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https://www.readbyqxmd.com/read/29473089/the-effects-of-cariprazine-and-aripiprazole-on-pcp-induced-deficits-on-attention-assessed-in-the-5-choice-serial-reaction-time-task
#1
Samuel A Barnes, Jared W Young, Athina Markou, Nika Adham, István Gyertyán, Béla Kiss
RATIONALE: Attentional processing deficits are a core feature of schizophrenia, likely contributing to the persistent functional and occupational disability observed in patients with schizophrenia. The pathophysiology of schizophrenia is hypothesized to involve dysregulation of NMDA receptor-mediated glutamate transmission, contributing to disruptions in normal dopamine transmission. Preclinical investigations often use NMDA receptor antagonists, such as phencyclidine (PCP), to induce cognitive disruptions relevant to schizophrenia...
February 22, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29470766/haloperidol-attenuates-methylphenidate-and-modafinil-induced-behavioural-sensitization-and-cognitive-enhancement
#2
Nausheen Alam, Kulsoom Choudhary
Previous studies have demonstrated that repeated psychostimulant administration produces behavioural sensitization and cognitive tolerance. Brain dopaminergic system and the involvement of dopamine D2 -receptors are considered to be important in psychostimulant-induced sensitization. Study designed to compared the motor activity by using familiar and novel enviroments and cognitive effects by water maze and passive avoidance test after long term administration of methylphenidate(at the dose 0.6 mg/kg/day, 2...
February 22, 2018: Metabolic Brain Disease
https://www.readbyqxmd.com/read/29466326/structure-of-the-d-2-dopamine-receptor-bound-to-the-atypical-antipsychotic-drug-risperidone
#3
Sheng Wang, Tao Che, Anat Levit, Brian K Shoichet, Daniel Wacker, Bryan L Roth
Dopamine is a neurotransmitter that has been implicated in processes as diverse as reward, addiction, control of coordinated movement, metabolism and hormonal secretion. Correspondingly, dysregulation of the dopaminergic system has been implicated in diseases such as schizophrenia, Parkinson's disease, depression, attention deficit hyperactivity disorder, nausea and vomiting, among others. Dopamine's actions are mediated by a family of five G-protein coupled receptors (GPCRs) (viz. D1 , D2 , D3 , D4 and D5 )1 ...
January 24, 2018: Nature
https://www.readbyqxmd.com/read/29459269/study-on-antidepressant-activity-of-chiisanoside-in-mice
#4
Xingbo Bian, Xiaofeng Liu, Jinping Liu, Yan Zhao, Haijun Li, Enbo Cai, Pingya Li, Yugang Gao
The antidepressant-like effect of chiisanoside from the leaves of Acanthopanax sessiliflorus was evaluated by using mice models of depression, forced swim test (FST) and tail suspension test (TST). The results showed that treatment with chiisanoside at dose of 5.0 mg/kg significantly decreased immobility time in the FST and TST. Pretreatment with haloperidol (a non-selective D2 receptor antagonist), bicuculline (a competitive GABA antagonist) and N-methyl-D-aspartic acid (NMDA, an agonist at the glutamate site) effectively reversed the antidepressant-like effect of chiisanoside (5...
February 16, 2018: International Immunopharmacology
https://www.readbyqxmd.com/read/29454493/updating-the-recommendations-for-treatment-of-tardive-syndromes-a-systematic-review-of-new-evidence-and-practical-treatment-algorithm
#5
REVIEW
Roongroj Bhidayasiri, Onanong Jitkritsadakul, Joseph H Friedman, Stanley Fahn
BACKGROUND: Management of tardive syndromes (TS) is challenging, with only a few evidence-based therapeutic algorithms reported in the American Academy of Neurology (AAN) guideline in 2013. OBJECTIVE: To update the evidence-based recommendations and provide a practical treatment algorithm for management of TS by addressing 5 questions: 1) Is withdrawal of dopamine receptor blocking agents (DRBAs) an effective TS treatment? 2) Does switching from typical to atypical DRBAs reduce TS symptoms? 3) What is the efficacy of pharmacologic agents in treating TS? 4) Do patients with TS benefit from chemodenervation with botulinum toxin? 5) Do patients with TS benefit from surgical therapy? METHODS: Systematic reviews were conducted by searching PsycINFO, Ovid MEDLINE, PubMed, EMBASE, Web of Science and Cochrane for articles published between 2012 and 2017 to identify new evidence published after the 2013 AAN guidelines...
February 5, 2018: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/29453947/evaluation-of-the-effects-of-rp5063-a-novel-multimodal-serotonin-receptor-modulator-as-single-agent-therapy-and-co-administrated-with-sildenafil-bosentan-and-treprostinil-in-a-monocrotaline-induced-pulmonary-arterial-hypertension-rat-model
#6
Laxminarayan Bhat, Jon Hawkinson, Marc Cantillon, Dasharatha G Reddy, Seema R Bhat, Charles-E Laurent, Annie Bouchard, Marzena Biernat, Dany Salvail
Pulmonary arterial hypertension (PAH), a condition that is defined by pulmonary vasculature constriction and remodeling, involves dysfunctional signaling of the serotonin (5-HT) receptors, 5-HT 2/2B/7 . In a rat model of monocrotaline (MCT)-induced PAH, the effectiveness of RP5063 (RP), a dopamine and 5-HT receptor modulator, was evaluated as monotherapy and as an adjunct to standard PAH treatments. After a single 60mg/kg dose of MCT, rats received vehicle (MCT+Veh; gavage twice-daily [b.i.d.]), RP (10mg/kg; gavage b...
February 14, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29451703/mechanisms-of-imidazoline-i-2-receptor-agonist-induced-antinociception-in-rats-involvement-of-monoaminergic-neurotransmission
#7
Justin N Siemian, Kaixuan Wang, Yanan Zhang, Jun-Xu Li
BACKGROUND AND PURPOSE: Although studies have established the antinociceptive efficacies of imidazoline I2 receptor (I2 R) agonists, its exact post-receptor mechanism remains unknown. This study tested the hypothesis that monoaminergic transmission is critical for I2 R agonist-induced antinociception. EXPERIMENTAL APPROACH: The von Frey filament test was used to examine the antinociceptive effects of the I2 R agonists 2-BFI and CR4056 on chronic constriction injury (CCI)-induced neuropathic pain or complete Freund's adjuvant (CFA)-induced inflammatory pain in rats...
February 16, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29444518/effects-of-environmental-enrichment-on-nicotine-sensitization-in-rats-neonatally-treated-with-quinpirole-analyses-of-glial-cell-line-derived-neurotrophic-factor-and-implications-towards-schizophrenia
#8
Russell W Brown, Marjorie A Schlitt, Alex S Owens, Caitlynn C DePreter, Elizabeth D Cummins, Seth L Kirby, W Drew Gill, Katherine C Burgess
The current study analyzed the effects of environmental enrichment versus isolation housing on the behavioral sensitization to nicotine in the neonatal quinpirole (NQ; dopamine D2-like agonist) model of dopamine D2 receptor supersensitivity, a rodent model of schizophrenia. NQ treatment in rats increases dopamine D2 receptor sensitivity throughout the animal's lifetime, consistent with schizophrenia. Animals were administered NQ (1 mg/kg) or saline (NS) from postnatal day (P)1 to P21, weaned, and immediately placed into enriched housing or isolated in wire cages throughout the experiment...
February 14, 2018: Developmental Neuroscience
https://www.readbyqxmd.com/read/29432883/regulation-of-phosphorylation-of-ampa-glutamate-receptors-by-muscarinic-m4-receptors-in-the-striatum-in-vivo
#9
Li-Min Mao, Nan He, Dao-Zhong Jin, John Q Wang
The acetylcholine muscarinic 4 (M4) receptor is a principal muscarinic receptor subtype present in the striatum. Notably, Gαi/o-coupled M4 receptors and Gαs/Golf-coupled dopamine D1 receptors are coexpressed in striatonigral projection neurons and are thought to interact with each other to regulate neuronal excitability, although underlying molecular mechanisms are poorly understood. In this study, we investigated the role of M4 receptors in the regulation of phosphorylation of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors in the rat normal and dopamine-stimulated striatum in vivo...
February 9, 2018: Neuroscience
https://www.readbyqxmd.com/read/29427922/psychotomimetic-like-behavioral-effects-of-memantine-in-the-mouse
#10
Nobue Kitanaka, Junichi Kitanaka, F Scott Hall, Yoshiro Kubota, Yumi Mimura, Sayaka Ogura, Yukiya Okada, George R Uhl, Motohiko Takemura
A single administration of mice with memantine (1-amino-3,5-dimethyladamantane), a glutamatergic N-methyl-d-aspartate (NMDA) receptor antagonist, induced stereotyped behaviors in dose- and time-dependent manners. The predominant behavioral component of the stereotypy was a continuous, exaggerated sniffing which was accompanied by persistent locomotion. In contrast, a psychostimulant methamphetamine (METH) predominantly induced a stereotyped biting and other forms of intense stationary stereotypical behaviors...
February 7, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29425815/computer-aided-insights-into-receptor-ligand-interaction-for-novel-5-arylhydantoin-derivatives-as-serotonin-5-ht7-receptor-agents-with-antidepressant-activity
#11
Katarzyna Kucwaj-Brysz, Rafał Kurczab, Magdalena Jastrzębska-Więsek, Ewa Żesławska, Grzegorz Satała, Wojciech Nitek, Anna Partyka, Agata Siwek, Agnieszka Jankowska, Anna Wesołowska, Katarzyna Kieć-Kononowicz, Jadwiga Handzlik
This paper presents a computer-aided insight into the receptor-ligand interaction for novel analogs of the lead structure 5-(4-fluorophenyl)-3-(2-hydroxy-3-(4-(2-methoxyphenyl)piperazin-1-yl)propyl)-5-methylimidazolidine-2,4-dione (1, MF-8), as part of the search for potent and selective serotonin 5-HT7 receptor (5-HT7R) agents. New hydantoin derivatives (4-19) were designed and synthesized. For 5-phenyl-3-(2-hydroxy-3-(4-(2-ethoxyphenyl)piperazin-1-yl)propyl)-5-methylimidazolidine-2,4-dione (4), its crystal structure was determined experimentally...
February 1, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29423959/low-resilience-to-stress-is-associated-with-candidate-gene-expression-alterations-in-the-dopaminergic-signalling-pathway
#12
Esfandiar Azadmarzabadi, Arvin Haghighatfard, Alireza Mohammadi
BACKGROUND: In stressful situations, a person's ability to appropriately complete tasks with minimal anxiety is known as stress resilience. Genetic variants in neuropeptide Y, Corticotropin releasing hormone receptor 1 (CRHR1), and serotonin transporter have been previously reported to be associated with low resilience, but the relationship between low resilience and the dopaminergic signalling pathway is not well understood. Here, we aimed to describe the association between comprehensive psychological characteristics and messenger RNA levels of dopamine receptor D1 (DRD1), dopamine receptor D2 (DRD2), dopamine receptor D3 (DRD3), dopamine receptor D4 (DRD4), dopamine receptor D5 (DRD5), COMT, Dopamine Beta-Hydroxylase (DBH), Tyrosine hydroxylase (TH), monoamine oxidase A (MAOM), dopa decarboxylase (DDC), dopamine transporter (DAT), serotonin transporter (5-HTT), brain-derived neurotrophic factor (BDNF) and glial cell line-derived neurotrophic factor (GDNF) genes based on peripheral blood samples from 400 subjects who react differently to major life event stressors...
February 8, 2018: Psychogeriatrics: the Official Journal of the Japanese Psychogeriatric Society
https://www.readbyqxmd.com/read/29417763/combined-treatment-with-a-selective-pde10a-inhibitor-tak-063-and-either-haloperidol-or-olanzapine-at-subeffective-doses-produces-potent-antipsychotic-like-effects-without-affecting-plasma-prolactin-levels-and-cataleptic-responses-in-rodents
#13
Kazunori Suzuki, Akina Harada, Hirobumi Suzuki, Clizia Capuani, Annarosa Ugolini, Mauro Corsi, Haruhide Kimura
Activation of indirect pathway medium spiny neurons (MSNs) via promotion of cAMP production is the principal mechanism of action of current antipsychotics with dopamine D2 receptor antagonism. TAK-063 [1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one] is a novel phosphodiesterase 10A inhibitor that activates both direct and indirect pathway MSNs through increasing both cAMP and cGMP levels by inhibition of their degradation. The activation of indirect pathway MSNs through the distinct mechanism of action of these drugs raises the possibility of augmented pharmacological effects by combination therapy...
February 2018: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29410048/a-daily-single-dose-of-a-novel-modafinil-analogue-ce-123-improves-memory-acquisition-and-memory-retrieval
#14
Martina Kristofova, Yogesh D Aher, Marija Ilic, Bojana Radoman, Predrag Kalaba, Vladimir Dragacevic, Nilima Y Aher, Johann Leban, Volker Korz, Lisa Zanon, Winfried Neuhaus, Marcus Wieder, Thierry Langer, Ernst Urban, Harald H Sitte, Harald Hoeger, Gert Lubec, Jana Aradska
Dopamine reuptake inhibitors have been shown to improve cognitive parameters in various tasks and animal models. We recently reported a series of modafinil analogues, of which the most promising, 5-((benzhydrylsulfinyl)methyl) thiazole (CE-123), was selected for further development. The present study aims to characterize pharmacological properties of CE-123 and to investigate the potential to enhance memory performance in a rat model. In vitro transporter assays were performed in cells expressing human transporters...
February 1, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29409499/mechanisms-of-multiple-neurotransmitters-in-the-effects-of-lycopene-on-brain-injury-induced-by-hyperlipidemia
#15
Weichun Yang, Ziyi Shen, Sixian Wen, Wei Wang, Minyu Hu
BACKGROUND: Lycopene is a kind of carotenoid, with a strong capacity of antioxidation and regulating the bloodlipid. There has been some evidence that lycopene has protective effects on the central nervous system, but few studies have rigorously explored the role of neurotransmitters in it. Therefore, the present study was designed to investigate the effects of several neurotransmitters as lycopene exerts anti-injury effects induced by hyperlipidemia. METHODS: Eighty adult SD rats, half male and half female, were randomly divided into eight groups on the basis of serum total cholesterol (TC) levels and body weight...
February 7, 2018: Lipids in Health and Disease
https://www.readbyqxmd.com/read/29408274/running-exercise-mitigates-the-negative-consequences-of-chronic-stress-on-dorsal-hippocampal-long-term-potentiation-in-male-mice
#16
Roxanne M Miller, David Marriott, Jacob Trotter, Tyler Hammond, Dane Lyman, Timothy Call, Bethany Walker, Nathanael Christensen, Deson Haynie, Zoie Badura, Morgan Homan, Jeffrey G Edwards
In the hippocampus, learning and memory are likely mediated by synaptic plasticity, known as long-term potentiation (LTP). While chronic intermittent stress is negatively correlated, and exercise positively correlated to LTP induction, we examined whether exercise could mitigate the negative consequences of stress on LTP when co-occurring with stress. Mice were divided into four groups: sedentary no stress, exercise no stress, exercise with stress, and sedentary with stress. Field electrophysiology performed on brain slices confirmed that stress alone significantly reduced dorsal CA1 hippocampal LTP and exercise alone increased LTP compared to controls...
February 9, 2018: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/29407613/effects-of-ammonia-n-exposure-on-the-concentrations-of-neurotransmitters-hemocyte-intracellular-signaling-pathways-and-immune-responses-in-white-shrimp-litopenaeus-vannamei
#17
Lan Zhang, Luqing Pan, Lijun Xu, Lingjun Si
The effects of ammonia-N exposure (transferred from 0.07 to 2, 10 and 20 mg L-1) on the mechanism of neuroendocrine-immunoregulatory network were investigated in Litopenaeus vannamei. The results showed that biogenic amines (dopamine, noradrenaline, 5-hydroxytryptamine) concentrations in treatment groups increased significantly within 12 h. The gene expression of guanylyl cyclase increased significantly from 3 h to 24 h. And dopamine receptor D4 and α2 adrenergic receptor gene expression in treatment groups decreased significantly within 12 h, whereas the mRNA expression of 5-HT7 receptor increased significantly within 3 h and reached the peak levels at 6 h...
January 30, 2018: Fish & Shellfish Immunology
https://www.readbyqxmd.com/read/29407591/novel-multi-target-azinesulfonamides-of-cyclic-amine-derivatives-as-potential-antipsychotics-with-pro-social-and-pro-cognitive-effects
#18
Paweł Zajdel, Tomasz Kos, Krzysztof Marciniec, Grzegorz Satała, Vittorio Canale, Krzysztof Kamiński, Małgorzata Hołuj, Tomasz Lenda, Robert Koralewski, Marek Bednarski, Leszek Nowiński, Jacek Wójcikowski, Władysława A Daniel, Agnieszka Nikiforuk, Irena Nalepa, Piotr Chmielarz, Justyna Kuśmierczyk, Andrzej J Bojarski, Piotr Popik
Currently used antipsychotics are characterized by multireceptor mode of action. While antagonism of dopamine D2 receptors is responsible for the alleviation of "positive" symptoms of schizophrenia and the effects at other, particularly serotonergic receptors are necessary for their additional therapeutic effects, there is no consensus regarding an "ideal" target engagement. Here, a detailed SAR analysis in a series of 45 novel azinesulfonamides of cyclic amine derivatives, involving the aryl-piperazine/piperidine pharmacophore, central alicyclic amine and azinesulfonamide groups has led to the selection of (S)-4-((2-(2-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)isoquinoline (62)...
February 10, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29401659/non-imidazole-histamine-h%C3%A2-ligands-part-vii-synthesis-in-vitro-and-in-vivo-characterization-of-5-substituted-2-thiazol-4-n-propylpiperazines
#19
Roman Guryn, Marek Staszewski, Anna Stasiak, Daniel McNaught Flores, Wiesława Agnieszka Fogel, Rob Leurs, Krzysztof Walczyński
H₃ receptors present on histaminergic and non-histaminergic neurons, act as autoreceptors or heteroreceptors controlling neurotransmitter release and synthesis. Previous, studies have found that the compound N-methyl-N-3-phenylalkyl-2-[2-(4-n-propylpiperazin-1-yl)-1,3-thiazol-5-yl]ethan-1-amine (ADS-531, 2c) exhibits high in vitro potency toward H₃ guinea pig jejunal receptors, with pA₂ = 8.27. To optimize the structure of the lead compound ADS-531, a series of 5-substituted-2-thiazol-4-n-propylpiperazines 3 were synthesized and subjected to in vitro pharmacological characterization; the alkyl chain between position 2 of the thiazole ring and the terminal secondary N-methylamino function was elongated from three to four methylene groups and the N-methylamino functionality was substituted by benzyl-, 2-phenylethyl-, and 3-phenyl-propyl- moieties...
February 3, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29400443/in-vivo-characterization-of-two-18f-labeled-pde10a-pet-radioligands-in-nonhuman-primate-brains
#20
Hui Liu, Hongjun Jin, Zhonghua Luo, Xuyi Yue, Xiang Zhang, Hubert Flores, Yi Su, Joel S Perlmutter, Zhude Tu
PET with Phosphodiesterase 10A (PDE10A) specific radioligands provide a noninvasive and quantitative imaging tool to access the expression of this enzyme in vivo under normal and diseased conditions. We recently reported two potent 18F-labeled PDE10A radioligands (18F-TZ19106B and 18F-TZ8110); initial evaluation in rats and nonhuman primates indicated stable metabolic profiles and excellent target-to-non-target ratio (striatum/cerebellum) for both tracers. Herein, we focused on in vivo characterization of 18F-TZ19106B and 18F-TZ8110 to identify a suitable radioligand for imaging PDE10A in vivo...
February 5, 2018: ACS Chemical Neuroscience
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