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D2 occupancy

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https://www.readbyqxmd.com/read/28643852/therapeutic-d2-3-receptor-occupancies-and-response-with-low-amisulpride-blood-concentrations-in-very-late-onset-schizophrenia-like-psychosis-vloslp
#1
Suzanne Reeves, Kate Eggleston, Elizabeth Cort, Emma McLachlan, Stuart Brownings, Akshay Nair, Suki Greaves, Alan Smith, Joel Dunn, Paul Marsden, Robert Kessler, David Taylor, Julie Bertrand, Robert Howard
OBJECTIVE: Antipsychotic drug sensitivity in very late-onset schizophrenia-like psychosis (VLOSLP) is well documented, but poorly understood. This study aimed to investigate blood drug concentration, D2/3 receptor occupancy and outcome in VLOSLP during open amisulpride prescribing, and compare this with Alzheimer's disease (AD). METHODS: Blood drug concentration, prolactin, symptoms and extrapyramidal side-effects (EPS) were serially assessed during dose titration...
June 23, 2017: International Journal of Geriatric Psychiatry
https://www.readbyqxmd.com/read/28541050/crystal-structure-of-pr3mgni14dx-studied-by-in-situ-neutron-diffraction
#2
Kenji Iwase, Kazuhiro Mori, Naoyoshi Terashita, Suguru Tashiro, Tetsuya Suzuki
The crystal structure of Pr3MgNi14D18 was determined by neutron diffraction. The determined structure of Pr3MgNi14D18 consisted of 89.0% Gd2Co7-type structure and 11.0% PuNi3-type structure. The lattice parameters of a and c of Gd2Co7-type structure were refined at 0.52903(7) nm and 3.90179(1) nm. The deuterium atoms were distributed among nine deuterium sites in both the CaCu5-type and MgZn2-type cells. The D2 occupancy in the Pr2Ni4 octahedral sites of the CaCu5-type cell was the largest (0.75) when compared with the other deuterium sites (<0...
May 25, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28486094/a-pharmacodynamic-modelling-and-simulation-study-identifying-gender-differences-of-daily-olanzapine-dose-and-dopamine-d2-receptor-occupancy
#3
Andy R Eugene, Jolanta Masiak
BACKGROUND: Gender differences in treatment response rates for patients treated with antipsychotics are known. However, the literature lacks a pharmacodynamic model to allow for gender-based clinical trial simulations from modelling parameters for Olanzapine and dopamine D2 receptor occupancy. Thus, the primary aim of this analysis is to test and quantify the effect of gender on the pharmacodynamics of Olanzapine. METHODS: Population pharmacodynamic modelling was performed using non-linear mixed effects modelling in MONOLIX, while the Clinical Trial Simulations were performed using R for statistical programming...
August 2017: Nordic Journal of Psychiatry
https://www.readbyqxmd.com/read/28412910/aripiprazole-a-drug-that-displays-partial-agonism-and-functional-selectivity
#4
Erin W Tuplin, Matthew R Holahan
The treatment of schizophrenia is challenging due to the wide range of symptoms (positive, negative, cognitive) associated with the disease. Typical antipsychotics that antagonize D2 receptors are effective in treating positive symptoms, but extrapyramidal side-effects (EPS) are a common occurrence. Atypical antipsychotics targeting 5-TH2A and D2 receptors are more effective at treating cognitive and negative symptoms compared to typical antipsychotics, but these drugs also result in side-effects such as metabolic syndromes...
April 13, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28395348/exposure-assessment-in-a-single-walled-carbon-nanotube-primary-manufacturer
#5
Serge Kouassi, Cyril Catto, Claude Ostiguy, Gilles L'Espérance, Jens Kroeger, Maximilien Debia
Objectives: This study was aimed at documenting and characterizing occupational exposure to single-walled carbon nanotubes (SWCNTs) generated in a primary manufacturing plant. It also compared various strategies of exposure monitoring. Methods: A 6-day measurement protocol was scheduled (D1-D6) including both (i) quasi-personal monitoring with an array of direct reading instruments (DRIs) and (ii) offline electron microscopy analyses of surface and breathing zone filter-based samples...
March 1, 2017: Annals of Work Exposures and Health
https://www.readbyqxmd.com/read/28365375/preclinical-molecular-imaging-of-glutamatergic-and-dopaminergic-neuroreceptor-kinetics-in-obsessive-compulsive-disorder
#6
S Servaes, D Glorie, J Verhaeghe, S Stroobants, S Staelens
BACKGROUND: Molecular neuroimaging was applied in the quinpirole rat model for compulsive checking in OCD to visualize the D2- and mGluR5-receptor occupancy with Raclopride and ABP-688 microPET/CT. METHODS: Animals (n=48) were exposed to either saline (CTRL; 1mL/kg) or quinpirole (QP; dopamine D2-agonist, 0.5mg/kg) in a single injection (RAC and ABP acute groups) or twice-weekly during 7weeks (chronic group). Animals underwent PET/CT after the 1st injection (acute) or before initial exposure and following the 10th injection in week 5 (chronic)...
March 30, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28334978/therapeutic-window-of-dopamine-d2-3-receptor-occupancy-to-treat-psychosis-in-alzheimer-s-disease
#7
Suzanne Reeves, Emma McLachlan, Julie Bertrand, Fabrizia D Antonio, Stuart Brownings, Akshay Nair, Suki Greaves, Alan Smith, David Taylor, Joel Dunn, Paul Marsden, Robert Kessler, Robert Howard
See Caravaggio and Graff-Guerrero (doi:10.1093/awx023) for a scientific commentary on this article.Antipsychotic drugs, originally developed to treat schizophrenia, are used to treat psychosis, agitation and aggression in Alzheimer's disease. In the absence of dopamine D2/3 receptor occupancy data to inform antipsychotic prescribing for psychosis in Alzheimer's disease, the mechanisms underpinning antipsychotic efficacy and side effects are poorly understood. This study used a population approach to investigate the relationship between amisulpride blood concentration and central D2/3 occupancy in older people with Alzheimer's disease by combining: (i) pharmacokinetic data (280 venous samples) from a phase I single (50 mg) dose study in healthy older people (n = 20, 65-79 years); (ii) pharmacokinetic, 18F-fallypride D2/3 receptor imaging and clinical outcome data on patients with Alzheimer's disease who were prescribed amisulpride (25-75 mg daily) to treat psychosis as part of an open study (n = 28; 69-92 years; 41 blood samples, five pretreatment scans, 19 post-treatment scans); and (iii) 18F-fallypride imaging of an antipsychotic free Alzheimer's disease control group (n = 10, 78-92 years), to provide additional pretreatment data...
April 1, 2017: Brain: a Journal of Neurology
https://www.readbyqxmd.com/read/28193454/new-developments-in-brain-research-of-internet-and-gaming-disorder
#8
REVIEW
Aviv Weinstein, Abigail Livny, Abraham Weizman
There is evidence that the neural mechanisms underlying Internet Gaming Disorder (IGD) resemble those of drug addiction. Functional Magnetic Resonance Imaging (fMRI) studies of the resting state and measures of gray matter volume have shown that Internet game playing was associated with changes to brain regions responsible for attention and control, impulse control, motor function, emotional regulation, sensory-motor coordination. Furthermore, Internet game playing was associated with lower white matter density in brain regions that are involved in decision-making, behavioral inhibition and emotional regulation...
April 2017: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/28187335/insight-into-illness-and-its-relationship-to-illness-severity-cognition-and-estimated-antipsychotic-dopamine-receptor-occupancy-in-schizophrenia-an-antipsychotic-dose-reduction-study
#9
Philip Gerretsen, Hiroyoshi Takeuchi, Miracle Ozzoude, Ariel Graff-Guerrero, Hiroyuki Uchida
Little is known about the influence of D2 receptor occupancy on impaired insight into illness (III)-a core feature of schizophrenia. III is associated with illness severity and cognitive dysfunction. Comparably, supratherapeutic D2 receptor occupancy can impair cognition. However, it is unclear how illness severity, cognition, and D2 receptor occupancy interact to influence III in schizophrenia. The aim of this study was to explore the influence of antipsychotic dose reduction on the relationships of illness severity and cognition to III...
May 2017: Psychiatry Research
https://www.readbyqxmd.com/read/28088727/representativeness-of-clinical-pet-study-participants-with-schizophrenia-a-systematic-review
#10
So Kirino, Takefumi Suzuki, Hiroyoshi Takeuchi, Masaru Mimura, Hiroyuki Uchida
While positron emission tomography (PET) studies have provided invaluable data on antipsychotic effects, selection bias remains a serious concern. A systematic review of PET studies that measured dopamine D2 receptor blockade with antipsychotics was conducted to examine their inclusion/exclusion criteria, using PubMed, EMBASE, and ClinicalTrials.gov (last search, September 2016). PET studies were included if they measured D2 receptor occupancy in patients with schizophrenia and included introduction of antipsychotic treatment or antipsychotic regimen change in a systematic manner...
May 2017: Journal of Psychiatric Research
https://www.readbyqxmd.com/read/28063918/simultaneous-in-vivo-receptor-occupancy-assays-for-serotonin-1a-2a-and-dopamine-2-receptors-with-the-use-of-non-radiolabelled-tracers-proposed-method-in-screening-antipsychotics
#11
Jagadeesh Babu Thentu, Ramakrishna Nirogi, Gopinadh Bhyrapuneni, Devender Reddy Ajjala, Raghupathi Reddy Aleti, Raghava Choudary Palacharla
INTRODUCTION: Conventionally, receptor occupancy assays employ radiolabelled tracer. However, recent advances with non-radiolabelled tracers brought a revolution in target engagement assays. Non-radiolabelled tracer based receptor occupancy uses LC-MS/MS based quantification. It offers simultaneous quantification of more than one tracer; thus, provides the feasibility of evaluating multiple targets in a single animal. In the present study, we demonstrated simultaneous measurement of serotonin 1A, serotonin 2A, and dopamine 2 receptor occupancy using non-radiolabelled tracers in rats...
May 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/27782768/extrastriatal-dopamine-d2-3-receptors-and-cortical-grey-matter-volumes-in-antipsychotic-na%C3%A3-ve-schizophrenia-patients-before-and-after-initial-antipsychotic-treatment
#12
Henrik Nørbak-Emig, Lars H Pinborg, Jayachandra M Raghava, Claus Svarer, William F C Baaré, Peter Allerup, Lars Friberg, Egill Rostrup, Birte Glenthøj, Bjørn H Ebdrup
OBJECTIVES: Long-term dopamine D2/3 receptor blockade, common to all antipsychotics, may underlie progressive brain volume changes observed in patients with chronic schizophrenia. In the present study, we examined associations between cortical volume changes and extrastriatal dopamine D2/3 receptor binding potentials (BPND) in first-episode schizophrenia patents at baseline and after antipsychotic treatment. METHODS: Twenty-two initially antipsychotic-naïve patients underwent magnetic resonance imaging (MRI), [(123)I]epidepride single-photon emission computerised tomography (SPECT), and psychopathology assessments before and after 3 months of treatment with either risperidone (N = 13) or zuclopenthixol (N = 9)...
October 26, 2016: World Journal of Biological Psychiatry
https://www.readbyqxmd.com/read/27745731/prediction-of-cns-occupancy-of-dopamine-d2-receptor-based-on-systemic-exposure-and-in%C3%A2-vitro-experiments
#13
Kayoko Kanamitsu, Ryosuke Arakawa, Yuichi Sugiyama, Tetsuya Suhara, Hiroyuki Kusuhara
The effect of drugs in the central nervous system (CNS) is closely related to occupancy of their target receptor. In this study, we integrated plasma concentrations, in vitro/in vivo data for receptor or protein binding, and in silico data, using a physiologically based pharmacokinetic model, to examine the predictability of receptor occupancy in humans. The occupancy of the dopamine D2 receptor and the plasma concentrations of the antipsychotic drugs quetiapine and perospirone in humans were collected from the literature or produced experimentally...
December 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27715007/dopamine-d3-d2-receptor-antagonist-pf-4363467-attenuates-opioid-drug-seeking-behavior-without-concomitant-d2-side-effects
#14
Travis T Wager, Thomas Chappie, David Horton, Ramalakshmi Y Chandrasekaran, Brian Samas, Elizabeth R Dunn-Sims, Cathleen Hsu, Nawshaba Nawreen, Michelle A Vanase-Frawley, Rebecca E O'Connor, Christopher J Schmidt, Keith Dlugolenski, Nancy C Stratman, Mark J Majchrzak, Bethany L Kormos, David P Nguyen, Aarti Sawant-Basak, Andy N Mead
Dopamine receptor antagonism is a compelling molecular target for the treatment of a range of psychiatric disorders, including substance use disorders. From our corporate compound file, we identified a structurally unique D3 receptor (D3R) antagonist scaffold, 1. Through a hybrid approach, we merged key pharmacophore elements from 1 and D3 agonist 2 to yield the novel D3R/D2R antagonist PF-4363467 (3). Compound 3 was designed to possess CNS drug-like properties as defined by its CNS MPO desirability score (≥4/6)...
January 18, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/27698361/short-term-effects-of-risperidone-monotherapy-on-spontaneous-brain-activity-in-first-episode-treatment-na%C3%A3-ve-schizophrenia-patients-a-longitudinal-fmri-study
#15
Mao-Lin Hu, Xiao-Fen Zong, Jun-Jie Zheng, Spiro P Pantazatos, Jeffrey M Miller, Zong-Chang Li, Yan-Hui Liao, Ying He, Jun Zhou, De-En Sang, Hong-Zeng Zhao, Lu-Xian Lv, Jin-Song Tang, J John Mann, Xiao-Gang Chen
It is unclear whether abnormal spontaneous neural activation patterns found in chronic schizophrenia patients (CSP) are part of the pathogenesis of disease, consequences of chronic illness, or effects of antipsychotic treatment. We performed a longitudinal resting-state functional magnetic resonance imaging (fMRI) study in 42 treatment-naïve first-episode schizophrenia patients (FESP) at baseline and then after 8-weeks of risperidone monotherapy, and compared the findings to 38 healthy volunteers. Spontaneous brain activity was quantified using the fractional amplitude of low-frequency fluctuations (fALFF) and regional homogeneity (ReHo) and compared between patients and controls...
October 4, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27687785/an-original-pharmacoepidemiological-pharmacodynamic-method-application-to-antipsychotic-induced-movement-disorders
#16
Thi Thu Ha Nguyen, Antoine Pariente, Jean-Louis Montastruc, Maryse Lapeyre-Mestre, Vanessa Rousseau, Olivier Rascol, Bernard Bégaud, François Montastruc
AIMS: Pharmacovigilance databases are usually used to detect new potential signals that are relevant for drug safety. They are seldom used for explanatory purposes, e.g. to understand the mechanisms of adverse drug reactions (ADRs). The aim of the present study was to combine pharmacovigilance and pharmacodynamic data to investigate the association between dopamine D2, serotonin 5HT2A, and muscarinic M1 receptor occupancy and the risks of antipsychotic drug (AP)-induced movement disorders...
March 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27631410/plasma-levels-and-estimated-dopamine-d2-receptor-occupancy-of-long-acting-injectable-risperidone-during-maintenance-treatment-of-schizophrenia-a-3-year-follow-up-study
#17
Saeko Ikai, Takefumi Suzuki, Masaru Mimura, Hiroyuki Uchida
INTRODUCTION: Dopamine D2 receptor occupancy levels needed for the maintenance treatment of schizophrenia remain to be elucidated. We examined 3-year clinical outcomes of patients with schizophrenia who received long-acting injectable risperidone (LAI risperidone) at baseline and investigated their dopamine D2 receptor occupancy levels, estimated from plasma drug concentrations. METHODS: A chart review of 52 outpatients with schizophrenia who participated in the original cross-sectional study was conducted to examine their 3-year clinical outcomes between April and September 2015...
September 8, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27617278/summary-data-of-potency-and-parameter-information-from-semi-mechanistic-pkpd-modeling-of-prolactin-release-following-administration-of-the-dopamine-d2-receptor-antagonists-risperidone-paliperidone-and-remoxipride-in-rats
#18
Amit Taneja, An Vermeulen, Dymphy R H Huntjens, Meindert Danhof, Elizabeth C M De Lange, Johannes H Proost
We provide the reader with relevant data related to our recently published paper, comparing two mathematical models to describe prolactin turnover in rats following one or two doses of the dopamine D2 receptor antagonists risperidone, paliperidone and remoxipride, "A comparison of two semi-mechanistic models for prolactin release and prediction of receptor occupancy following administration of dopamine D2 receptor antagonists in rats" (Taneja et al., 2016) [1]. All information is tabulated. Summary level data on the in vitro potencies and the physicochemical properties is presented in Table 1...
September 2016: Data in Brief
https://www.readbyqxmd.com/read/27600596/the-dopamine-d3-receptor-a-quarter-century-later
#19
REVIEW
Pierre Sokoloff, Bernard Le Foll
This review updates the existing knowledge suggesting a role for the D3 receptor in schizophrenia and drug addiction. The D3 receptor is expressed in brain regions controlling reward, emotions, and motivation. Antipsychotics bind in vitro to the D3 receptor with similar affinity as to the D2 receptor, and occupancy of D3 receptors in vivo by these compounds given acutely at clinical dosage have been demonstrated in Positron Emission Tomography (PET) studies. The D3 receptor modulates glutamatergic pathways from the prefrontal cortex to subcortical areas, either directly by interacting with N-methyl-D-aspartate (NMDA) receptors in the nucleus accumbens, or indirectly by controlling dopamine release from ventral tegmental area neurons...
January 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/27557949/lack-of-association-between-dopaminergic-antagonism-and-negative-symptoms-in-schizophrenia-a-positron-emission-tomography-dopamine-d2-3-receptor-occupancy-study
#20
Gagan Fervaha, Fernando Caravaggio, David C Mamo, Benoit H Mulsant, Bruce G Pollock, Shinichiro Nakajima, Philip Gerretsen, Tarek K Rajji, Wanna Mar, Yusuke Iwata, Eric Plitman, Jun Ku Chung, Gary Remington, Ariel Graff-Guerrero
RATIONALE: Several pre-clinical studies suggest that antipsychotic medications cause secondary negative symptoms. However, direct evidence for a relationship among antipsychotic medications, their direct effects on neurotransmitter systems, and negative symptoms in schizophrenia remains controversial. OBJECTIVE: The objective of this study was to examine the relationship between antipsychotic-related dopamine D2/3 receptor occupancy and negative symptoms in patients with schizophrenia...
October 2016: Psychopharmacology
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