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https://www.readbyqxmd.com/read/28828976/brexpiprazole-a-partial-dopamine-agonist-for-the-treatment-of-schizophrenia
#1
Asli Ekinci, Okan Ekinci
BACKGROUND: Schizophrenia is a chronic and debilitating mental disorder that affects the patient's and their family's life. The disease remains a complicated disorder that is challenging to treat, despite there being a large antipsychotic armamentarium. Brexpiprazole acts both as a partial agonist at the serotonin 5-HT1A and dopamine D2 receptors and as an antagonist at the serotonin 5-HT2A and noradrenaline alpha1B and alpha2C receptors, all with similar potency. This balanced receptor profile may produce promising antipsychotic effects on positive, negative and cognitive symptoms in schizophrenia with minimal adverse effects...
August 20, 2017: Reviews on Recent Clinical Trials
https://www.readbyqxmd.com/read/28828729/dr1-activation-reduces-the-proliferation-of-vascular-smooth-muscle-cells-by-jnk-c-jun-dependent-increasing-of-prx3
#2
Junting Chen, Sa Shi, Xiaona Cai, Hongzhu Li, Lina Wang, Hong Li, Changqing Xu
Vascular smooth muscle cells (VSMCs) proliferation is a key process in atherosclerosis. However, little is known about the underlying mechanisms, leading to a lack of effective therapy. This study was to investigate whether dopamine receptor 1 (DR1) is involved in the VSMCs proliferation and related mechanisms. A7r5 cells were treated with oxidized low-density lipoprotein (ox-LDL, 10, 20, 50, 100, 200 µg/mL) in the presence or absence of the SKF38393 (DR1agonist), SCH23390 (DR1antiagonist), SP600125 (JNK inhibitor), PD98059(ERK1/2 inhibitor) or NAC (ROS inhibitor)...
August 21, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28828402/neuregulin-and-dopamine-d4-receptors-contribute-independently-to-depotentiation-of-schaffer-collateral-ltp-by-temperoammonic-path-stimulation
#3
Yukitoshi Izumi, Charles F Zorumski
Prior studies have found that dopamine (DA), acting at D4 receptors, and neuregulin (NRG), likely acting at ErbB4 receptors, are involved in a form of depotentiation of long-term potentiation (LTP) at Schaffer collateral (SC) synapses in the hippocampus. Furthermore, DA and NRG actions are intertwined in that NRG induces DA release. We previously found that low-frequency stimulation (LFS) of temperoammonic (TA) inputs to area CA1 also depotentiates previously established SC LTP through a complex signaling pathway involving endocannabinoids, GABA, adenosine, and mitogen-activated protein kinases (MAPKs), but not glutamate...
July 2017: ENeuro
https://www.readbyqxmd.com/read/28826524/small-molecule-receptor-ligands-for-pet-studies-of-the-central-nervous-system-focus-on-g-protein-coupled-receptors
#4
REVIEW
Robert H Mach
G protein-coupled receptors (GPRCs) are a class of proteins that are expressed in high abundance and are responsible for numerous signal transduction pathways in the central nervous system. Consequently, alterations in GPRC function have been associated with a wide variety of neurologic and neuropsychiatric disorders. The development of PET probes for imaging GPRCs has served as a major emphasis of PET radiotracer development and PET imaging studies over the past 30 years. In this review, a basic description of the biology of G proteins and GPRCs is provided...
September 2017: Seminars in Nuclear Medicine
https://www.readbyqxmd.com/read/28826502/sexual-dimorphism-in-striatal-dopaminergic-responses-promotes-monogamy-in-social-songbirds
#5
Kirill Tokarev, Julia Hyland Bruno, Iva Ljubičić, Paresh J Kothari, Santosh A Helekar, Ofer Tchernichovski, Henning U Voss
In many songbird species, males sing to attract females and repel rivals. How can gregarious, non-territorial songbirds such as zebra finches, where females have access to numerous males, sustain monogamy? We found that the dopaminergic reward circuitry of zebra finches can simultaneously promote social cohesion and breeding boundaries. Surprisingly, in unmated males but not in females, striatal dopamine neurotransmission was elevated after hearing songs. Behaviorally too, unmated males but not females persistently exchanged mild punishments in return for songs...
August 11, 2017: ELife
https://www.readbyqxmd.com/read/28822602/time-dependent-role-of-prefrontal-cortex-and-hippocampus-on-cognitive-improvement-by-aripiprazole-in-olfactory-bulbectomized-mice
#6
Kohei Takahashi, Osamu Nakagawasai, Wataru Nemoto, Takayo Odaira, Yuichiro Arai, Tadashi Hisamitsu, Koichi Tan-No
Dopamine (DA) modulates cognitive functions in the prefrontal cortex (PFC) and hippocampus. Olfactory bulbectomy (OBX) in mice induces cognitive dysfunctions. Recently, we reported that aripiprazole (ARI) normalizes the behavioral hyper-responsivity to DA agonists in OBX mice. However, it remains unclear whether ARI affects OBX-induced cognitive dysfunctions. To address this question we evaluated ARI-treated and untreated OBX mice in a passive avoidance test. Then, we investigated the effects of ARI on cell proliferation in the hippocampal dentate gyrus by immunohistochemistry, and on c-fos levels in the PFC and hippocampus, as well as nerve growth factor (NGF) levels in the hippocampus by western blotting...
August 16, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28822047/the-quinpirole-hypolocomotive-effects-are-strain-and-route-of-administration-dependent-in-shr-and-sla16-isogenic-rats
#7
R A N Pértile, M E Corvino, R C N Marchette, E Pavesi, J Cavalli, A Ramos, G S Izídio
The SHR and SLA16 inbred strains present behavioral differences in anxiety/emotionality that could be under the influence of dopaminergic neurotransmission. In order to investigate the role of D2 receptors in modulating such differences, an agonist (quinpirole) and an antagonist (haloperidol) of this receptor were administered, either via systemic injection (IP), or microinjected into the ventral area of the hippocampus (vHIP). Quinpirole and haloperidol IP decreased locomotor activity, only in SLA16 rats in the open-field (OF), and in both strains in the elevated plus-maze (EPM)...
August 18, 2017: Behavior Genetics
https://www.readbyqxmd.com/read/28821667/fibroblast-growth-factor-2-in-the-dorsomedial-striatum-is-a-novel-positive-regulator-of-alcohol-consumption
#8
Oren Even-Chen, Yossi Sadot-Sogrin, Ohad Shaham, Segev Barak
Repeated alcohol intake leads to mesostriatal neuroadaptations, resulting in drinking escalation and addiction phenotypes. Fibroblast growth factor 2 (FGF2) has been shown to interact with the mesostriatal dopaminergic system, and has been implicated in the actions of psychostimulants in the brain, and in several psychiatric disorders. Here, we report on a positive regulatory feedback loop of alcohol and FGF2 in rodent models. Specifically, we found that acute alcohol exposure (2.5 g/kg, i.p.) increased the mRNA expression of Fgf2 in the dorsal hippocampus, nucleus accumbens and dorsal striatum...
August 8, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28821448/cognitive-impairment-and-gene-expression-alterations-in-a-rodent-model-of-binge-eating-disorder
#9
A Chawla, Z A Cordner, G Boersma, T H Moran
Binge eating disorder (BED) is defined as recurrent, distressing over-consumption of palatable food (PF) in a short time period. Clinical studies suggest that individuals with BED may have impairments in cognitive processes, executive functioning, impulse control, and decision-making, which may play a role in sustaining binge eating behavior. These clinical reports, however, are limited and often conflicting. In this study, we used a limited access rat model of binge-like behavior in order to further explore the effects of binge eating on cognition...
August 15, 2017: Physiology & Behavior
https://www.readbyqxmd.com/read/28820571/comparison-of-spreading-depolarizations-in-the-motor-cortex-and-nucleus-accumbens-similar-patterns-of-oxygen-responses-and-the-role-of-dopamine
#10
Caddy Noahl Hobbs, Gordon Holzberg, Akira S Min, R Mark Wightman
Spreading depolarizations (SD) are pathophysiological phenomena that spontaneously arise in traumatized neural tissue and can promote cellular death. Most investigations of SD are performed in the cortex, a brain region that is susceptible to these depolarizing waves and accessible via a variety of monitoring techniques. Here, we describe SD responses in the cortex and the deep brain region of the nucleus accumbens (NAc) of the anesthetized rat with a minimally invasive, implantable sensor. With high temporal resolution, we characterize the time course of oxygen responses to SD in relation to the electrophysiological depolarization signal...
August 18, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28820054/qsar-modeling-of-histamine-h3r-antagonists-inverse-agonists-as-future-drugs-for-neurodegenerative-diseases
#11
Michelle Fidelis Corrêa, João Paulo Dos Santos Fernandes
Histamine H3 receptor (H3R) is associated with several neuropsychological diseases. It is predominantly expressed in the central nervous system as presynaptic receptor, especially in regions associated with cognition and behavior, and is responsible for modulate the synthesis and release of histamine and other neurotransmitters such as acetylcholine, dopamine and serotonin. Therefore, H3R is an important target involved in several CNS disorders, such as narcolepsy, attention deficit hyperactivity disorder and schizophrenia...
August 17, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28818747/antidepressant-like-activity-of-methyl-jasmonate-involves-modulation-of-monoaminergic-pathways-in-mice
#12
Solomon Umukoro, Adaeze Adebesin, Gladys Agu, Osarume Omorogbe, Stephen Babajide Asehinde
PURPOSE: The efficacy of current antidepressant drugs has been compromised by adverse effects, low remission and delay onset of action necessitating the search for alternative agents. Methyl jasmonate (MJ), a bioactive compound isolated from Jasminum grandiflorum has been shown to demonstrate antidepressant activity but its mechanism of action remains unknown. Thus, the role of monoaminergic systems in the antidepression-like activity of MJ was investigated in this study. MATERIALS AND METHODS: Mice were given i...
August 14, 2017: Advances in Medical Sciences
https://www.readbyqxmd.com/read/28818716/positron-emission-tomography-pet-imaging-of-nicotine-induced-dopamine-release-in-squirrel-monkeys-using-18-f-fallypride
#13
Jennifer E Naylor, Takato Hiranita, Katelin S Matazel, Xuan Zhang, Merle G Paule, Amy K Goodwin
BACKGROUND: Nicotine, the principal psychoactive tobacco constituent, is thought to produce its reinforcing effects via actions within the mesolimbic dopamine (DA) system. The objective of the current study was to examine the effect of nicotine on DA D2/D3 receptor availability in the nonhuman primate brain with the use of the radioligand [(18)F]fallypride and positron emission tomography (PET). METHODS: Ten adult male squirrel monkeys were used in the current study...
August 8, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28816835/acute-worsening-of-tics-on-varenicline
#14
Shivam Om Mittal, Bryan T Klassen, Anhar Hassan, James H Bower, Elizabeth A Coon
OBJECTIVE: The aim of this study was to report worsening of Tourette syndrome (TS) in 2 patients treated with varenicline. BACKGROUND: Abnormal dopaminergic signaling is likely involved in the pathophysiology of TS. Varenicline is a partial α4β2 nicotinic acetylcholine agonist that enhances dopamine release. Therefore, the use of varenicline may influence tics in patients with TS. METHOD: We analyzed and described 2 case studies on patients with significant worsening of tics after treatment with varenicline...
August 14, 2017: Clinical Neuropharmacology
https://www.readbyqxmd.com/read/28816571/effects-of-flow-changes-on-radiotracer-binding-simultaneous-measurement-of-neuroreceptor-binding-and-cerebral-blood-flow-modulation
#15
Christin Y Sander, Joseph B Mandeville, Hsiao-Ying Wey, Ciprian Catana, Jacob M Hooker, Bruce R Rosen
The potential effects of changes in blood flow on the delivery and washout of radiotracers has been an ongoing question in PET bolus injection studies. This study provides practical insight into this topic by experimentally measuring cerebral blood flow (CBF) and neuroreceptor binding using simultaneous PET/MRI. Hypercapnic challenges (7% CO2) were administered to non-human primates in order to induce controlled increases in CBF, measured with pseudo-continuous arterial spin labeling. Simultaneously, dopamine D2/D3 receptor binding of [(11)C]raclopride or [(18)F]fallypride was monitored with dynamic PET...
January 1, 2017: Journal of Cerebral Blood Flow and Metabolism
https://www.readbyqxmd.com/read/28816243/dopamine-synthesis-capacity-is-associated-with-d2-3-receptor-binding-but-not-dopamine-release
#16
Anne S Berry, Vyoma D Shah, Daniella J Furman, Robert L White, Suzanne L Baker, James P O'Neil, Mustafa Janabi, Mark D'Esposito, William J Jagust
Positron Emission Tomography (PET) imaging allows the estimation of multiple aspects of dopamine function including dopamine synthesis capacity, dopamine release, and D2/3 receptor binding. Though dopaminergic dysregulation characterizes a number of neuropsychiatric disorders including schizophrenia and addiction, there has been relatively little investigation into the nature of relationships across dopamine markers within healthy individuals. Here we used PET imaging in 40 healthy adults to compare, within individuals, estimates of dopamine synthesis capacity (Ki) using 6-[(18)F]fluoro-l-m-tyrosine ([(18)F]FMT; a substrate for aromatic amino acid decarboxylase), baseline D2/3 receptor binding potential using [(11)C]raclopride (a weak competitive D2/3 receptor antagonist), and dopamine release using [(11)C]raclopride paired with oral methylphenidate administration...
August 17, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28815728/effects-of-bifenthrin-exposure-on-the-estrogenic-and-dopaminergic-pathways-in-zebrafish-embryos-and-juveniles
#17
Luísa Becker Bertotto, Jaben Richards, Jay Gan, David Christopher Volz, Daniel Schlenk
Bifenthrin (BF) is a pyrethroid insecticide used in urban and agricultural applications. Previous studies have shown that environmentally relevant (ng/L) concentrations of BF increased plasma concentrations of 17β-estradiol (E2) and altered the expression of dopaminergic (DA) pathway components. DA neurons can indirectly regulate E2 biosynthesis, suggesting that BF may disrupt the hypothalamic-pituitary-gonadal (HPG) axis. Since embryos do not have a complete HPG axis, the hypothesis that BF impairs DA regulation was tested in embryonic and one-month old juvenile zebrafish (Danio rerio) with exposure to measured concentrations of 0...
August 16, 2017: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/28814122/flibanserin-toxicity-in-a-toddler-following-ingestion
#18
Nicholas Granzella, Betty C Chen, Geoffrey S Baird, Matthew Valento
INTRODUCTION: Flibanserin is a medication recently approved by the FDA for treatment of generalized hypoactive sexual desire disorder (HSDD) in premenopausal women. Its mechanism of action is not fully understood but is thought to modulate serotonin receptors and increase levels of norepinephrine and dopamine. While much is known about toxicity of other drugs which affect these systems, there is little information about toxicity of flibanserin at this time. CASE: We present a case of a 2-year-old boy who ingested an estimated 600 mg of his mother's flibanserin...
August 17, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28812266/oxytocin-and-social-relationships-from-attachment-to-bond-disruption
#19
Oliver J Bosch, Larry J Young
Social relationships throughout life are vital for well-being and physical and mental health. A significant amount of research in animal models as well as in humans suggests that oxytocin (OT) plays an important role in the development of the capacity to form social bonds, the mediation of the positive aspects of early-life nurturing on adult bonding capacity, and the maintenance of social bonding. Here, we focus on the extensive research on a socially monogamous rodent model organism, the prairie vole (Microtus ochrogaster)...
August 16, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28812124/clozapine-chlorpromazine-and-risperidone-dose-dependently-reduce-emotional-hyperthermia-a-biological-marker-of-salience
#20
William W Blessing, Esther M Blessing, Mazher Mohammed, Youichirou Ootsuka
RATIONALE: We recently introduced a new rat model of emotional hyperthermia in which a salient stimulus activates brown adipose tissue (BAT) thermogenesis and tail artery constriction. Antipsychotic drugs, both classical and second generation, act to reduce excessive assignment of salience to objects and events in the external environment. The close association between salient occurrences and increases in body temperature suggests that antipsychotic drugs may also reduce emotional hyperthermia...
August 15, 2017: Psychopharmacology
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