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https://www.readbyqxmd.com/read/28921163/discriminative-stimulus-properties-of-the-atypical-antipsychotic-amisulpride-comparison-to-its-isomers-and-to-other-benzamide-derivatives-antipsychotic-antidepressant-and-antianxiety-drugs-in-c57bl-6-mice
#1
Timothy J Donahue, Todd M Hillhouse, Kevin A Webster, Richard Young, Eliseu O De Oliveira, Joseph H Porter
RATIONALE: Racemic (RS)-amisulpride (Solian(®)) is an atypical antipsychotic drug used to treat schizophrenia and dysthymia. Blockade of dopamine D2/D3 and/or serotonin 5-HT7 receptors is implicated in its pharmacological effects. While the (S)-amisulpride isomer possesses a robust discriminative cue, discriminative stimulus properties of (RS)-amisulpride have not been evaluated. OBJECTIVES: The present study established (RS)-amisulpride as a discriminative stimulus and assessed amisulpride-like effects of amisulpride stereoisomers, other benzamide derivatives, and antipsychotic, antidepressant, and anxiolytic drugs...
September 18, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28916921/potential-effect-of-prolonged-sevoflurane-anesthesia-on-the-kinetics-of-11-c-raclopride-in-non-human-primates
#2
Ryosuke Arakawa, Lars Farde, Junya Matsumoto, Naoki Kanegawa, Igor Yakushev, Kai-Chun Yang, Akihiro Takano
PURPOSE: Positron emission tomography (PET) in non-human primates (NHP) is commonly performed under anesthesia, with sevoflurane being a widely used inhaled anesthetic. PET measurement in NHP can be repeated, and a difference in radioligand kinetics has previously been observed between the first and second PET measurement on the same day using sevoflurane anesthesia. In this study, we evaluated the effect of prolonged sevoflurane anesthesia on kinetics and binding potential (BPND) of [(11)C]raclopride in NHP...
September 15, 2017: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
https://www.readbyqxmd.com/read/28895569/the-effects-of-the-monoamine-stabilizer-osu6162-on-binge-like-eating-and-cue-controlled-food-seeking-behavior-in-rats
#3
K Feltmann, C Giuliano, B J Everitt, P Steensland, J Alsiö
Binge eating disorder (BED) is characterized by recurring episodes of excessive consumption of palatable food and an increased sensitivity to food cues. Patients with BED display an addiction-like symptomatology and the dopamine system might be a potential treatment target. The clinically safe monoamine stabilizer (-)-OSU6162 (OSU6162) restores dopaminergic dysfunction in long-term alcohol drinking rats and shows promise as a novel treatment for alcohol use disorder. Here, the effects of OSU6162 on consummatory (binge-like eating) and appetitive (cue-controlled seeking) behavior motivated by chocolate-flavored sucrose pellets were evaluated in non-food-restricted male Lister Hooded rats...
September 12, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28879087/chronic-exposure-to-dopamine-agonists-affects-the-integrity-of-striatal-d2-receptors-in-parkinson-s-patients
#4
Marios Politis, Heather Wilson, Kit Wu, David J Brooks, Paola Piccini
We aimed to investigate the integrity and clinical relevance of striatal dopamine receptor type-2 (D2R) availability in Parkinson's disease (PD) patients. We studied 68 PD patients, spanning from early to advanced disease stages, and 12 healthy controls. All participants received one [(11)C]raclopride PET scan in an OFF medication condition for quantification of striatal D2R availability in vivo. Parametric images of [(11)C]raclopride non-displaceable binding potential were generated from the dynamic [(11)C]raclopride scans using implementation of the simplified reference tissue model with cerebellum as the reference tissue...
2017: NeuroImage: Clinical
https://www.readbyqxmd.com/read/28878639/differential-associations-between-cortical-thickness-and-striatal-dopamine-in-treatment-na%C3%A3-ve-adults-with-adhd-vs-healthy-controls
#5
Mariya V Cherkasova, Nazlie Faridi, Kevin F Casey, Kevin Larcher, Gillian A O'Driscoll, Lily Hechtman, Ridha Joober, Glen B Baker, Jennifer Palmer, Alan C Evans, Alain Dagher, Chawki Benkelfat, Marco Leyton
Alterations in catecholamine signaling and cortical morphology have both been implicated in the pathophysiology of attention deficit/hyperactivity disorder (ADHD). However, possible links between the two remain unstudied. Here, we report exploratory analyses of cortical thickness and its relation to striatal dopamine transmission in treatment-naïve adults with ADHD and matched healthy controls. All participants had one magnetic resonance imaging (MRI) and two [(11)C]raclopride positron emission tomography scans...
2017: Frontiers in Human Neuroscience
https://www.readbyqxmd.com/read/28870629/microinjection-of-the-dopamine-d2-receptor-antagonist-raclopride-into-the-medial-preoptic-area-reduces-rem-sleep-in-lactating-rats
#6
Luciana Benedetto, Mayda Rivas, Matias Cavelli, Florencia Peña, Jaime Monti, Annabel Ferreira, Pablo Torterolo
The medial preoptic area (mPOA) is a brain structure classically related to both non-REM (NREM) sleep and maternal behavior. Although the dopaminergic system is known to play a role in the control of the states of sleep and wakefulness, its effects within the mPOA on sleep are still not clear. Microinjection of the dopamine D2 receptor antagonist Raclopride into the mPOA has been shown to promote nursing postures in lactating dams with no effects on active maternal behavior. We hypothesized that the facilitation of nursing postures may be also associated with the promotion of NREM sleep...
September 1, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28870407/striatal-dopamine-d2-3-receptor-mediated-neurotransmission-in-major-depression-implications-for-anhedonia-anxiety-and-treatment-response
#7
Marta Peciña, Magdalena Sikora, Erich T Avery, Joseph Heffernan, Susana Peciña, Brian J Mickey, Jon-Kar Zubieta
Dopamine (DA) neurotransmission within the brain's reward circuit has been implicated in the pathophysiology of depression and in both, cognitive and pharmacological mechanisms of treatment response. Still, a direct relationship between measures of DA neurotransmission and reward-related deficits in patients with depression has not been demonstrated. To gain insight into the symptom-specific alterations in the DA system in patients with depression, we used positron emission tomography (PET) and the D2/3 receptor-selective radiotracer [(11)C]raclopride in twenty-three non-smoking un-medicated Major Depressive Disorder (MDD) patients and sixteen healthy controls (HC)...
September 1, 2017: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28857231/challenges-in-the-development-of-dopamine-d2-and-d3-selective-radiotracers-for-pet-imaging-studies
#8
Robert H Mach, Robert R Luedtke
The dopamine D2-like receptors (i.e., D2/3 receptors) have been the most extensively studied CNS receptor with PET. The three different radiotracers which have been used in these studies are [(11) C]raclopride, [(18) F]fallypride, and [(11) C]PHNO. Since these radiotracers have a high affinity for both dopamine D2 and D3 receptors, the density of dopamine receptors in the CNS is reported as the D2/3 binding potential, which reflects a measure of the density of both receptor subtypes. Although the development of D2- and D3-selective PET radiotracers has been an active area of research for many years, this by and large presents an unmet need in the area of translational PET imaging studies...
August 31, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/28822101/revisiting-the-logan-plot-to-account-for-non-negligible-blood-volume-in-brain-tissue
#9
Martin Schain, Patrik Fazio, Ladislav Mrzljak, Nahid Amini, Nabil Al-Tawil, Cheryl Fitzer-Attas, Juliana Bronzova, Bernhard Landwehrmeyer, Christina Sampaio, Christer Halldin, Andrea Varrone
BACKGROUND: Reference tissue-based quantification of brain PET data does not typically include correction for signal originating from blood vessels, which is known to result in biased outcome measures. The bias extent depends on the amount of radioactivity in the blood vessels. In this study, we seek to revisit the well-established Logan plot and derive alternative formulations that provide estimation of distribution volume ratios (DVRs) that are corrected for the signal originating from the vasculature...
August 18, 2017: EJNMMI Research
https://www.readbyqxmd.com/read/28816571/effects-of-flow-changes-on-radiotracer-binding-simultaneous-measurement-of-neuroreceptor-binding-and-cerebral-blood-flow-modulation
#10
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
#11
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/28776962/simultaneous-multiple-ms-binding-assays-addressing-d%C3%A2-and-d%C3%A2-dopamine-receptors
#12
Marion Schuller, Georg Höfner, Klaus Theodor Wanner
MS Binding Assays represent a label-free alternative to radioligand binding assays. They provide basically the same capabilities as the latter, however, employ a nonlabelled reporter ligand instead of a radioligand. In contrast to radioligand binding assays, MS Binding Assays offer - due to the selectivity of mass spectrometric detection - basically the opportunity to monitor binding of different reporter ligands towards different targets simultaneously. The present study shows a proof of concept for this strategy as exemplified for MS Binding Assays addressing selectively D₁ and D₂ Dopamine receptors in a single binding experiment...
August 4, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28769095/increased-dopamine-release-after-working-memory-updating-training-neurochemical-correlates-of-transfer
#13
Lars Bäckman, Otto Waris, Jarkko Johansson, Micael Andersson, Juha O Rinne, Kati Alakurtti, Anna Soveri, Matti Laine, Lars Nyberg
Previous work demonstrates that working-memory (WM) updating training results in improved performance on a letter-memory criterion task, transfers to an untrained n-back task, and increases striatal dopamine (DA) activity during the criterion task. Here, we sought to replicate and extend these findings by also examining neurochemical correlates of transfer. Four positron emission tomography (PET) scans using the radioligand raclopride were performed. Two of these assessed DAD2 binding (letter memory; n-back) before 5 weeks of updating training, and the same two scans were performed post training...
August 2, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28752565/the-relationship-between-subcortical-brain-volume-and-striatal-dopamine-d2-3-receptor-availability-in-healthy-humans-assessed-with-11-c-raclopride-and-11-c-phno-pet
#14
Fernando Caravaggio, Jun Ku Chung, Eric Plitman, Isabelle Boileau, Philip Gerretsen, Julia Kim, Yusuke Iwata, Raihaan Patel, M Mallar Chakravarty, Gary Remington, Ariel Graff-Guerrero
BACKGROUND: Abnormalities in dopamine (DA) and brain morphology are observed in several neuropsychiatric disorders. However, it is not fully understood how these abnormalities may relate to one another. For such in vivo findings to be used as biomarkers for neuropsychiatric disease, it must be understood how variability in DA relates to brain structure under healthy conditions. We explored how the availability of striatal DA D2/3 receptors (D2/3 R) is related to the volume of subcortical brain structures in a sample of healthy humans...
July 28, 2017: Human Brain Mapping
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
#15
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/28685616/cerebral-serotonin-release-correlates-with-11-c-az10419369-pet-measures-of-5-ht1b-receptor-binding-in-the-pig-brain
#16
Louise M Jørgensen, Pia Weikop, Claus Svarer, Ling Feng, Sune H Keller, Gitte M Knudsen
Positron emission tomography (PET) can, when used with appropriate radioligands, non-invasively capture temporal and spatial information about acute changes in brain neurotransmitter systems. We here evaluate the 5-HT1B receptor partial agonist PET radioligand, [(11)C]AZ10419369, for its sensitivity to detect changes in endogenous cerebral serotonin levels, as induced by different pharmacological challenges. To enable a direct translation of PET imaging data to changes in brain serotonin levels, we compared the [(11)C]AZ10419369 PET signal in the pig brain to simultaneous measurements of extracellular serotonin levels with microdialysis after various acute interventions (saline, escitalopram, fenfluramine)...
January 1, 2017: Journal of Cerebral Blood Flow and Metabolism
https://www.readbyqxmd.com/read/28666837/operant-responding-for-optogenetic-excitation-of-ldtg-inputs-to-the-vta-requires-d1-and-d2-dopamine-receptor-activation-in-the-nacc
#17
Stephan Steidl, Shannon O'Sullivan, Dustin Pilat, Nancy Bubula, Jason Brown, Paul Vezina
Behavioral studies in rats and mice indicate that laterodorsal tegmental nucleus (LDTg) inputs to the ventral tegmental area (VTA) importantly contribute to reward function. Further evidence from anesthetized rat and mouse preparations suggests that these LTDg inputs may exert this effect by regulating mesolimbic dopamine (DA) signaling. Direct evidence supporting this possibility remains lacking however. To address this lack, rat LDTg neurons were transfected with adeno-associated viral vectors encoding channelrhodopsin2 and eYFP (ChR2) or eYFP alone (eYFP) and rats were subsequently trained to lever press for intracranial self-stimulation (ICSS) of the inputs of these neurons to the VTA...
August 30, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28656313/dopamine-attenuates-ethanol-induced-neuroapoptosis-in-the-developing-rat-retina-via-the-camp-pka-pathway
#18
Junde Han, Lingqi Gao, Jing Dong, Yingtian Wang, Mazhong Zhang, Jijian Zheng
Apoptosis has been identified as the primary cause of fetal alcohol spectrum disorder (FASD), and the development of methods to prevent and treat FASD have been based on the mechanisms of alcohol-induced apoptosis. The present study aimed to explore the effects of dopamine on alcohol‑induced neuronal apoptosis using whole‑mount cultures of rat retinas (postnatal day 7). Retinas were initially incubated with ethanol (100, 200 or 500 mM), and in subsequent analyses retinas were co‑incubated with ethanol (200 mM) and dopamine (10 µM)...
August 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28643800/striatal-dopamine-d2-d3-receptor-availability-varies-across-smoking-status
#19
Corinde E Wiers, Elizabeth A Cabrera, Dardo Tomasi, Christopher T Wong, Şükrü B Demiral, Sung Won Kim, Gene-Jack Wang, Nora D Volkow
To assess how tobacco smoking status affects baseline dopamine D2/D3 (D2R) receptor availability and methylphenidate-induced dopamine (DA) release, we retrospectively analyzed D2R availability measures of 8 current smokers, 10 ex-smokers, and 18 non-smokers who were scanned with Positron Emission Tomography and [(11)C]raclopride, after administration of an injection of placebo or 0.5 mg/kg iv methylphenidate. There was a significant effect of smoking status on baseline striatal D2R availability; with current smokers showing lower striatal D2R availability compared to non-smokers (caudate, putamen and ventral striatum) and to ex-smokers (caudate and putamen)...
June 23, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28583881/altered-adenosine-2a-and-dopamine-d2-receptor-availability-in-the-6-hydroxydopamine-treated-rats-with-and-without-levodopa-induced-dyskinesia
#20
X Zhou, J Doorduin, P H Elsinga, R A J O Dierckx, E F J de Vries, C Casteels
Several lines of evidence imply alterations in adenosine signaling in Parkinson's disease (PD). Here, we investigated cerebral changes in adenosine 2A receptor (A2AR) availability in 6-hydroxydopamine (6-OHDA)-lesioned rats with and without levodopa-induced dyskinesia (LID) using positron-emission tomography (PET) with [(11)C]preladenant. In parallel dopamine type 2 receptor (D2R) imaging with [(11)C]raclopride PET and behavioral tests for motor and cognitive function were performed. METHODS: Parametric A2AR and D2R binding potential (BPND) images were reconstructed using reference tissue models with midbrain and cerebellum as reference tissue, respectively...
June 2, 2017: NeuroImage
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