keyword
MENU ▼
Read by QxMD icon Read
search

D2 receptor

keyword
https://www.readbyqxmd.com/read/28716664/advances-and-challenges-in-the-search-for-d2-and-d3-dopamine-receptor-selective-compounds
#1
REVIEW
Amy E Moritz, R Benjamin Free, David R Sibley
Compounds that target D2-like dopamine receptors (DRs) are currently used as therapeutics for several neuropsychiatric disorders including schizophrenia (antagonists) and Parkinson's disease (agonists). However, as the D2R and D3R subtypes are highly homologous, creating compounds with sufficient subtype-selectivity as well as drug-like properties for therapeutic use has proved challenging. This review summarizes the progress that has been made in developing D2R- or D3R-selective antagonists and agonists, and also describes the experimental conditions that need to be considered when determining the selectivity of a given compound, as apparent selectivity can vary widely depending on assay conditions...
July 14, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28716589/the-role-of-dopamine-d2-receptors-in-the-nucleus-accumbens-during-taste-aversive-learning-and-memory-extinction-after-long-term-sugar-consumption
#2
María Isabel Miranda, José Alejandro Rangel-Hernández, Gabriela Vera-Rivera, Nadia Edith García-Medina, Gerardo Soto-Alonso, Gabriela Rodríguez-García, Luis Núñez-Jaramillo
The nucleus accumbens (NAcc) is a forebrain region that may significantly contribute to the integration of taste and visceral signals during food consumption. Changes in dopamine release in the NAcc have been observed during consumption of a sweet taste and during compulsive consumption of dietary sugars, suggesting that NAcc dopaminergic transmission is strongly correlated with taste familiarity and the hedonic value content. NAcc core and shell nuclei are differentially involved during and after sugar exposure and, particularly, previous evidence suggests that dopamine D2 receptors could be related with the strength of the latent inhibition (LI) of conditioned taste aversion (CTA), which depends on the length of the taste stimulus pre-exposure...
July 14, 2017: Neuroscience
https://www.readbyqxmd.com/read/28710248/microrna-9-regulates-fetal-alcohol-induced-changes-in-d2-receptor-to-promote-prolactin-production
#3
Omkaram Gangisetty, Shaima Jabbar, Olivia Wynne, Dk K Sarkar
Fetal alcohol exposure (FAE) is known to increase prolactin (PRL) secretion from the pituitary lactotropes. In this study we determined whether microRNAs (miRs) are involved in FAE induced alteration in PRL release. We employed a rat animal model of FAE involving feeding pregnant Fisher 344 rats with a liquid diet containing 6.7% alcohol between gestational day 7 to 21 (AF). Both cyclic and estradiol implanted FAE females showed increased levels of plasma PRL and pituitary PRL mRNA but reduced levels of pituitary dopamine D2 receptor (D2R) and its short spliced form (D2S)...
July 14, 2017: Journal of Endocrinology
https://www.readbyqxmd.com/read/28708709/genetics-influence-neurocognitive-performance-at-baseline-but-not-concussion-history-in-collegiate-student-athletes
#4
Graham D Cochrane, Mark H Sundman, Eric E Hall, Matthew C Kostek, Kirtida Patel, Kenneth P Barnes, Caroline J Ketcham
OBJECTIVE: This study investigates 4 single-nucleotide polymorphisms [Apolipoprotein E (APOE), APOE promoter, catechol-O-methyl transferase (COMT), and dopamine D2 receptor] that have been implicated in concussion susceptibility and/or cognitive ability in collegiate student-athletes. DESIGN: Cross-sectional study. SETTING: Neuroscience laboratory at Elon University. PARTICIPANTS: Two hundred fifty division I collegiate student-athletes (66 women, 184 men) from various sports...
July 11, 2017: Clinical Journal of Sport Medicine: Official Journal of the Canadian Academy of Sport Medicine
https://www.readbyqxmd.com/read/28708260/effect-of-optogenetic-manipulation-of-accumbal-medium-spiny-neurons-expressing-dopamine-d2-receptors-in-cocaine-induced-behavioral-sensitization
#5
Byeong Jun Kang, Shelly Sooyun Song, Lei Wen, Ki-Pyo Hong, George J Augustine, Ja-Hyun Baik
Repetitive exposure to addictive drugs causes synaptic modification in the mesocorticolimbic dopamine (DA) system. Dopamine D1 receptors (D1R) or D2 receptors (D2R) expressed in the medium spiny neurons (MSNs) of the nucleus accumbens (NAc) play critical roles in the control of addictive behaviors. Optogenetic activation of D2R-expressing MSNs (D2R-MSNs) in the NAc previously demonstrated that these neurons play a key role in withdrawal-induced plasticity. Here, we examined the effect of optogenetic inhibition of D2R-MSNs in the NAc on cocaine-induced behavioral sensitization...
July 14, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/28704278/trace-amine-associated-receptor-1-agonists-ro5263397-and-ro5166017-attenuate-quinpirole-induced-yawning-but-not-hypothermia-in-rats
#6
Justin N Siemian, Yanan Zhang, Jun-Xu Li
Increasing evidence suggests that trace amine-associated receptor 1 (TAAR1) is an important modulator of the dopaminergic system. Existing molecular evidence indicates that TAAR1 regulates dopamine levels through interactions with dopamine transporters and D2 receptors. However, investigations to date have not been exhaustive and other pathways may be involved. In this study, we used a well-described set of behaviors, quinpirole-induced yawning and hypothermia, to explore the potential interaction of TAAR1 and D3 receptors, which are members of the 'D2-like' dopamine receptor subfamily...
July 12, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28704276/effects-of-d1-and-d2-receptor-antagonists-on-the-discriminative-stimulus-effects-of-methylendioxypyrovalerone-and-mephedrone-in-male-sprague-dawley-rats-trained-to-discriminate-d-amphetamine
#7
Eric L Harvey, Rachel L Burroughs, Lisa E Baker
Psychopharmacology research has amassed substantial evidence for similarities between synthetic cathinones and other commonly abused psychostimulants. Few studies have utilized drug discrimination methods to investigate synthetic cathinones, and the precise neurochemical substrates underlying their interoceptive effects have not been examined. The present study assessed the involvement of D1 and D2 dopaminergic receptors in the stimulus effects of 3,4-methylenedioxypyrovalerone (MDPV) and mephedrone (MEPH) in rats trained to discriminate D-amphetamine...
July 12, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28700819/posterior-dopamine-d2-3-receptors-and-brain-network-functional-connectivity
#8
Atsuko Nagano-Saito, Jennifer I Lissemore, Paul Gravel, Marco Leyton, Felix Carbonell, Chawki Benkelfat
Recent studies suggest that dopaminergic tone influences resting state activity in multiple brain networks. Although dopamine receptors and transporters have been identified in the posteromedial and parietal cortices, which are linked to functional networks such as the default mode network (DMN), the relationship between dopamine receptor distribution in these posterior regions and resting-state connectivity has yet to be explored. Here, we used a multi-modal neuroimaging strategy, combining resting-state functional magnetic resonance imaging (rsfMRI) and [18F]-fallypride high-resolution positron emission tomography (PET), to examine the association between within-network functional connectivity and the dopamine D2/3 receptor distribution in the posterior portion of the brain in 13 healthy adults...
July 12, 2017: Synapse
https://www.readbyqxmd.com/read/28700108/gpr88-in-a2a-receptor-expressing-neurons-modulates-locomotor-response-to-dopamine-agonists-but-not-sensorimotor-gating
#9
A C Meirsman, A de Kerchove d'Exaerde, B L Kieffer, A M Ouagazzal
The orphan receptor, GPR88, is emerging as a key player in the pathophysiology of several neuropsychiatric diseases, including psychotic disorders. Knockout (KO) mice lacking GPR88 throughout the brain exhibit many abnormalities relevant to schizophrenia including locomotor hyperactivity, behavioral hypersensitivity to dopaminergic psychostimulants and deficient sensorimotor gating. Here, we used conditional knockout (cKO) mice lacking GPR88 selectively in striatal medium spiny neurons expressing A2A receptor to determine neuronal circuits underlying these phenotypes...
July 12, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/28695985/intrastriatal-administration-of-botulinum-neurotoxin-a-normalizes-striatal-d2-r-binding-and-reduces-striatal-d1-r-binding-in-male-hemiparkinsonian-rats
#10
Franziska Wedekind, Angela Oskamp, Markus Lang, Alexander Hawlitschka, Karl Zilles, Andreas Wree, Andreas Bauer
Cerebral administration of botulinum neurotoxin A (BoNT-A) has been shown to improve disease-specific motor behavior in a rat model of Parkinson disease (PD). Since the dopaminergic system of the basal ganglia fundamentally contributes to motor function, we investigated the impact of BoNT-A on striatal dopamine receptor expression using in vitro and in vivo imaging techniques (positron emission tomography and quantitative autoradiography, respectively). Seventeen male Wistar rats were unilaterally lesioned with 6-hydroxydopamine (6-OHDA) and assigned to two treatment groups 7 weeks later: 10 rats were treated ipsilaterally with an intrastriatal injection of 1 ng BoNT-A, while the others received vehicle (n = 7)...
July 11, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28692863/identification-of-genetic-correlates-of-response-to-risperidone-findings-of-a-multicentric-schizophrenia-study-from-india
#11
Gurjit Kaur, Deepti Gupta, Bir Singh Chavan, Vikas Sinhmar, Rajendra Prasad, Adarsh Tripathi, P D Garg, Rajiv Gupta, Hitesh Khurana, Shiv Gautam, Mushtaq Ahmed Margoob, Jitender Aneja
Risperidone is most commonly used as an antipsychotic in India for treatment of schizophrenia. However, the response to treatment with risperidone is affected by many factors, genetic factors being one of them. So, we attempted to evaluate the association between dopamine D2 (DRD2) receptor, serotonergic (5HT2A) receptor and CYP2D6 gene polymorphisms and response to treatment with risperidone in persons with schizophrenia from North India. It was a multicentric 12-weeks prospective study, undertaken in patients diagnosed with schizophrenia according to International Classification of Diseases 10th revision, Diagnostic Criteria for Research module (ICD-10 DCR)...
July 6, 2017: Asian Journal of Psychiatry
https://www.readbyqxmd.com/read/28692485/safety-and-tolerability-of-cariprazine-in-patients-with-acute-exacerbation-of-schizophrenia-a-pooled-analysis-of-four-phase-ii-iii-randomized-double-blind-placebo-controlled-studies
#12
Willie Earley, Suresh Durgam, Kaifeng Lu, István Laszlovszky, Marc Debelle, John M Kane
Cariprazine, a potent dopamine D3 and D2 receptor partial agonist antipsychotic with preferential binding to D3 receptors, is Food and Drug Administration approved for treating schizophrenia and manic or mixed episodes of bipolar I disorder. A post-hoc safety/tolerability analysis of data from the four acute trials in the cariprazine schizophrenia clinical development program (NCT00404573; NCT00694707; NCT01104766; NCT01104779) was carried out using the overall safety population (all patients who received ≥1 dose of study drug) and modal daily dose subgroups (1...
July 7, 2017: International Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28692418/contribution-of-genetic-polymorphisms-and-haplotypes-in-drd2-bdnf-and-opioid-receptors-to-heroin-dependence-and-endophenotypes-among-the-han-chinese
#13
Xuan Gao, Youxin Wang, Minglin Lang, Li Yuan, Albert Stuart Reece, Wei Wang
Heroin and drug dependence are major contributors to global health burden worldwide, but their underlying mechanisms remain elusive and may vary from population to population. Reward- and memory-related candidate genes dopamine D2 receptor (DRD2) and brain-derived neurotrophic factor (BDNF), as well as the opioid receptor genes (OPRM1, OPRD1, and OPRK1), have been implicated in drug dependence, but relatively little is known on their contributions to heroin dependence in populations worldwide. Hence, we evaluated the contributions of the above five candidate genes in heroin dependence and several important related endophenotypes (the onset age of heroin use and subjective response to first heroin use), at single single-nucleotide polymorphism as well as haplotype levels, in a Han Chinese population sample...
July 2017: Omics: a Journal of Integrative Biology
https://www.readbyqxmd.com/read/28691798/structure-and-affinity-of-two-bicyclic-glutamate-analogues-at-ampa-and-kainate-receptors
#14
Stine Møllerud, Andrea Pinto, Laura Marconi, Karla Frydenvang, Thor S Thorsen, Saara K Laulumaa, Raminta Venskutonyte, Sebastian Winther, Ana M C Moral, Lucia Tamborini, Paola Conti, Darryl S Pickering, Jette Sandholm Kastrup
Ionotropic glutamate receptors (iGluRs) are involved in most of the fast excitatory synaptic transmission in the central nervous system. These receptors are important for learning and memory formation, but are also involved in the development of diseases such as Alzheimer's disease, epilepsy and depression. In order to understand the function of different types of iGluRs, selective agonists are invaluable as pharmacological tool compounds. Here, we report binding affinities of two bicyclic, conformationally restricted analogues of glutamate (CIP-AS and LM-12b) at AMPA (GluA2 and GluA3) and kainate receptor subunits (GluK1-3 and GluK5)...
July 10, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28687316/levodopa-l-dopa-attenuates-endoplasmic-reticulum-stress-response-and-cell-death-signaling-through-drd2-in-sh-sy5y-neuronal-cells-under-%C3%AE-synuclein-induced-toxicity
#15
Juhyun Song, Byeong C Kim, Dai-Trang T Nguyen, Manikandan Samidurai, Seong-Min Choi
Parkinson's disease (PD) is characterized by the formation of Lewy bodies (LBs) in dopaminergic neurons. α-Synuclein (α-syn), a major protein component of LBs, is known to regulate synaptic plasticity, with a crucial role in memory and motor function in the central nervous system. Levodopa (L-3,4-dihydroxyphenylalanine; also known as L-DOPA) is considered the most effective medication for controlling the symptoms of PD. However, it is unclear whether L-DOPA improves the neuropathology of PD. In the present study, we investigated the effect of L-DOPA on SH-SY5Y neuronal cells under α-syn-induced toxicity...
July 4, 2017: Neuroscience
https://www.readbyqxmd.com/read/28687229/the-phosphodiesterase-10a-selective-inhibitor-tak-063-induces-c-fos-expression-in-both-direct-and-indirect-pathway-medium-spiny-neurons-and-sub-regions-of-the-medial-prefrontal-cortex-in-rats
#16
Atsushi Nakatani, Sayuri Nakamura, Haruhide Kimura
TAK-063, a selective phosphodiesterase 10A (PDE10A) inhibitor, produces potent antipsychotic-like and pro-cognitive effects in rodents via balanced activation of striatal direct and indirect pathway medium spiny neurons (MSNs). Brain activity modulation by TAK-063 has been characterized using pharmacological magnetic resonance imaging and electroencephalography in animals, revealing modulation of activity in the prefrontal cortex (PFC) where there is little or no PDE10A expression. To understand the specific brain regions and cells affected by TAK-063 in rats, we assessed neural activation in the striatal complex and PFC using immunofluorescence staining to measure c-Fos expression...
July 4, 2017: Neuroscience Research
https://www.readbyqxmd.com/read/28685972/kir2ds5-allotypes-that-recognize-the-c2-epitope-of-hla-c-are-common-among-africans-and-absent-from-europeans
#17
Jeroen H Blokhuis, Hugo G Hilton, Lisbeth A Guethlein, Paul J Norman, Neda Nemat-Gorgani, Annettee Nakimuli, Olympe Chazara, Ashley Moffett, Peter Parham
INTRODUCTION: KIR2DS5 is an activating human NK cell receptor of lineage III KIR. These include both inhibitory KIR2DL1, 2 and 3 and activating KIR2DS1 that recognize either the C1 or C2 epitope of HLA-C. In Europeans KIR2DS5 is essentially monomorphic, with KIR2DS5*002 being predominant. Pioneering investigations showed that KIR2DS5*002 has activating potential, but cannot recognize HLA-A, -B, or -C. Subsequent studies have shown that KIR2DS5 is highly polymorphic in Africans, and that KIR2DS5*006 protects pregnant Ugandan women from preeclampsia...
July 6, 2017: Immunity, Inflammation and Disease
https://www.readbyqxmd.com/read/28684424/il-4-upregulates-cyclooxygenase-1-expression-in-macrophages
#18
Ashley E Shay, Bastihalli T Diwakar, Bo-Jhih Guan, Vivek Narayan, Joseph F Urban, K Sandeep Prabhu
Macrophages use various cell-surface receptors to sense their environment and undergo polarized responses. The cytokines IL-4 and IL-13, released from T-helper type 2 (Th2) cells, drive macrophage polarization toward an alternatively activated phenotype (M2). This phenotype is associated with the expression of potent pro-resolving mediators, such as the prostaglandin (PG) D2-derived cyclopentenone metabolite, 15d-PGJ2, produced by the cyclooxygenase (Ptgs; Cox) pathway. Interestingly, IL-4 treatment of bone marrow-derived macrophages significantly downregulates Cox-2 protein expression, while Cox-1 levels are significantly increased...
July 6, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28676746/regulation-of-fear-extinction-in-the-basolateral-amygdala-by-dopamine-d2-receptors-accompanied-by-altered-glur1-glur1-ser845-and-nr2b-levels
#19
Yan-Wei Shi, Bu-Fang Fan, Li Xue, Jia-Ling Wen, Hu Zhao
The amygdala, a critical structure for both Pavlovian fear conditioning and fear extinction, receives sparse but comprehensive dopamine innervation and contains dopamine D1 and D2 receptors. Fear extinction, which involves learning to suppress the expression of a previously learned fear, appears to require the dopaminergic system. The specific roles of D2 receptors in mediating associative learning underlying fear extinction require further study. Intra-basolateral amygdala (BLA) infusions of a D2 receptor agonist, quinpirole, and a D2 receptor antagonist, sulpiride, prior to fear extinction and extinction retention were tested 24 h after fear extinction training for long-term memory (LTM)...
2017: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/28674764/a-pilot-study-of-cabergoline-for-the-treatment-of-metastatic-breast-cancer
#20
Ricardo Costa, C A Santa-Maria, D M Scholtens, S Jain, L Flaum, W J Gradishar, C V Clevenger, V G Kaklamani
PURPOSE: The prolactin (PRL) receptor is over-expressed in breast cancer, and pre-clinical data indicate that it contributes to breast oncogenesis. Cabergoline is a potent dopamine receptor agonist of D2 receptors and has a direct inhibitory effect on pituitary PRL secretion. METHODS: A phase II study of cabergoline in patients with metastatic breast cancer was conducted. The primary end point of the study was to determine the clinical benefit rate (CBR) at 2 months...
July 3, 2017: Breast Cancer Research and Treatment
keyword
keyword
81541
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"