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D2 occupancy

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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
#1
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
#2
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...
July 30, 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
#3
Travis T Wager, Thomas A Chappie, David Horton, Ramalakshmi Y Chandrasekaran, Brian M Samas, Elizabeth Dunn-Sims, Cathleen Hsu, Nawshaba Nawreen, Michelle A Vanase-Frawley, Rebecca E O'Connor, Christopher Schmidt, Keith Dlugolenski, Nancy C Stratman, Mark J Majchrzak, Bethany L Kormos, David 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)...
October 7, 2016: 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
#4
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-pharmacoepidemiologic-pharmacodynamic-method-application-to-antipsychotic-induced-movement-disorders
#5
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 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 D2, 5HT2A, and M1 receptor occupancy and the risks of antipsychotic (AP)-induced movement disorders. METHODS: First, we performed a case non-case analysis using spontaneous reports from the World Health Organization (WHO) Global Individual Case Safety Report (ICSR) database, VigiBase®...
September 30, 2016: 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
#6
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
#7
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
#8
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...
September 7, 2016: 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
#9
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
https://www.readbyqxmd.com/read/27549374/brain-imaging-studies-on-the-cognitive-pharmacological-and-neurobiological-effects-of-cannabis-in-humans-evidence-from-studies-of-adult-users
#10
A Weinstein, A Livny-Ezer, A Weizman
Cannabis is the most widely used illicit drug worldwide. Regular cannabis use has been associated with a range of acute and chronic mental health problems, such as anxiety, depression, psychotic symptoms and neurocognitive impairments and their neural mechanisms need to be examined. This review summarizes and critically evaluates brain-imaging studies of cannabis in recreational and regular cannabis users between January 2000 and January 2016. The search has yielded eligible 103 structural and functional studies...
August 22, 2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/27525990/preferential-binding-to-dopamine-d3-over-d2-receptors-by-cariprazine-in-patients-with-schizophrenia-using-pet-with-the-d3-d2-receptor-ligand-11-c-phno
#11
Ragy R Girgis, Mark Slifstein, Deepak D'Souza, Yih Lee, Antonia Periclou, Parviz Ghahramani, István Laszlovszky, Suresh Durgam, Nika Adham, Nabeel Nabulsi, Yiyun Huang, Richard E Carson, Béla Kiss, Margit Kapás, Anissa Abi-Dargham, Ashok Rakhit
RATIONALE: Second-generation antipsychotics occupy dopamine D2 receptors and act as antagonists or partial agonists at these receptors. While these drugs alleviate positive symptoms in patients with schizophrenia, they are less effective for treating cognitive deficits and negative symptoms. Dopamine D3 receptors are highly expressed in areas of the brain thought to play a role in the regulation of motivation and reward-related behavior. Consequently, the dopamine D3 receptor has become a target for treating negative symptoms in combination with D2 antagonism to treat positive symptoms in patients with schizophrenia...
October 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27490263/the-association-of-dopamine-pathway-gene-score-nicotine-dependence-and-smoking-cessation-in-a-rural-male-population-of-shandong-china
#12
Suyun Li, Qiang Wang, Lulu Pan, Huijie Li, Xiaorong Yang, Fan Jiang, Nan Zhang, Mingkui Han, Chongqi Jia
BACKGROUND AND OBJECTIVES: Smoking and smoking cessation are both psychological and physiological traits. We aimed to investigate the interaction between dopamine pathway gene scores and nicotine dependence on smoking cessation in a rural Chinese male population. METHODS: Participants were recruited from 17 villages in Shandong, China. DNA was extracted from blood sample of 819 participants. 25 single nucleotide polymorphisms (SNPs) in 8 dopamine (DA) pathway genes were genotyped...
September 2016: American Journal on Addictions
https://www.readbyqxmd.com/read/27434874/two-binding-geometries-for-risperidone-in-dopamine-d3-re-ceptors-insights-on-the-fast-off-mechanism-through-docking-quantum-biochemistry-and-molecular-dynamics-simulations
#13
Geancarlo Zanatta, Gustavo Della Flora Nunes, Eveline Matias Bezerra, Roner F da Costa, Alice Maria Martins, Ewerton Wagner Santos Caetano, Valder Nogueira Freire, Carmem Gottfried
Risperidone is an atypical antipsychotic used in the treatment of schizophrenia and of symptoms of irritability associated with autism spectrum disorder (ASD). Its main action mechanism is the blockade of D2-like receptors acting over positive and negative symptoms of schizophrenia with small risk of extrapyramidal symptoms (EPS) at doses corresponding to low/moderate D2 occupancy. Such decrease in the side effect incidence can be associated to its fast unbinding from D2 receptors in the nigrostriatal region allowing the recovery of dopamine signaling pathways...
July 19, 2016: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/27408789/occupancy-of-pramipexole-sifrol-at-cerebral-dopamine-d2-3-receptors-in-parkinson-s-disease-patients
#14
Angela Deutschländer, Christian la Fougère, Kai Boetzel, Nathalie L Albert, Franz-Josef Gildehaus, Peter Bartenstein, Guoming Xiong, Paul Cumming
Whereas positron emission tomography (PET) with the antagonist ligand [(18)F]fallypride reveals the composite of dopamine D2 and D3 receptors in brain, treatment of Parkinson's disease (PD) patients with the D3-prefering agonist pramipexole should result in preferential occupancy in the nucleus accumbens, where the D3-subtype is most abundant. To test this prediction we obtained pairs of [(18)F]fallypride PET recordings in a group of nine PD patients, first in a condition of treatment as usual with pramipexole (ON-Sifrol; 3 × 0...
2016: NeuroImage: Clinical
https://www.readbyqxmd.com/read/27395799/a-comparison-of-two-semi-mechanistic-models-for-prolactin-release-and-prediction-of-receptor-occupancy-following-administration-of-dopamine-d2-receptor-antagonists-in-rats
#15
Amit Taneja, An Vermeulen, Dymphy R H Huntjens, Meindert Danhof, Elizabeth C M De Lange, Johannes H Proost
We compared the model performance of two semi-mechanistic pharmacokinetic-pharmacodynamic models, the precursor pool model and the agonist-antagonist interaction model, to describe prolactin response following the administration of the dopamine D2 receptor antagonists risperidone, paliperidone or remoxipride in rats. The time course of pituitary dopamine D2 receptor occupancy was also predicted. Male Wistar rats received a single dose (risperidone, paliperidone, remoxipride) or two consecutive doses (remoxipride)...
October 15, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27371496/risperidone-long-acting-injectable-in-the-treatment-of-treatment-resistant-schizophrenia-with-dopamine-supersensitivity-psychosis-results-of-a-2-year-prospective-study-including-an-additional-1-year-follow-up
#16
Hiroshi Kimura, Nobuhisa Kanahara, Tsuyoshi Sasaki, Naoya Komatsu, Minoru Ishige, Katsumasa Muneoka, Hidetoshi Ino, Kazuyuki Yoshimura, Hiroshi Yamanaka, Tomotaka Suzuki, Hideki Komatsu, Hiroyuki Watanabe, Eiji Shimizu, Masaomi Iyo
UNLABELLED: Dopamine supersensitivity psychosis (DSP) resulting from antipsychotic treatment is related to treatment-resistant schizophrenia (TRS), and its treatment has not been established to date. Maintaining thoroughly stable occupancy of the dopamine D2 receptor by risperidone long-acting injectable (RLAI) is one strategy for treatment. In this study, RLAI was given as an adjunctive medication to oral antipsychotic(s), which were switched partially and gradually to RLAI in 108 treatment-resistant patients for an additional 1-year follow-up in a 2-year study, and to compare the effects in 72 patients with a DSP history (DSP group) and 36 patients without this history (NonDSP group)...
August 2016: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/27343365/current-drug-treatments-targeting-dopamine-d3-receptor
#17
Gian Marco Leggio, Claudio Bucolo, Chiara Bianca Maria Platania, Salvatore Salomone, Filippo Drago
Dopamine receptors (DR) have been extensively studied, but only in recent years they became object of investigation to elucidate the specific role of different subtypes (D1R, D2R, D3R, D4R, D5R) in neural transmission and circuitry. D1-like receptors (D1R and D5R) and D2-like receptors (D2R, D2R and D4R) differ in signal transduction, binding profile, localization in the central nervous system and physiological effects. D3R is involved in a number of pathological conditions, including schizophrenia, Parkinson's disease, addiction, anxiety, depression and glaucoma...
September 2016: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/27207908/olanzapine-treatment-of-adolescent-rats-alters-adult-d2-modulation-of-cortical-inputs-to-the-ventral-striatum
#18
Julie M Brooks, Patricio O'Donnell, Douglas O Frost
BACKGROUND: The striatal dopamine system undergoes vast ontogenetic changes during adolescence, making the brain vulnerable to drug treatments that target this class of neurotransmitters. Atypical antipsychotic drugs are often prescribed to children and adolescents for off-label treatment of neuropsychiatric disorders, yet the long-term impact this treatment has on brain development remains largely unknown. METHODS: Adolescent male rats were treated with olanzapine or vehicle for 3 weeks (during postnatal day 28-49) using a dosing condition designed to approximate closely D2 receptor occupancies in the human therapeutic range...
May 12, 2016: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27199528/psychopharmacological-treatment-for-schizophrenia-less-is-more
#19
Chuanyue Wang
Antipsychotic polypharmacy in the treatment of schizophrenia is more common in China and other Asian countries than in Western countries. The reasons for this are unclear, but it may be related to an unsubstantiated belief among clinicians that multiple medications are more likely to achieve the desired clinical outcome. Antipsychotic medications are the mainstay of treatment for individuals with schizophrenia, but the use of antipsychotic polypharmacy and of high dosages of antipsychotic medication are associated with substantially increased risks without conferring improved clinical outcomes...
December 25, 2015: Shanghai Archives of Psychiatry
https://www.readbyqxmd.com/read/27167902/risperidone-induced-extrapyramidal-side-effects-is-the-need-for-anticholinergics-the-consequence-of-high-plasma-concentrations
#20
Georgios Schoretsanitis, Ekkehard Haen, Christoph Hiemke, Gerhard Gründer, Benedikt Stegmann, Koen R J Schruers, Tanja Veselinovic, Sarah E Lammertz, Michael Paulzen
Antipsychotic drugs can induce various undesirable adverse motor reactions, such as extrapyramidal side effects (EPS). A widely accepted pharmacodynamic mechanism underlying EPS includes an increase in striatal D2-receptor occupancy. However, less is known about the pharmacokinetic background of EPS. The aim of this study was to analyze in-vivo possible pharmacokinetic patterns underlying biperiden-treated EPS in risperidone (RIS)-medicated patients. A large therapeutic drug monitoring database containing plasma concentrations of RIS and its metabolite 9-hydroxyrisperidone (9-OH-RIS) of 2293 adult inpatients and outpatients was analyzed...
September 2016: International Clinical Psychopharmacology
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