically regulates responses of the Organ of Corti to sound through descending connections to both the medial (MOC) and lateral (LOC) olivocochlear efferent systems. We have recently provided evidence that AC has a reinforcement role in the responses to sound of the auditory brainstem nuclei. In a molecular level, we have shown that descending inputs from AC are needed to regulate the expression of molecules involved in outer hair cell (OHC) electromotility control, such as prestin and the α10 nicotinic acetylcholine receptor (nAchR)...
February 16, 2017: Hearing Research
https://www.readbyqxmd.com/read/28214075/asymmetric-total-synthesis-of-tetrahydroprotoberberine-derivatives-and-evaluation-of-their-binding-affinities-at-dopamine-receptors
#5
David Y W Lee, Jing Liu, Shuzhen Zhang, Peng Huang, Lee-Yuan Liu-Chen
Cocaine addiction remains a serious challenge for clinical and medical research because there is no effective pharmacological treatment. l-THP, a natural product isolated from Corydalis yanhusuo W.T. Wang, is one of the most frequently used traditional herbs to treat drug addiction in China. Our laboratory first reported that its demethylated metabolites l-ICP, l-CD, and l-CP had high affinity at dopamine D1, D2, and D5 receptors. Here we report the chemical synthesis of these metabolites and other derivatives and their binding affinities at dopamine receptors...
January 31, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28212944/acute-and-long-term-effects-of-adolescent-methylphenidate-on-decision-making-and-dopamine-receptor-mrna-expression-in-the-orbitofrontal-cortex
#6
Leslie R Amodeo, Eliza Jacobs-Brichford, Matthew S McMurray, Jamie D Roitman
Though commonly used as a treatment for ADHD, the psychostimulant methylphenidate (MPH) is also misused and abused in adolescence in both clinical and general populations. Although MPH acts via pathways activated by other drugs of abuse, the short- and long-term effects of MPH on reward processing in learning and decision-making are not clearly understood. We examined the effect of adolescent MPH treatment on a battery of reward-directed behaviors both in adolescence during its administration and in adulthood after its discontinuation...
February 14, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28212943/effects-of-acute-dopaminergic-and-serotonergic-manipulations-in-the-aci-paradigm-depend-on-the-basal-valence-of-cognitive-judgement-bias-in-rats
#7
Joanna Golebiowska, Rafal Rygula
Recent findings have revealed that pharmacological enhancement of dopaminergic (DA) function by the administration of a DA precursor (dihydroxy-L-phenylalanine; L-DOPA), but not the selective serotonin reuptake inhibitor (SSRI) citalopram, increases an optimism bias in humans. To test whether dopamine might play a similar role in non-human animals, in the present study, we evaluated the effects of acute injections of L-DOPA, the D2 receptor antagonist haloperidol, and the SSRI escitalopram on cognitive judgement bias of rats in the ambiguous-cue interpretation (ACI) paradigm...
February 14, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28203201/modulation-of-synaptic-plasticity-in-the-cortex-needs-to-understand-all-the-players
#8
REVIEW
Claire N J Meunier, Pascal Chameau, Philippe M Fossier
The prefrontal cortex (PFC) is involved in cognitive tasks such as working memory, decision making, risk assessment and regulation of attention. These functions performed by the PFC are supposed to rely on rhythmic electrical activity generated by neuronal network oscillations determined by a precise balance between excitation and inhibition balance (E/I balance) resulting from the coordinated activities of recurrent excitation and feedback and feedforward inhibition. Functional alterations in PFC functions have been associated with cognitive deficits in several pathologies such as major depression, anxiety and schizophrenia...
2017: Frontiers in Synaptic Neuroscience
https://www.readbyqxmd.com/read/28193454/new-developments-in-brain-research-of-internet-and-gaming-disorder
#9
REVIEW
Aviv Weinstein, Abigail Livny, Abraham Weizman
There is evidence that the neural mechanisms underlying Internet Gaming Disorder (IGD) resemble those of drug addiction. Functional Magnetic Resonance Imaging (fMRI) studies of the resting state and measures of gray matter volume have shown that Internet game playing was associated with changes to brain regions responsible for attention and control, impulse control, motor function, emotional regulation, sensory-motor coordination. Furthermore, Internet game playing was associated with lower white matter density in brain regions that are involved in decision-making, behavioral inhibition and emotional regulation...
February 11, 2017: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/28192174/does-genetic-bdnf-deficiency-in-rats-interact-with-neurotransmitter-control-of-prepulse-inhibition-implications-for-schizophrenia
#10
Maarten van den Buuse, Davina Biel, Kathrin Radscheit
Several studies have suggested a role of BDNF in the development of schizophrenia. For example, post-mortem studies have shown significantly reduced levels of BDNF protein expression in the brain of schizophrenia patients. We investigated the relationship between reduced levels of BDNF in the brain and the regulation of prepulse inhibition (PPI), a behavioral endophenotype of schizophrenia. We used BDNF heterozygous mutant rats which display a 50% decrease of mature BDNF protein levels. Previously, we observed normal baseline PPI and responses to the dopamine D1/D2 receptor agonist, apomorphine, in these rats...
February 10, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28190661/the-novel-antipsychotic-drug-brexpiprazole-alone-and-in-combination-with-escitalopram-facilitates-prefrontal-glutamatergic-transmission-via-a-dopamine-d1-receptor-dependent-mechanism
#11
Carl Björkholm, Monica M Marcus, Åsa Konradsson-Geuken, Kent Jardemark, Torgny H Svensson
Brexpiprazole (Rexulti(®)), a novel D2/3 receptor (R) partial agonist, was recently approved as monotherapy for schizophrenia, demonstrating effectiveness against both positive and negative symptoms, and also approved as add-on treatment to antidepressant drugs, inducing a potent antidepressant effect with a faster onset compared to an antidepressant given alone. Moreover, brexpiprazole has demonstrated pro-cognitive effects in preclinical studies. To explore whether the observed effects may be mediated via modulation of prefrontal glutamatergic transmission, we investigated the effect of brexpiprazole, alone and in combination with the SSRI escitalopram, on prefrontal glutamatergic transmission using in vitro electrophysiological intracellular recordings of deep layer pyramidal cells of the rat medial prefrontal cortex (mPFC)...
February 9, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28188355/repeated-mdma-administration-increases-mdma-produced-locomotor-activity-and-facilitates-the-acquisition-of-mdma-self-administration-role-of-dopamine-d2-receptor-mechanisms
#12
Ross van de Wetering, Susan Schenk
RATIONALE: Repeated exposure to ±3, 4-methylenedioxymethamphetamine (MDMA) produces sensitization to MDMA-produced hyperactivity, but the mechanisms underlying the development of this sensitized response or the relationship to the reinforcing effects of MDMA is unknown. OBJECTIVES: This study determined the effect of a sensitizing regimen of MDMA exposure on the acquisition of MDMA self-administration and investigated the role of dopamine D2 receptor mechanisms...
February 10, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28187335/insight-into-illness-and-its-relationship-to-illness-severity-cognition-and-estimated-antipsychotic-dopamine-receptor-occupancy-in-schizophrenia-an-antipsychotic-dose-reduction-study
#13
Philip Gerretsen, Hiroyoshi Takeuchi, Miracle Ozzoude, Ariel Graff-Guerrero, Hiroyuki Uchida
Little is known about the influence of D2 receptor occupancy on impaired insight into illness (III)-a core feature of schizophrenia. III is associated with illness severity and cognitive dysfunction. Comparably, supratherapeutic D2 receptor occupancy can impair cognition. However, it is unclear how illness severity, cognition, and D2 receptor occupancy interact to influence III in schizophrenia. The aim of this study was to explore the influence of antipsychotic dose reduction on the relationships of illness severity and cognition to III...
February 1, 2017: Psychiatry Research
https://www.readbyqxmd.com/read/28187160/the-effects-of-dopamine-receptor-1-and-2-agonists-and-antagonists-on-sexual-and-aggressive-behaviors-in-male-green-anoles
#14
Alexandra N Smith, David Kabelik
The propensity to exhibit social behaviors during interactions with same-sex and opposite-sex conspecifics is modulated by various neurotransmitters, including dopamine. Dopamine is a conserved neurotransmitter among vertebrates and dopaminergic receptors are also highly conserved among taxa. Activation of D1 and D2 dopamine receptor subtypes has been shown to modulate social behaviors, especially in mammalian and avian studies. However, the specific behavioral functions of these receptors vary across taxa...
2017: PloS One
https://www.readbyqxmd.com/read/28186762/synthesis-and-pharmacological-characterization-of-novel-trans-cyclopropylmethyl-linked-bivalent-ligands-that-exhibit-selectivity-and-allosteric-pharmacology-at-the-dopamine-d3-receptor-d3r
#15
Vivek Kumar, Amy E Moritz, Thomas M Keck, Alessandro Bonifazi, Michael P Ellenberger, Christopher D Sibley, R Benjamin Free, Lei Shi, J Robert Lane, David R Sibley, Amy Hauck Newman
The development of bitopic ligands directed toward D2-like receptors has proven to be of particular interest to improve the selectivity and/or affinity of these ligands and as an approach to modulate and bias their efficacies. The structural similarities between dopamine D3 receptor (D3R)-selective molecules that display bitopic or allosteric pharmacology and those that are simply competitive antagonists are subtle and intriguing. Herein we synthesized a series of molecules in which the primary and secondary pharmacophores were derived from the D3R-selective antagonists SB269,652 (1) and SB277011A (2) whose structural similarity and pharmacological disparity provided the perfect templates for SAR investigation...
February 10, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28186680/the-group-ii-metabotropic-glutamate-receptor-agonist-ly354740-and-the-d2-receptor-antagonist-haloperidol-reduce-locomotor-hyperactivity-but-fail-to-rescue-spatial-working-memory-in-glua1-knockout-mice
#16
Thomas Boerner, Alexei Bygrave, Jingkai Chen, Anushka Fernando, Stephanie Jackson, Chris Barkus, Rolf Sprengel, Peter H Seeburg, Paul J Harrison, Gary Gilmour, David M Bannerman, David J Sanderson
Group II metabotropic glutamate receptor agonists have been suggested as potential anti-psychotics, at least in part, based on the observation that the agonist LY354740 appeared to rescue the cognitive deficits caused by non-competitive N-methyl-D-aspartate receptor (NMDAR) antagonists, including spatial working memory deficits in rodents. Here, we tested the ability of LY354740 to rescue spatial working memory performance in mice that lack the GluA1 subunit of the AMPA glutamate receptor, encoded by Gria1, a gene recently implicated in schizophrenia by genome-wide association studies...
February 10, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/28182408/design-synthesis-structure-activity-relationship-studies-and-three-dimensional-quantitative-structure-activity-relationship-3d-qsar-modeling-of-a-series-of-o-biphenyl-carbamates-as-dual-modulators-of-dopamine-d3-receptor-and-fatty-acid-amide-hydrolase
#17
Alessio De Simone, Debora Russo, Gian Filippo Ruda, Alessandra Micoli, Mariarosaria Ferraro, Rita Maria Concetta Di Martino, Giuliana Ottonello, Maria Summa, Andrea Armirotti, Tiziano Bandiera, Andrea Cavalli, Giovanni Bottegoni
We recently reported molecules designed according to the multi-target-directed ligand paradigm to exert combined activity at human fatty acid amide hydrolase (FAAH) and dopamine receptor subtype D3 (D3R). Both targets are relevant for tackling several types of addiction (most notably nicotine addiction) and other compulsive behaviors. Here, we report an SAR exploration of a series of biphenyl-N-[4-[4-(2,3-substituted-phenyl)piperazine-1-yl]alkyl]carbamates, a novel class of molecules that had shown promising activities at the FAAH - D3R target combination in preliminary studies...
February 9, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28181484/bim-23a760-influences-key-functional-endpoints-in-pituitary-adenomas-and-normal-pituitaries-molecular-mechanisms-underlying-the-differential-response-in-adenomas
#18
Alejandro Ibáñez-Costa, Laura M López-Sánchez, Manuel D Gahete, Esther Rivero-Cortés, Mari C Vázquez-Borrego, María A Gálvez, Andrés de la Riva, Eva Venegas-Moreno, Luis Jiménez-Reina, Alberto Moreno-Carazo, Francisco J Tinahones, Silvia Maraver-Selfa, Miguel A Japón, Juan A García-Arnés, Alfonso Soto-Moreno, Susan M Webb, Rhonda D Kineman, Michael D Culler, Justo P Castaño, Raúl M Luque
Chimeric somatostatin/dopamine compounds such as BIM-23A760, an sst2/sst5/D2 receptors-agonist, have emerged as promising new approaches to treat pituitary adenomas. However, information on direct in vitro effects of BIM-23A760 in normal and tumoral pituitaries remains incomplete. The objective of this study was to analyze BIM-23A760 effects on functional parameters (Ca(2+) signaling, hormone expression/secretion, cell viability and apoptosis) in pituitary adenomas (n = 74), and to compare with the responses of normal primate and human pituitaries (n = 3-5)...
February 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28180960/dissociable-effects-of-the-d-and-l-enantiomers-of-govadine-on-the-disruption-of-prepulse-inhibition-by-mk-801-and-apomorphine-in-male-long-evans-rats
#19
Brittney R Lins, Wendie N Marks, Anthony G Phillips, John G Howland
RATIONALE: The search for novel antipsychotic drugs to treat schizophrenia is driven by the poor treatment efficacy, serious side effects, and poor patient compliance of current medications. Recently, a class of compounds known as tetrahydroprotoberberines, which includes the compound d,l-govadine, have shown promise in preclinical rodent tests relevant to schizophrenia. To date, the effect of govadine on prepulse inhibition (PPI), a test for sensorimotor gating commonly used to assess the effects of putative treatments for schizophrenia, has not been determined...
February 8, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28179504/your-genes-are-conspiring-against-you
#20
Olga Peñagarikano
Gene variants in the dopamine receptor D2 expression network predict physiological and clinical features as well as treatment responses in schizophrenia.
February 8, 2017: Science Translational Medicine
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