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D2 occupancy

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https://www.readbyqxmd.com/read/29717334/the-role-of-striatal-dopamine-d-2-3-receptors-in-cognitive-performance-in-drug-free-patients-with-schizophrenia
#1
Tanja Veselinović, Ingo Vernaleken, Hildegard Janouschek, Paul Cumming, Michael Paulzen, Felix M Mottaghy, Gerhard Gründer
OBJECTIVE: A considerable body of research links cognitive function to dopaminergic transmission in the prefrontal cortex, but less is known about cognition in relation to striatal dopamine D2/3 receptors in unmedicated patients with psychosis. METHODS: We investigated this association by obtaining PET recordings with the high-affinity D2/3 antagonist ligand [18 F] fallypride in 15 medication-free patients with schizophrenia and 11 healthy controls. On the day of PET scanning, we undertook comprehensive neuropsychological testing and assessment of psychopathology using the Positive and Negative Syndrome Scale (PANSS)...
May 1, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29686254/the-relationship-between-dopamine-receptor-blockade-and-cognitive-performance-in-schizophrenia-a-11-c-raclopride-pet-study-with-aripiprazole
#2
Sangho Shin, Seoyoung Kim, Seongho Seo, Jae Sung Lee, Oliver D Howes, Euitae Kim, Jun Soo Kwon
Aripiprazole's effects on cognitive function in patients with schizophrenia are unclear because of the difficulty in disentangling specific effects on cognitive function from secondary effects due to the improvement in other schizophrenic symptoms. One approach to address this is to use an intermediate biomarker to investigate the relationship between the drug's effect on the brain and change in cognitive function. This study aims to investigate aripiprazole's effect on working memory by determining the correlation between dopamine D2/3 (D2/3) receptor occupancy and working memory of patients with schizophrenia...
April 24, 2018: Translational Psychiatry
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
#3
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...
May 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29458172/modelling-human-myoblasts-survival-upon-xenotransplantation-into-immunodeficient-mouse-muscle
#4
Christophe Praud, Karine Vauchez, Pascal Zongo, Jean-Thomas Vilquin
Cell transplantation has been challenged in several clinical indications of genetic or acquired muscular diseases, but therapeutic success were mitigated. To understand and improve the yields of tissue regeneration, we aimed at modelling the fate of CD56-positive human myoblasts after transplantation. Using immunodeficient severe combined immunodeficiency (SCID) mice as recipients, we assessed the survival, integration and satellite cell niche occupancy of human myoblasts by a triple immunohistochemical labelling of laminin, dystrophin and human lamin A/C...
March 15, 2018: Experimental Cell Research
https://www.readbyqxmd.com/read/29432503/therapeutic-drug-monitoring-of-atypical-antipsychotics
#5
REVIEW
Anna Emilia Urban, Wiesław Jerzy Cubała
The paper presents an overview and analysis of the results of research on therapeutic ranges of concentrations and receptor occupancy, mainly D2 receptors, in the treatment with some atypical antipsychotic drugs. Amisulpride, aripiprazole, clozapine, quetiapine, olanzapine, risperidone, paliperidone, sertindole, and ziprasidone were taken into account. The benefits of therapeutic drug monitoring to optimize the effectiveness of treatment and avoid side effects or toxicity were shown. The safety of patients, with the possibility to use the lowest effective dose, is an undoubted profit of TDM...
December 30, 2017: Psychiatria Polska
https://www.readbyqxmd.com/read/29346639/comparison-of-dopamine-d3-and-d2-receptor-occupancies-by-a-single-dose-of-blonanserin-in-healthy-subjects-a-positron-emission-tomography-study-with-11c-phno
#6
Amane Tateno, Takeshi Sakayori, Woo-Chan Kim, Kazuyoshi Honjo, Haruo Nakayama, Ryosuke Arakawa, Yoshiro Okubo
Background: Blockade of D3 receptor, a member of the dopamine D2-like receptor family, has been suggested as a possible medication for schizophrenia. Blonanserin has high affinity in vitro for D3 as well as D2 receptors. We investigated whether a single dose of 12 mg blonanserin, which was within the daily clinical dose range (i.e., 8-24 mg) for the treatment of schizophrenia, occupies D3 as well as D2 receptors in healthy subjects. Methods: Six healthy males (mean 35...
January 13, 2018: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29334326/predicting-the-dopamine-d-2-receptor-occupancy-of-ropinirole-in-rats-using-positron-emission-tomography-and-pharmacokinetic-pharmacodynamic-modeling
#7
Chenrong Huang, Ziteng Wang, Linsheng Liu, Xiaoxue Liu, Ji Dong, Qingqing Xu, Bin Zhang, Liyan Miao
1. The purpose of this study was to measure dopamine D2/3 receptor occupancy (RO) as a marker of the clinical efficacy of ropinirole in rats via positron emission tomography (PET) using 18 F-fallypride as the radiotracer and to explore the relationship between dopamine RO and the plasma concentration of ropinirole via pharmacokinetic-pharmacodynamic modeling. 2. Plasma was collected from 16 rats treated with one of four doses of ropinirole. For the time-dependent study, the data of 16 rats in the 15 mg/kg dose group at four time points were averaged, and another 24 rats were divided into three dose groups (5 mg/kg, 30 mg/kg and 60 mg/kg) for the dose-dependent study; the animals were assessed via 18 F-fallypride PET scans...
March 14, 2018: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/29229351/evaluation-of-measuring-methods-of-spinal-canal-occupation-rate-in-thoracic-ossification-of-ligamentum-flavum
#8
Sheng-Yuan Zhou, Bo Yuan, Chuang Qian, Xiong-Sheng Chen, Lian-Shun Jia
OBJECTIVE: The degree of hypertrophy of thoracic ossification of ligamentum flavum (TOLF) is related to the severity of the myelopathy. There is no uniform measuring method to calculate the spinal canal occupation ratio (COR) of TOLF simply and effectively. The study was to determine an appropriate measuring method to calculate the COR of TOLF. METHODS: A total of 37 computed tomography cross-sectional imaging scans (bone window) from 22 patients were analyzed retrospectively in this study...
February 2018: World Neurosurgery
https://www.readbyqxmd.com/read/29226628/modeling-of-prolactin-response-following-dopamine-d-2-receptor-antagonists-in-rats-can-it-be-translated-to-clinical-dosing
#9
Amit Taneja, An Vermeulen, Dymphy R H Huntjens, Meindert Danhof, Elizabeth C M De Lange, Johannes H Proost
Prolactin release is a side effect of antipsychotic therapy with dopamine antagonists, observed in rats as well as humans. We examined whether two semimechanistic models could describe prolactin response in rats and subsequently be translated to predict pituitary dopamine D2 receptor occupancy and plasma prolactin concentrations in humans following administration of paliperidone or remoxipride. Data on male Wistar rats receiving single or multiple doses of risperidone, paliperidone, or remoxipride was described by two semimechanistic models, the precursor pool model and the agonist-antagonist interaction model...
December 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29223715/development-of-two-fluorine-18-labeled-pet-radioligands-targeting-pde10a-and-in-vivo-pet-evaluation-in-nonhuman-primates
#10
Vladimir Stepanov, Akihiro Takano, Ryuji Nakao, Nahid Amini, Shotaro Miura, Tomoaki Hasui, Haruhide Kimura, Takahiko Taniguchi, Christer Halldin
INTRODUCTION: Phosphodiesterase 10A (PDE10A) is a member of the PDE enzyme family that degrades cyclic adenosine and guanosine monophosphates (cAMP and cGMP). Based on the successful development of [11 C]T-773 as PDE10A positron emission tomography (PET) radioligand, in this study our aim was to develop and evaluate fluorine-18 analogs of [11 C]T-773. METHODS: [18 F]FM-T-773-d2 and [18 F]FE-T-773-d4 were synthesized from the same precursor used for11 C-labeling of T-773 in a two-step approach via18 F-fluoromethylation and18 F-fluoroethylation, respectively, using corresponding deuterated synthons...
February 2018: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29110353/amotivation-is-associated-with-smaller-ventral-striatum-volumes-in-older-patients-with-schizophrenia
#11
Fernando Caravaggio, Gagan Fervaha, Yusuke Iwata, Eric Plitman, Jun Ku Chung, Shinichiro Nakajima, Wanna Mar, Philip Gerretsen, Julia Kim, M Mallar Chakravarty, Benoit Mulsant, Bruce Pollock, David Mamo, Gary Remington, Ariel Graff-Guerrero
OBJECTIVE: Motivational deficits are prevalent in patients with schizophrenia, persist despite antipsychotic treatment, and predict long-term outcomes. Evidence suggests that patients with greater amotivation have smaller ventral striatum (VS) volumes. We wished to replicate this finding in a sample of older, chronically medicated patients with schizophrenia. Using structural imaging and positron emission tomography, we examined whether amotivation uniquely predicted VS volumes beyond the effects of striatal dopamine D2/3 receptor (D2/3 R) blockade by antipsychotics...
March 2018: International Journal of Geriatric Psychiatry
https://www.readbyqxmd.com/read/29106979/development-of-a-population-pharmacokinetic-model-to-predict-brain-distribution-and-dopamine-d2-receptor-occupancy-of-raclopride-in-non-anesthetized-rat
#12
Yin Cheong Wong, Trayana Ilkova, Rob C van Wijk, Robin Hartman, Elizabeth C M de Lange
BACKGROUND: Raclopride is a selective antagonist of the dopamine D2 receptor. It is one of the most frequently used in vivo D2 tracers (at low doses) for assessing drug-induced receptor occupancy (RO) in animals and humans. It is also commonly used as a pharmacological blocker (at high doses) to occupy the available D2 receptors and antagonize the action of dopamine or drugs on D2 in preclinical studies. The aims of this study were to comprehensively evaluate its pharmacokinetic (PK) profiles in different brain compartments and to establish a PK-RO model that could predict the brain distribution and RO of raclopride in the freely moving rat using a LC-MS based approach...
November 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29016875/occupancy-of-norepinephrine-transporter-by-duloxetine-in-human-brains-measured-by-positron-emission-tomography-with-s-s-18f-fmener-d2
#13
Sho Moriguchi, Harumasa Takano, Yasuyuki Kimura, Tomohisa Nagashima, Keisuke Takahata, Manabu Kubota, Soichiro Kitamura, Tatsuya Ishii, Masanori Ichise, Ming-Rong Zhang, Hitoshi Shimada, Masaru Mimura, Jeffrey H Meyer, Makoto Higuchi, Tetsuya Suhara
Background: The norepinephrine transporter in the brain has been targeted in the treatment of psychiatric disorders. Duloxetine is a serotonin and norepinephrine reuptake inhibitor that has been widely used for the treatment of depression. However, the relationship between dose and plasma concentration of duloxetine and norepinephrine transporter occupancy in the human brain has not been determined. In this study, we examined norepinephrine transporter occupancy by different doses of duloxetine...
December 1, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28858444/a-population-approach-to-guide-amisulpride-dose-adjustments-in-older-patients-with-alzheimer-s-disease
#14
Suzanne Reeves, Julie Bertrand, Emma McLachlan, Fabrizia D'Antonio, Stuart Brownings, Akshay Nair, Suki Greaves, Alan Smith, Joel T Dunn, Paul Marsden, Robert Kessler, Hiroyuki Uchida, David Taylor, Robert Howard
OBJECTIVE: We have previously reported high dopamine D2/3 receptor occupancies at low amisulpride concentrations in older people with Alzheimer's disease (AD), during off-label treatment of AD-related psychosis. This post hoc analysis explored pharmacokinetic (concentration) and pharmacodynamic (prolactin, D2/3 occupancy) contributions to symptom reduction and extrapyramidal side effects (EPS) to inform AD-specific dose adjustments. METHODS: Population pharmacokinetic-pharmacodynamic models were developed by combining pharmacokinetic data from a phase 1 study in 20 healthy older people with pharmacokinetic prolactin, [¹⁸F]fallypride D2/3 receptor imaging, and clinical outcome data from 28 older patients prescribed open amisulpride (25-75 mg/d) to treat AD-related psychosis...
July 2017: Journal of Clinical Psychiatry
https://www.readbyqxmd.com/read/28839266/neutron-crystallography-of-photoactive-yellow-protein-reveals-unusual-protonation-state-of-arg52-in-the-crystal
#15
Kento Yonezawa, Nobutaka Shimizu, Kazuo Kurihara, Yoichi Yamazaki, Hironari Kamikubo, Mikio Kataoka
Because of its high pKa, arginine (Arg) is believed to be protonated even in the hydrophobic environment of the protein interior. However, our neutron crystallographic structure of photoactive yellow protein, a light sensor, demonstrated that Arg52 adopts an electrically neutral form. We also showed that the hydrogen bond between the chromophore and Glu46 is a so-called low barrier hydrogen bond (LBHB). Because both the neutral Arg and LBHB are unusual in proteins, these observations remain controversial. To validate our findings, we carried out neutron crystallographic analysis of the E46Q mutant of PYP...
August 24, 2017: Scientific Reports
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
#16
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-pr-3-mgni-14-d-x-studied-by-in-situ-neutron-diffraction
#17
Kenji Iwase, Kazuhiro Mori, Naoyoshi Terashita, Suguru Tashiro, Tetsuya Suzuki
The crystal structure of Pr3 MgNi14 D18 was determined by neutron diffraction. The determined structure of Pr3 MgNi14 D18 consisted of 89.0% Gd2 Co7 -type structure and 11.0% PuNi3 -type structure. The lattice parameters of a and c of Gd2 Co7 -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 Pr2 Ni4 octahedral sites of the CaCu5 -type cell was the largest (0.75) when compared with the other deuterium sites (<0...
June 19, 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
#18
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
#19
Erin W Tuplin, Matthew R Holahan
BACKGROUND: 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-HT2A 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...
November 14, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28395348/exposure-assessment-in-a-single-walled-carbon-nanotube-primary-manufacturer
#20
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
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