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https://www.readbyqxmd.com/read/29458223/what-does-antidepressant-drug-level-monitoring-reveal-about-outpatient-treatment-and-patient-adherence
#1
Petr Silhan, Romana Urinovska, Ivana Kacirova, Martin Hyza, Milan Grundmann, Eva Ceskova
INTRODUCTION: The evaluation of plasma levels of antidepressants may improve the treatment outcome. The aim was to verify adherence and adequacy of administered doses of antidepressants among patients hospitalized for inadequate outpatient therapeutic response. METHODS: Selective serotonin reuptake inhibitors or venlafaxine plasma levels were assessed on the first day of hospitalization and after 3 days of controlled administration. The patients were considered adherent if the plasma level on admission was within the interval of the minimum and maximum plasma level on the fourth day, expanded by 30%...
February 19, 2018: Pharmacopsychiatry
https://www.readbyqxmd.com/read/29457876/pharmacokinetics-of-metformin-in-patients-with-gastrointestinal-intolerance
#2
L McCreight, T B Stage, P Connelly, M Lonergan, F Nielsen, C Prehn, J Adamski, K Brosen, E R Pearson
AIMS: Metformin intolerance symptoms are gastrointestinal in nature, but the underlying mechanism is poorly understood. The aim of this study was to assess potential causes of metformin intolerance including: altered metformin uptake from the intestine; increased anaerobic glucose utilisation and subsequent lactate production; altered serotonin uptake; and altered bile acid pool. METHODS: This pharmacokinetic study recruited ten severely intolerant and ten tolerant individuals matched for age, sex and BMI...
February 19, 2018: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/29457871/a-qtl-on-chromosome-1-modulates-inter-male-aggression-in-mice
#3
Anna Delprato, Brice Bonheur, Marie-Paule Algéo, Alba Murillo, Esha Dhawan, Lu Lu, Robert W Williams, Wim E Crusio
Aggression between male conspecifics is a complex social behavior that is likely modulated by multiple gene variants. In this study the BXD recombinant inbred mouse strains (RIS) were used to map quantitative trait loci (QTLs) underlying behaviors associated with intermale aggression. Four hundred and fifty-seven males from 55 strains (including the parentals) were observed at an age of 13 +/- 1 week in a resident-intruder test following 10 days of isolation. Attack latency was measured directly within a 10 minute time period and the test was repeated 24 hours later...
February 19, 2018: Genes, Brain, and Behavior
https://www.readbyqxmd.com/read/29456827/impairment-of-social-behaviors-in-arhgef10-knockout-mice
#4
Dai-Hua Lu, Hsiao-Mei Liao, Chia-Hsiang Chen, Huang-Ju Tu, Houng-Chi Liou, Susan Shur-Fen Gau, Wen-Mei Fu
Background: Impaired social interaction is one of the essential features of autism spectrum disorder (ASD). Our previous copy number variation (CNV) study discovered a novel deleted region associated with ASD. One of the genes included in the deleted region is ARHGEF10 . A missense mutation of ARHGEF10 has been reported to be one of the contributing factors in several diseases of the central nervous system. However, the relationship between the loss of ARHGEF10 and the clinical symptoms of ASD is unclear...
2018: Molecular Autism
https://www.readbyqxmd.com/read/29456406/health-related-quality-of-life-anxiety-depression-and-impulsivity-in-patients-with-advanced-gastroenteropancreatic-neuroendocrine-tumours
#5
Alexandra R Lewis, Xin Wang, Laurice Magdalani, Paolo D'Arienzo, Colsom Bashir, Was Mansoor, Richard Hubner, Juan W Valle, Mairéad G McNamara
AIM: To compare health-related quality of life (HRQoL), anxiety, depression, and impulsivity scores in patients with and without carcinoid syndrome (CS), and correlated them with serum 5-hydroxyindoleacetic acid (5-HIAA) levels. METHODS: Patients with advanced gastroenteropancreatic neuroendocrine tumours (GEPNET), with and without CS completed HRQoL QLQ-C30 and QLQ-GI.NET21, Hospital Anxiety and Depression Scale (HADS) and Barratt Impulsivity Scale (BIS) questionnaires...
February 14, 2018: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/29456112/discovery-of-dsp-1053-a-novel-benzylpiperidine-derivative-with-potent-serotonin-transporter-inhibitory-activity-and-partial-5-ht-1a-receptor-agonistic-activity
#6
Hidefumi Yoshinaga, Tomoaki Nishida, Izumi Sasaki, Taro Kato, Hitomi Oki, Kazuki Yabuuchi, Tomohiro Toyoda
We have previously shown that SMP-304, a serotonin uptake inhibitor with weak 5-HT1A partial agonistic activity, may act under high serotonin levels as a 5-HT1A antagonist that improves the onset of paroxetine in the rat swimming test. However, SMP-304 is mostly metabolized by CYP2D6, indicating limited efficacy among individuals and increased side effects. To reduce CYP2D6 metabolic contribution and enhance SERT/5-HT1A binding affinity, we carried out a series of substitutions at the bromine atom in the left part of the benzene ring of SMP-304 and replaced the right part of SMP-304 with a chroman-4-one...
February 8, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29454752/effects-of-5-ht-2-receptor-antagonists-on-bronchoconstriction-and-pulmonary-remodeling-processes
#7
Anna Löfdahl, Christina Wenglén, Kristina Rydell-Törmänen, Gunilla Westergren-Thorsson, Anna-Karin Larsson-Callerfelt
Serotonin (5-hydroxytryptamine, 5-HT) is associated with several chronic pulmonary diseases, recognizing 5-HT2 receptor antagonists as potential inhibitors of tissue remodeling. However, the effects of 5-HT2 receptors, especially, 5-HT2B receptors on airway function and remodeling, are unclear. We investigated the role of 5-HT2B receptors on airway smooth muscle contractility and remodeling processes. Murine precision-cut lung slices were pre-treated with 5-HT2B receptor antagonists; EXT5, EXT9, RS127445, and PRX08066, as well as ketanserin (5-HT2A/2C receptor antagonist) (1 μM, 10 μM), prior to addition of cumulative concentrations of 5-HT to induce bronchoconstriction...
February 15, 2018: American Journal of Pathology
https://www.readbyqxmd.com/read/29453947/evaluation-of-the-effects-of-rp5063-a-novel-multimodal-serotonin-receptor-modulator-as-single-agent-therapy-and-co-administrated-with-sildenafil-bosentan-and-treprostinil-in-a-monocrotaline-induced-pulmonary-arterial-hypertension-rat-model
#8
Laxminarayan Bhat, Jon Hawkinson, Marc Cantillon, Dasharatha G Reddy, Seema R Bhat, Charles-E Laurent, Annie Bouchard, Marzena Biernat, Dany Salvail
Pulmonary arterial hypertension (PAH), a condition that is defined by pulmonary vasculature constriction and remodeling, involves dysfunctional signaling of the serotonin (5-HT) receptors, 5-HT 2/2B/7 . In a rat model of monocrotaline (MCT)-induced PAH, the effectiveness of RP5063 (RP), a dopamine and 5-HT receptor modulator, was evaluated as monotherapy and as an adjunct to standard PAH treatments. After a single 60mg/kg dose of MCT, rats received vehicle (MCT+Veh; gavage twice-daily [b.i.d.]), RP (10mg/kg; gavage b...
February 14, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29453804/probiotics-affect-one-carbon-metabolites-and-catecholamines-in-a-genetic-rat-model-of-depression
#9
Sandra Tillmann, Hussain M Awwad, Amanda R Eskelund, Giulia Treccani, Juergen Geisel, Gregers Wegener, Rima Obeid
SCOPE: Probiotics may influence one-carbon (C1) metabolism, neurotransmitters, liver function markers, or behavior. METHODS AND RESULTS: Male adult Flinders Sensitive Line rats (model of depression, FSL; n = 22) received Lactobacillus helveticus R0052 and Bifidobacterium longum R0175 (10 9 or 10 10 colony-forming units/d) or vehicle for 10 weeks. The controls, Flinders Resistant Line rats (FRL, n = 8), only received vehicle. C1-related metabolites were measured in plasma, urine, and different tissues...
February 17, 2018: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/29453444/positive-regulation-of-raphe-serotonin-neurons-by-serotonin-2b-receptors
#10
Arnauld Belmer, Emily Quentin, Silvina L Diaz, Bruno P Guiard, Sebastian P Fernandez, Stéphane Doly, Sophie M Banas, Pothitos M Pitychoutis, Imane Moutkine, Aude Muzerelle, Anna Tchenio, Anne Roumier, Manuel Mameli, Luc Maroteaux
Serotonin is a neurotransmitter involved in many psychiatric diseases. In humans, a lack of 5-HT 2B receptors is associated with serotonin-dependent phenotypes, including impulsivity and suicidality. A lack of 5-HT 2B receptors in mice eliminates the effects of molecules that directly target serotonergic neurons including amphetamine derivative serotonin releasers, and selective serotonin reuptake inhibitor antidepressants. In this work, we tested the hypothesis that 5-HT 2B receptors directly and positively regulate raphe serotonin neuron activity...
February 5, 2018: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29451954/novel-5-ht7-antagonists-with-an-unprecedented-selectivity-profile
#11
Ali Ates, Pierre Burssens, Olivier Lorthioir, Patrick Lo Brutto, Gwenael Dehon, Jean Keyaerts, Francis Coloretti, Lallemand Bénédicte, Verbois Valérie, Gillard Michel, Vermeiren Céline
In the present study, a novel chemical series of serotonin 5-HT7 antagonist is described. The synthesis, structure-activity relationships and selectivity profile are reported. This series includes 5-HT7 antagonists with unprecedented good selectivity for 5-HT7 receptor.
February 16, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29451703/mechanisms-of-imidazoline-i-2-receptor-agonist-induced-antinociception-in-rats-involvement-of-monoaminergic-neurotransmission
#12
Justin N Siemian, Kaixuan Wang, Yanan Zhang, Jun-Xu Li
BACKGROUND AND PURPOSE: Although studies have established the antinociceptive efficacies of imidazoline I2 receptor (I2 R) agonists, its exact post-receptor mechanism remains unknown. This study tested the hypothesis that monoaminergic transmission is critical for I2 R agonist-induced antinociception. EXPERIMENTAL APPROACH: The von Frey filament test was used to examine the antinociceptive effects of the I2 R agonists 2-BFI and CR4056 on chronic constriction injury (CCI)-induced neuropathic pain or complete Freund's adjuvant (CFA)-induced inflammatory pain in rats...
February 16, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29451362/simultaneous-multiple-ms-binding-assays-for-the-dopamine-norepinephrine-and-serotonin-transporters
#13
Patrick Neiens, Angela De Simone, Georg Höfner, Klaus T Wanner
In this work, we present label-free, mass-spectrometry-based binding assays (MS Binding Assays), targeting the human dopamine, norepinephrine, and serotonin transporters (hDAT, hNET, and hSERT) in simultaneous binding experiments. Using a validated LC-ESI-MS/MS method for quantification of the selective dopamine transporter inhibitor (R,R)-4-(2-benzhydryloxyethyl)-1-(4-fluorobenzyl)piperidin-3-ol ((R,R)-D-84), the selective norepinephrine transporter inhibitor (S,S)-reboxetine, and the selective serotonin reuptake inhibitor (S)-citalopram, binding affinities at the three monoamine transporters could be characterized simultaneously in a single binding experiment...
February 16, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29451321/predicting-recovery-in-acute-post-stroke-aphasia
#14
Argye E Hillis, Yuan Ye Beh, Rajani Sebastian, Bonnie Breining, Donna C Tippett, Amy Wright, Sadhvi Saxena, Chris Rorden, Leonardo Bonilha, Alexandra Basilakos, Grigori Yourganov, Julius Fridriksson
OBJECTIVE: Many stroke patients show remarkable recovery of language after initial severe impairment, but it is difficult to predict which patients will show good recovery. We aimed to identify patient and lesion characteristics that together predict the best naming outcome in four studies. METHODS: We report two longitudinal studies that identified two variables at onset that were strongly associated with good recovery of naming (the most common residual deficit in aphasia) in the first six months after stroke: damage to left posterior superior temporal gyrus (pSTG) and/or superior longitudinal fasciculus/arcuate fasciculus (SLF/AF) and selective serotonin reuptake inhibitor (SSRI) use...
February 16, 2018: Annals of Neurology
https://www.readbyqxmd.com/read/29451186/-lactobacillus-acidophilus-and-bifidobacterium-longum-supernatants-upregulate-the-serotonin-transporter-expression-in-intestinal-epithelial-cells
#15
Ya-Nan Cao, Li-Juan Feng, Bang-Mao Wang, Kui Jiang, Shu Li, Xin Xu, Wei-Qiang Wang, Jing-Wen Zhao, Yu-Ming Wang
Background/Aims: Probiotics play a role in relieving irritable bowel syndrome (IBS); however, the underlying mechanism is yet unclear. The aim of the study was to investigate the effects of the supernatants of Lactobacillus acidophilus and Bifidobacterium longum on the expression of serotonin transporter (SERT) messenger ribonucleic acid (mRNA) and protein. Materials and Methods: HT-29 and Caco-2 cells were treated with different concentrations of L. acidophilus and B...
January 2018: Saudi Journal of Gastroenterology: Official Journal of the Saudi Gastroenterology Association
https://www.readbyqxmd.com/read/29451034/cytochrome-p450-in-the-central-nervous-system-as-a-therapeutic-target-in-neurodegenerative-diseases
#16
Cynthia Navarro-Mabarak, Rafael Camacho-Carranza, Jesús Javier Espinosa-Aguirre
Cytochromes P450 (CYPs) constitute a family of enzymes that can be found in the endoplasmic reticulum (ER), mitochondria or the cell surface of the cells. CYPs are characterized by carrying out the oxidation of organic compounds and they are mainly recognized as mediators of the biotransformation of xenobiotics to polar hydrophilic metabolites that can be eliminated from the organism. However, these enzymes play a key role in many other physiological processes, being involved in diverse indispensable metabolic pathways since they metabolize many endogenous substrates...
February 16, 2018: Drug Metabolism Reviews
https://www.readbyqxmd.com/read/29451001/parallel-artificial-liquid-membrane-extraction-of-psychoactive-analytes-a-novel-approach-in-therapeutic-drug-monitoring
#17
Katharina Norgren Olsen, Kristine Skoglund Ask, Stig Pedersen-Bjergaard, Astrid Gjelstad
AIM: Liquid-liquid extraction is widely used in therapeutic drug monitoring of antipsychotics, but difficulties in automation of the technique can result in long operational time. In this paper, parallel artificial liquid membrane extraction was used for extraction of serotonin- and serotonin-norepinephrine reuptake inhibitors from human plasma, and an approach to automate the technique was investigated. RESULTS: Eight model analytes were extracted from 125 μl human plasma with recoveries in the range 72-111% (relative standard deviation [RSD] ≤12...
February 16, 2018: Bioanalysis
https://www.readbyqxmd.com/read/29448224/a-review-on-electrochemical-detection-of-serotonin-based-on-surface-modified-electrodes
#18
REVIEW
Shikha Sharma, Nidhi Singh, Vartika Tomar, Ramesh Chandra
Serotonin is one of the important neurotransmitters of our body. It's abnormal concentration is associated with multiple disorders and diseases. Sensitive and precise electrochemical determination of serotonin is not possible with bare working electrodes due to various reasons viz. electro-chemical fouling, presence of other biological molecules having similar oxidation potential, and lower concentration of serotonin in biological samples. Surface modification of working electrode is required for fast, precise, selective, and sensitive detection of serotonin...
February 6, 2018: Biosensors & Bioelectronics
https://www.readbyqxmd.com/read/29448118/calcium-channel-blockers-as-drug-repurposing-candidates-for-gestational-diabetes-mining-large-scale-genomic-and-electronic-health-records-data-to-repurpose-medications
#19
Jeffery A Goldstein, Lisa A Bastarache, Joshua C Denny, Dan M Roden, Jill M Pulley, David M Aronoff
New therapeutic approaches are needed for gestational diabetes mellitus (GDM), but must show safety and efficacy in a historically understudied population. We studied associations between electronic medical record (EMR) phenotypes and genetic variants to uncover drugs currently considered safe in pregnancy that could treat or prevent GDM. We identified 129 systemically active drugs considered safe in pregnancy targeting the proteins produced from 196 genes. We tested for associations between GDM and/or type 2 diabetes (DM2) and 306 SNPs in 130 genes represented on the Illumina Infinium Human Exome Bead Chip (DM2 was included due to shared pathophysiological features with GDM)...
February 12, 2018: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/29448091/evidence-and-prospective-of-plant-derived-flavonoids-as-antiplatelet-agents-strong-candidates-to-be-drugs-of-future
#20
Harron Khan, Mohammad Jawad, Mohammad Ajmal Kamal, Alessandra Baldi, Jianbo Xiao, Seyed Mohammad Nabavi, Maria Daglia
Platelets are involved in hemostasis, inflammation, and thrombosis processes. Following a vascular damage, the endothelium releases protein factors, allowing the adhesion of subendothelium to platelets. Then platelets are activated, leading to the secretion of biologically-active ligands including thromboxane A2, adenosine diphosphate and serotonin. Aspirin, clopidogrel and warfarin are the most common drugs used to meet the challenges of platelet aggregation. However, these agents face issues with aspirin resistance and bleeding...
February 12, 2018: Food and Chemical Toxicology
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