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Dopamine receptor 2

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https://www.readbyqxmd.com/read/28319392/scaffold-repurposing-of-nucleosides-adenosine-receptor-agonists-enhanced-activity-at-the-human-dopamine-and-norepinephrine-sodium-symporters
#1
Dilip K Tosh, Aaron Janowsky, Amy J Eshleman, Eugene Warnick, Zhan-Guo Gao, Zhoumou Chen, Elizabeth Gizewski, John A Auchampach, Daniela Salvemini, Kenneth A Jacobson
We have repurposed (N)-methanocarba adenosine derivatives (A3 adenosine receptor (AR) agonists) to enhance radioligand binding allosterically at the human dopamine (DA) transporter (DAT) and inhibit DA uptake. We extended the structure-activity relationship of this series with small N(6)-alkyl substitution, 5'-esters, deaza modifications of adenine, and ribose restored in place of methanocarba. C2-(5-Halothien-2-yl)-ethynyl 5'-methyl 9 (MRS7292) and 5'-ethyl 10 (MRS7232) esters enhanced binding at DAT (EC50 ∼ 35 nM) and at the norepinephrine transporter (NET)...
March 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28316027/validation-of-dopamine-receptor-drd1-and-drd2-antibodies-using-receptor-deficient-mice
#2
Tamara Stojanovic, Michaela Orlova, Fernando J Sialana, Harald Höger, Stanislav Stuchlik, Ivan Milenkovic, Jana Aradska, Gert Lubec
Dopamine receptors 1 and 2 (DRD1, DRD2) are essential for signaling in the brain for a multitude of brain functions. Previous work using several antibodies against these receptors is abundant but only the minority of antibodies used have been validated and, therefore, the results of these studies remain uncertain. Herein, antibodies against DRD1 (Merck Millipore AB1765P, Santa Cruz Biotechnology sc-14001, Sigma Aldrich D2944, Alomone Labs ADR-001) and DRD2 (Abcam ab21218, Merck Millipore AB5084P, Santa Cruz Biotechnology sc-5303) have been tested using western blotting and immunohistochemistry on mouse striatum (wild type and corresponding knock-out mice) and when specific, they were further evaluated on rat and human striatum...
March 18, 2017: Amino Acids
https://www.readbyqxmd.com/read/28314679/an-analysis-of-the-rewarding-and-aversive-associative-properties-of-nicotine-in-the-neonatal-quinpirole-model-effects-on-glial-cell-line-derived-neurotrophic-factor-gdnf
#3
Russell W Brown, Seth L Kirby, Adam R Denton, John M Dose, Elizabeth D Cummins, Wesley Drew Gill, Katherine C Burgess
This study analyzed the associative properties of nicotine in a conditioned place preference (CPP) paradigm in adolescent rats neonatally treated with quinpirole (NQ) or saline (NS). NQ produces dopamine D2 receptor supersensitivity that persists throughout the animal's lifetime, and therefore has relevance towards schizophrenia. In two experiments, rats were ip administered quinpirole (1mg/kg) or saline from postnatal day (P)1-21. After an initial preference test at P42-43, animals were conditioned for eight consecutive days with saline or nicotine (0...
March 14, 2017: Schizophrenia Research
https://www.readbyqxmd.com/read/28306571/cns-syndromes-associated-with-antibodies-against-metabotropic-receptors
#4
Eric Lancaster
PURPOSE OF REVIEW: Autoantibodies to Central nervous system (CNS) metabotropic receptors are associated with a growing family of autoimmune brain diseases, including encephalitis, basal ganglia encephalitis, Ophelia syndrome, and cerebellitis. The purpose of this review is to summarize the state of knowledge regarding the target receptors, the neurological autoimmune disorders, and the pathogenic mechanisms. RECENT FINDINGS: Antibodies to the γ-aminobutyric acid B receptor are associate with limbic encephalitis and severe seizures, often with small cell lung cancers...
March 16, 2017: Current Opinion in Neurology
https://www.readbyqxmd.com/read/28302436/pharmacological-characterization-of-dopamine-receptors-in-the-rice-striped-stem-borer-chilo-suppressalis
#5
Gang Xu, Shun-Fan Wu, Gui-Xiang Gu, Zi-Wen Teng, Gong-Yin Ye, Jia Huang
Dopamine is an important neurotransmitter and neuromodulator in both vertebrates and invertebrates and is the most abundant monoamine present in the central nervous system of insects. A complement of functionally distinct dopamine receptors mediate the signal transduction of dopamine by modifying intracellular Ca(2+) and cAMP levels. In the present study, we pharmacologically characterized three types of dopamine receptors, CsDOP1, CsDOP2 and CsDOP3, from the rice striped stem borer, Chilo suppressalis. All three receptors show considerable sequence identity with orthologous dopamine receptors...
March 13, 2017: Insect Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28290500/pramipexole-restores-depressed-transmission-in-the-ventral-hippocampus-following-mptp-lesion
#6
Javier Castro-Hernández, Paul A Adlard, David I Finkelstein
The hippocampus has a significant association with memory, cognition and emotions. The dopaminergic projections from both the ventral tegmental area and substantia nigra are thought to be involved in hippocampal activity. To date, however, few studies have investigated dopaminergic innervation in the hippocampus or the functional consequences of reduced dopamine in disease models. Further complicating this, the hippocampus exhibits anatomical and functional differentiation along its dorso-ventral axis. In this work we investigated the role of dopamine on hippocampal long term potentiation using D-amphetamine, which stimulates dopamine release, and also examined how a dopaminergic lesion affects the synaptic transmission across the anatomic subdivisions of the hippocampus...
March 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28289242/acupuncture-attenuated-vascular-dementia-induced-hippocampal-long-term-potentiation-impairments-via-activation-of-d1-d5-receptors
#7
Yang Ye, Hui Li, Jing-Wen Yang, Xue-Rui Wang, Guang-Xia Shi, Chao-Qun Yan, Si-Ming Ma, Wen Zhu, Qian-Qian Li, Tian-Ran Li, Ling-Yong Xiao, Cun-Zhi Liu
BACKGROUND AND PURPOSE: Emerging evidence suggests that acupuncture could improve cognitive impairment in vascular dementia by enhancing synaptic plasticity in the hippocampus. The purpose of this study is to investigate whether dopamine, a key mediator of synaptic plasticity, is involved in this cognitive improvement. METHODS: Vascular dementia model was established by bilateral common carotid arteries occlusion in male Wistar rats. Three days after the operation, animals received acupuncture treatment for 2 weeks, once daily...
March 13, 2017: Stroke; a Journal of Cerebral Circulation
https://www.readbyqxmd.com/read/28289129/helios-expression-coordinates-the-development-of-a-subset-of-striatopallidal-medium-spiny-neurons
#8
Raquel Martín-Ibáñez, Mónica Pardo, Albert Giralt, Andrés Miguez, Inés Guardia, Lucile Marion-Poll, Cristina Herranz, Miriam Esgleas, Gerardo Garcia-Díaz Barriga, Michael J Edel, Carlos Vicario-Abejón, Jordi Alberch, Jean-Antoine Girault, Susan Chan, Philippe Kastner, Josep M Canals
Here we unravel the mechanism of action of Helios (He) during the development of striatal medium spiny neurons (MSNs). He regulates the second wave of striatal neurogenesis involved in the generation of striatopallidal neurons that express dopamine 2 receptor (D2R) and enkephalin (ENK). To exert this effect He is expressed in neural progenitor cells (NPCs) retaining them into the G1/G0 phase of the cell cycle. Thus, the lack of He produces an increase of S-phase entry and S-phase length of NPCs which in turn impairs striatal neurogenesis and produces an accumulation of the number of cycling NPCs in the germinal zone (GZ) that end up dying at postnatal stages...
March 13, 2017: Development
https://www.readbyqxmd.com/read/28283350/ultrafine-carbon-particles-promote-rotenone-induced-dopamine-neuronal-loss-through-activating-microglial-nadph-oxidase
#9
Yinxi Wang, Dan Liu, Huifeng Zhang, Yixin Wang, Ling Wei, Yutong Liu, Jieying Liao, Hui-Ming Gao, Hui Zhou
BACKGROUND: Atmospheric ultrafine particles (UFPs) and pesticide rotenone were considered as potential environmental risk factors for Parkinson's disease (PD). However, whether and how UFPs alone and in combination with rotenone affect the pathogenesis of PD remains largely unknown. METHODS: Ultrafine carbon black (ufCB, a surrogate of UFPs) and rotenone were used individually or in combination to determine their roles in chronic dopaminergic (DA) loss in neuron-glia, and neuron-enriched, mix-glia cultures...
March 7, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28282463/family-based-association-study-of-drd4-gene-in-methylphenidate-responded-attention-deficit-hyperactivity-disorder
#10
Patrick Wing-Leung Leung, Janice Ka Yan Chan, Lu Hua Chen, Chi Chiu Lee, Se Fong Hung, Ting Pong Ho, Chun Pan Tang, Robert K Moyzis, James M Swanson
The 48-basepair (48-bp) variable number tandem repeat (VNTR) polymorphism in exon 3 of the dopamine receptor D4 gene (DRD4) is implicated in the etiology of attention-deficit/ hyperactivity disorder (ADHD). In particular, ADHD in European-ancestry population is associated with an increased prevalence of the 7-repeat (7R) allele of the exon 3 VNTR. However, it is intriguing to note that the 7R allele has been found to be of very low prevalence in the Chinese general population. In a previous case-control study, our research team had found that the 7R allele was similarly absent in Chinese ADHD children in Hong Kong...
2017: PloS One
https://www.readbyqxmd.com/read/28280480/the-efficacy-and-tolerability-of-the-clonidine-transdermal-patch-in-the-treatment-for-children-with-tic-disorders-a-prospective-open-single-group-self-controlled-study
#11
Pan-Pan Song, Li Jiang, Xiu-Juan Li, Si-Qi Hong, Shuang-Zi Li, Yue Hu
BACKGROUND: To evaluate the efficacy and tolerability of a clonidine transdermal patch in the treatment of children with tic disorders (TD) and to establish a predictive model for patients. METHODS: Forty-one patients who met the inclusion criteria entered into 12 weeks of prospective, open, single-group, self-controlled treatment with a clonidine transdermal patch. The Yale Global Tic Severity Scale (YGTSS) was employed before therapy (baseline) and at 4, 8, and 12 weeks after therapy...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28280410/lamotrigine-an-antiepileptic-drug-inhibits-5-ht3-receptor-currents-in-ncb-20-neuroblastoma-cells
#12
Ki Jung Kim, Seung Hyun Jeun, Ki-Wug Sung
Lamotrigine is an antiepileptic drug widely used to treat epileptic seizures. Using whole-cell voltage clamp recordings in combination with a fast drug application approach, we investigated the effects of lamotrigine on 5-hydroxytryptamine (5-HT)3 receptors in NCB-20 neuroblastoma cells. Co-application of lamotrigine (1~300 µM) resulted in a concentration-dependent reduction in peak amplitude of currents induced by 3 µM of 5-HT for an IC50 value of 28.2±3.6 µM with a Hill coefficient of 1.2±0.1. These peak amplitude decreases were accompanied by the rise slope reduction...
March 2017: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/28275342/prefrontal-dopaminergic-mechanisms-of-extinction-in-adolescence-compared-to-adulthood-in-rats
#13
Isabel C Zbukvic, Chun Hui J Park, Despina E Ganella, Andrew J Lawrence, Jee Hyun Kim
Adolescents with anxiety disorders attain poorer outcomes following extinction-based treatment compared to adults. Extinction deficit during adolescence has been identified to involve immaturity in the medial prefrontal cortex (mPFC). Findings from adult rodents suggest extinction involves dopamine signaling in the mPFC. This system changes dramatically during adolescence, but its role in adolescent extinction is unknown. Therefore, we investigated the role of prefrontal dopamine in extinction using Pavlovian fear conditioning in adolescent and adult rats...
2017: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/28273852/caloric-restriction-protects-against-lactacystin-induced-degeneration-of-dopamine-neurons-independent-of-the-ghrelin-receptor
#14
Jessica Coppens, Eduard Bentea, Jacqueline A Bayliss, Thomas Demuyser, Laura Walrave, Giulia Albertini, Joeri Van Liefferinge, Lauren Deneyer, Najat Aourz, Ann Van Eeckhaut, Jeanelle Portelli, Zane B Andrews, Ann Massie, Dimitri De Bundel, Ilse Smolders
Parkinson's disease (PD) is a neurodegenerative disorder, characterized by a loss of dopamine (DA) neurons in the substantia nigra pars compacta (SNc). Caloric restriction (CR) has been shown to exert ghrelin-dependent neuroprotective effects in the 1-methyl-4-phenyl-1,2,3,6-tetrathydropyridine (MPTP)-based animal model for PD. We here investigated whether CR is neuroprotective in the lactacystin (LAC) mouse model for PD, in which proteasome disruption leads to the destruction of the DA neurons of the SNc, and whether this effect is mediated via the ghrelin receptor...
March 4, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28272861/analysis-of-the-glutamate-agonist-ly404-039-binding-to-non-static-dopamine-receptor-d2-dimer-structures-and-consensus-docking
#15
Ramin Ekhteiari Salmas, Philip Seeman, Busecan Aksoydan, Ismail Erol, Isik Kantarcioglu, Matthias Stein, Mine Yurtsever, Serdar Durdagi
The dopamine receptor D2 (D2R) plays an important role in the human central nervous system and is a focal target of antipsychotic agents. The previously developed D2HighR and D2LowR dimeric models by our group are used to investigate the prediction of binding affinity of LY404,039 ligand and its binding mechanism within the catalytic domain. The obtained computational data using molecular dynamics (MD) simulations fits well with the experimental results. The calculated binding affinities of LY404,039 using MM/PBSA for the D2HighR and D2LowR targets were -12...
March 8, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28271626/acupuncture-reduces-relapse-to-cocaine-seeking-behavior-via-activation-of-gaba-neurons-in-the-ventral-tegmental-area
#16
Wyju Jin, Min Sun Kim, Eun Young Jang, Jun Yeon Lee, Jin Gyeom Lee, Hong Yu Kim, Seong Shoon Yoon, Bong Hyo Lee, Suchan Chang, Jae Hyo Kim, Kwang H Choi, Ho Koo, Young Seob Gwak, Scott C Steffensen, Yeon-Hee Ryu, Hee Young Kim, Chae Ha Yang
There is growing public interest in alternative approaches to addiction treatment and scientific interest in elucidating the neurobiological underpinnings of acupuncture. Our previous studies showed that acupuncture at a specific Shenmen (HT7) points reduced dopamine (DA) release in the nucleus accumbens (NAc) induced by drugs of abuse. The present study was carried out to evaluate the effects of HT7 acupuncture on γ-aminobutyric acid (GABA) neuronal activity in the ventral tegmental area (VTA) and the reinstatement of cocaine-seeking behavior...
March 7, 2017: Addiction Biology
https://www.readbyqxmd.com/read/28271233/regulation-of-glomerulotubular-balance-flow-activated-proximal-tubule-function
#17
REVIEW
Tong Wang, Sheldon Weinbaum, Alan M Weinstein
The purpose of this review is to summarize our knowledge and understanding of the physiological importance and the mechanisms underlying flow-activated proximal tubule transport. Since the earliest micropuncture studies of mammalian proximal tubule, it has been recognized that tubular flow is an important regulator of sodium, potassium, and acid-base transport in the kidney. Increased fluid flow stimulates Na(+) and HCO3(-) absorption in the proximal tubule via stimulation of Na/H-exchanger isoform 3 (NHE3) and H(+)-ATPase...
March 7, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28270751/understanding-the-role-of-gpcr-heteroreceptor-complexes-in-modulating-the-brain-networks-in-health-and-disease
#18
REVIEW
Dasiel O Borroto-Escuela, Jens Carlsson, Patricia Ambrogini, Manuel Narváez, Karolina Wydra, Alexander O Tarakanov, Xiang Li, Carmelo Millón, Luca Ferraro, Riccardo Cuppini, Sergio Tanganelli, Fang Liu, Malgorzata Filip, Zaida Diaz-Cabiale, Kjell Fuxe
The introduction of allosteric receptor-receptor interactions in G protein-coupled receptor (GPCR) heteroreceptor complexes of the central nervous system (CNS) gave a new dimension to brain integration and neuropsychopharmacology. The molecular basis of learning and memory was proposed to be based on the reorganization of the homo- and heteroreceptor complexes in the postjunctional membrane of synapses. Long-term memory may be created by the transformation of parts of the heteroreceptor complexes into unique transcription factors which can lead to the formation of specific adapter proteins...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28266723/contribution-of-dopamine-neurotransmission-in-proconvulsant-effect-of-toxoplasma-gondii-infection-in-male-mice
#19
Jalal Babaie, Mohammad Sayyah, Pezhman Fard-Esfahani, Majid Golkar, Kourosh Gharagozli
Epilepsy is one of the most common neurologic disorders worldwide with no distinguishable cause in 60% of patients. One-third of world's population is infected with Toxoplasma gondii (T. gondii). This intracellular parasite has high tendency to excitable cells including neurons. We assessed seizure susceptibility and involvement of dopaminergic system in male mice with acute and chronic T. gondii infection. Mice were infected by intraperitoneal injection of T. gondii cysts. Acute and chronic stages of infection were determined by quantification of SAG1/BAG1 transcripts and level of repetitive REP-529 sequence in the brain of mice by real-time PCR...
March 7, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28266501/the-novel-modafinil-analog-jjc8-016-as-a-potential-cocaine-abuse-pharmacotherapeutic
#20
Hai-Ying Zhang, Guo-Hua Bi, Hong-Ju Yang, Yi He, Gilbert Xue, Jian-Jing Cao, Gianluigi Tanda, Eliot L Gardner, Amy Hauck Newman, Zheng-Xiong Xi
(±)Modafinil ((±)MOD) and its R-enantiomer (R-modafinil; R-MOD) have been investigated for their potential as treatments for psychostimulant addiction. We recently reported a series of (±)MOD analogues, of which JJC8-016 (N-(2-((bis(4-fluorophenyl)methyl)thio)ethyl)-3-phenylpropan-1-amine) was selected for further development. JJC8-016 and R-MOD were evaluated for binding across ~70 receptors, transporters and enzymes. Although at a concentration of 10 μM, there were many hits for JJC8-016, binding affinities in the range of its DAT affinity were only observed at the serotonin transporter (SERT), dopamine D2-like and sigma1 receptors...
March 7, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
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