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Journal of Pharmacological and Toxicological Methods

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https://www.readbyqxmd.com/read/28818556/receptor-binding-kinetics-equations-derivation-using-the-laplace-transform-method
#1
Sam R J Hoare
INTRODUCTION: Measuring unlabeled ligand receptor binding kinetics is valuable in optimizing and understanding drug action. Unfortunately, deriving equations for estimating kinetic parameters is challenging because it involves calculus; integration can be a frustrating barrier to the pharmacologist seeking to measure simple rate parameters. Here, a well-known tool for simplifying the derivation, the Laplace transform, is applied to models of receptor-ligand interaction. The method transforms differential equations to a form in which simple algebra can be applied to solve for the variable of interest, for example the concentration of ligand-bound receptor...
August 14, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28807796/high-content-image-analysis-hcia-assay-has-the-highest-correlation-with-direct-counting-cell-suspension-compared-to-the-atp-wst-8-and-alamar-blue-assays-for-measurement-of-cytotoxicity
#2
Haruna Tahara, Shun Matsuda, Yusuke Yamamoto, Hiroe Yoshizawa, Masaharu Fujita, Yasuhiro Katsuoka, Toshihiko Kasahara
INTRODUCTION: Various cytotoxicity assays measuring indicators such as enzyme activity, dye uptake, or cellular ATP content are often performed using 96-well microplates. However, recent reports show that cytotoxicity assays such as the ATP assay and MTS assay underestimate cytotoxicity when compounds such as anti-cancer drugs or mutagens induce cell hypertrophy whilst increasing intracellular ATP content. Therefore, we attempted to evaluate the reliability of a high-content image analysis (HCIA) assay to count cell number in a 96-well microplate automatically without using a cell-number indicator...
August 12, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28797764/inflammatory-pain-assessment-in-the-arthritis-of-the-temporomandibular-joint-in-rats-a-comparison-between-two-phlogistic-agents
#3
Joana Cláudia Bezerra de Araújo, Delane Viana Gondim, André Luiz Cunha Cavalcante, Mario Roberto Pontes Lisboa, Gerly Anne de Castro Brito, Mariana Lima Vale
Temporomandibular joint (TMJ) disorders are a group of conditions that result in TMJ pain, which frequently limits basic daily activities. Experimental models that allow the study of the mechanisms underlying these inflammatory and pain conditions are of great clinical relevance. The aim of this study was to evaluate nociception, inflammation and participation of the macrophage/microglia cells in the arthritis of the TMJ induced by two phlogistic agents. 84 rats were divided into 2 groups: Zy, which received zymosan intra-articularly, or Cg, which received carrageenan intra-articularly...
August 8, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28797763/the-safety-pharmacology-society-salary-survey
#4
Michael K Pugsley, Simon Authier, Tiffini Brabham, Maxim Soloviev, Carrie G Markgraf, Krystle Correll, Martin Traebert, Andrea Greiter-Wilke, Jean-Pierre Valentin, Hugo Vargas, Alfred Botchway, Derek J Leishman, Michael J Curtis
INTRODUCTION: Safety pharmacology is a growing discipline with scientists broadly distributed across international geographical regions. This electronic salary survey is the first to be distributed amongst the entire Safety Pharmacology Society (SPS) membership. An electronic survey was sent to all members of the Society. Categorical survey questions assessed membership employment types, annual incomes, and professional certifications, along with other associated career attributes. METHODS: This survey was distributed to the SPS membership that is comprised of safety pharmacologists, toxicologists and pharmacologists working globally in the pharmaceutical industry, at contract research organizations (CRO), regulatory agencies, and academia or within the technology provider industry...
August 7, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28780373/provision-of-food-and-water-in-rodent-whole-body-plethysmography-safety-pharmacology-respiratory-studies-impact-on-animal-welfare-and-data-quality
#5
Claire Grant, Louise Marks, Helen Prior
INTRODUCTION: We evaluated the feasibility of providing food and water to rodents during whole body plethysmography (WBP) studies as a welfare improvement to standard conditions. METHODS: Male Han Wistar rats or CD1 mice (n=8) were placed in WBP chambers and respiratory parameters recorded for approximately 6h on four separate occasions. On each occasion the animals were exposed to a different plethysmography chamber environment using a randomised design: no food/water (the standard conditions), water bottle, hydrating gel and wet food...
August 2, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28716665/applying-label-free-dynamic-mass-redistribution-assay-for-studying-endogenous-fpr1-receptor-signalling-in-human-neutrophils
#6
Hanna B Christensen, David E Gloriam, Daniel Sejer Pedersen, Jack B Cowland, Niels Borregaard, Hans Bräuner-Osborne
INTRODUCTION: The label-free dynamic mass redistribution-based assay (DMR) is a powerful method for studying signalling pathways of G protein-coupled receptors (GPCRs). Herein we present the label-free DMR assay as a robust readout for pharmacological characterization of formyl peptide receptors (FPRs) in human neutrophils. METHODS: Neutrophils were isolated from fresh human blood and their responses to FPR1 and FPR2 agonists, i.e. compound 43, fMLF and WKYMVm were measured in a label-free DMR assay using Epic Benchtop System from Corning®...
July 15, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28712933/measuring-drug-absorption-improves-interpretation-of-behavioral-responses-in-a-larval-zebrafish-locomotor-assay-for-predicting-seizure-liability
#7
Steven Cassar, Laura Breidenbach, Amanda Olson, Xin Huang, Heather Britton, Clarissa Woody, Pankajkumar Sancheti, DeAnne Stolarik, Karsten Wicke, Katja Hempel, Bruce LeRoy
INTRODUCTION: Unanticipated effects on the central nervous system are a concern during new drug development. A larval zebrafish locomotor assay can reveal seizure liability of experimental molecules before testing in mammals. Relative absorption of compounds by larvae is lacking in prior reports of such assays; having those data may be valuable for interpreting seizure liability assay performance. METHODS: Twenty-eight reference drugs were tested at multiple dose levels in fish water and analyzed by a blinded investigator...
July 13, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28688881/the-abdominal-skin-of-female-sprague-dawley-rats-is-more-sensitive-than-the-back-skin-to-drug-induced-phototoxicity
#8
Kazuhiro Kuga, Hironobu Yasuno, Yumi Sakai, Yumiko Harada, Fumi Shimizu, Yumiko Miyamoto, Yuki Takamatsu, Makoto Miyamoto, Keiichiro Sato
In vivo phototoxicity studies are important to predict drug-induced phototoxicity in humans; however, a standard methodology has not established. To determine differences in sensitivity to drug-induced phototoxicity among various skin sites, we evaluated phototoxic reactions in the back and abdominal skin of female Sprague-Dawley rats orally dosed with phototoxic drugs (pirfenidone, 8-methoxysoraren, doxycycline, and lomefloxacin) or a non-phototoxic drug (gatifloxacin) followed by solar-simulated light irradiation comprising 18J/cm(2) ultraviolet A...
July 5, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28658603/physiological-approaches-to-assess-diminished-sympathetic-activity-in-the-conscious-rat
#9
Matthew R Zahner, Chang-Ning Liu, Vincent Bernardo, Carrie Northcott, Cheryl Tyszkiewicz, Carlin Okerberg, Magalie Boucher, Ingrid Pardo, Chris J Somps
The purpose of this study was to evaluate functional measures of diminished sympathetic activity after postganglionic neuronal loss in the conscious rat. To produce variable degrees of sympathetic postganglionic neuronal loss, adult rats were treated daily with toxic doses of guanethidine (100mg/kg) for either 5days or 11days, followed by a recovery period of at least 18days. Heart rate, blood pressure, cardiac baroreflex responsiveness, urinalysis (for catecholamine metabolite, 3-methoxy-4-hydroxyphenylethylenglycol; MHPG), and pupillometry were performed during the recovery period...
June 27, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28642085/comparison-of-glutathione-levels-measured-using-optimized-monochlorobimane-assay-with-those-from-ortho-phthalaldehyde-assay-in-intact-cells
#10
Jan Čapek, Martina Hauschke, Lenka Brůčková, Tomáš Roušar
Fluorometric glutathione assays have been generally preferred for their high specificity and sensitivity. An additional advantage offered by fluorescent bimane dyes is their ability to penetrate inside the cell. Their ability to react with glutathione within intact cells is frequently useful in flow cytometry and microscopy. Hence, the aims of our study were to use monochlorobimane for optimizing a spectrofluorometric glutathione assay in cells and then to compare that assay with the frequently used ortho-phthalaldehyde assay...
June 19, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28552278/assessments-of-the-qt-qrs-restitution-in-perfused-guinea-pig-heart-can-discriminate-safe-and-arrhythmogenic-drugs
#11
Oleg E Osadchii
INTRODUCTION: Drug-induced arrhythmia remains a matter of serious clinical concern, partly due to low prognostic value of currently available arrhythmic biomarkers. METHODS: This study examined whether arrhythmogenic risks can be predicted through assessments of the rate adaptation of QT interval, ventricular effective refractory period (ERP), or the QT/QRS ratio, in perfused guinea-pig hearts. RESULTS: When the maximum restitution slope was taken as a metric of proarrhythmia, neither QT interval nor ERP measurements at progressively increased pacing rates were found to fully discriminate arrhythmogenic drugs (dofetilide, quinidine, flecainide, and procainamide) from those recognized as safe antiarrhythmics (lidocaine and mexiletine)...
May 24, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28552277/the-determination-of-hepatic-glutathione-at-tissue-and-subcellular-level
#12
Tamás Lőrincz, András Szarka
INTRODUCTION: Glutathione (GSH) through its important function in the antioxidant protection of cells and in the conjugation of drugs and xenobiotics has crucial importance in pharmacology and toxicology. Since GSH is most often measured in liver tissue and different cell organelles it is important to choose the method that best suits for the determination of GSH. METHODS: The GSH content of cell organelles isolated from control and BSO-treated liver tissues was determined by the GSH-NEM-HPLC-UV, monochlorobimane-GSH-HPLC-fluorescence method and DTNB-GSH recycling assay to find the most suitable method for GSH determination from cell organelles...
May 24, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28549786/action-potential-based-mea-platform-for-in-vitro-screening-of-drug-induced-cardiotoxicity-using-human-ipscs-and-rat-neonatal-myocytes
#13
Danny Jans, Geert Callewaert, Olga Krylychkina, Luis Hoffman, Francesco Gullo, Dimiter Prodanov, Dries Braeken
Drug-induced cardiotoxicity poses a negative impact on public health and drug development. Cardiac safety pharmacology issues urged for the preclinical assessment of drug-induced ventricular arrhythmia leading to the design of several in vitro electrophysiological screening assays. In general, patch clamp systems allow for intracellular recordings, while multi-electrode array (MEA) technology detect extracellular activity. Here, we demonstrate a complementary metal oxide semiconductor (CMOS)-based MEA system as a reliable platform for non-invasive, long-term intracellular recording of cardiac action potentials at high resolution...
May 23, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28522142/integration-and-validation-of-the-ex-vivo-human-placenta-perfusion-model
#14
Sigrid Conings, Frédéric Amant, Pieter Annaert, Kristel Van Calsteren
INTRODUCTION: The ex vivo human placenta perfusion model is an effective and non-invasive method to study transplacental passage of drugs and environmental compounds in humans. Due to many challenges and its high complexity it remains difficult to incorporate it routinely into laboratories. METHODS: This article describes a step-by-step protocol for the implementation and validation of a closed-closed ex vivo perfusion model. Antipyrine, a small molecule that passes the placental barrier by passive diffusion, was used as a measurement of overlap between foetal and maternal circulation...
May 15, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28501647/application-of-optical-action-potentials-in-human-induced-pluripotent-stem-cells-derived-cardiomyocytes-to-predict-drug-induced-cardiac-arrhythmias
#15
H R Lu, M P Hortigon-Vinagre, V Zamora, I Kopljar, A De Bondt, D J Gallacher, G Smith
INTRODUCTION: Human induced pluripotent stem cell-derived cardiomyocytes (hiPS-CMs) are emerging as new and human-relevant source in vitro model for cardiac safety assessment that allow us to investigate a set of 20 reference drugs for predicting cardiac arrhythmogenic liability using optical action potential (oAP) assay. METHODS: Here, we describe our examination of the oAP measurement using a voltage sensitive dye (Di-4-ANEPPS) to predict adverse compound effects using hiPS-CMs and 20 cardioactive reference compounds...
May 10, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28476566/qsar-model-for-blood-brain-barrier-permeation
#16
Andrey A Toropov, Alla P Toropova, Marten Beeg, Marco Gobbi, Mario Salmona
BACKGROUND AND OBJECTIVE: Predicting blood-brain barrier permeability for novel compounds is an important goal for neurotherapeutics-focused drug discovery. It is impossible to determine experimentally the blood-brain barrier partitioning of all possible candidates. Consequently, alternative evaluation methods based on computational models are desirable or even necessary. The CORAL software (http://www.insilico.eu/coral) has been checked up as a tool to build up quantitative structure - activity relationships for blood-brain barrier permeation...
May 2, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28476565/a-simple-short-term-method-to-study-thyroid-disruption-using-a-fetal-rat-thyroid-culture
#17
Pablo Olivares-Trigo, Camilo Fuentes Peña, María Fernanda Cavieres
INTRODUCTION: Thyroid modulation activity has not been investigated for many chemical substances. Due to ethical, practical and financial reasons, in vivo evaluation of a large number of compounds is not feasible. It has been proposed that an in vitro mechanism-based strategy could be more adequate for the identification of thyroid hormone disrupting chemicals. Here we describe a simple and mostly inexpensive, short term culture assay to study thyroid disruption. METHODS: Fetal thyroids collected from gestation day 20...
May 2, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28216425/repeated-day-1-fob-testing-in-ich-s7a-safety-assessment-protocols-the-influence-of-within-and-between-session-learning
#18
REVIEW
David V Gauvin, Zachary J Zimmermann, Jill A Dalton, Theodore J Baird
A large number of CNS safety assessment studies using the standard Functional Observational Battery (FOB) are conducted each year at Contract Research Organizations throughout the globe. Study design characteristics are as varied as the Sponsors for whom they are contracted. Gender inclusion, sample sizes, and timing of the FOBs are generally negotiated during protocol development. The ICH S7A guidelines describe a dose-effect study design for CNS safety assessment to be conducted prior to the first dose administration in man...
May 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28167230/adaptation-to-a-blood-pressure-telemetry-system-revealed-by-measures-of-activity-agility-and-operant-learning-in-mice
#19
Anfisa Popova, Darya Tsvirkun, Oleg Dolgov, Konstantin Anokhin, Jeffrey Alberts, Evgeniia Lagereva, Marc-Antoine Custaud, Guillemette Gauquelin-Koch, Olga Vinogradova, Alexander Andreev-Andrievskiy
INTRODUCTION: Implantable telemetry enables continuous monitoring of physiological functions in freely moving animals and can greatly complement pharmacological research. Despite its miniaturization, a sensor/transmitter constitutes 5% or more of a mouse's bodyweight. The aim of the present study was to evaluate whether factors related to the presence of a probe/transmitter influence the ambulatory activity, strength, agility, or operant, motivated behaviors of this small rodent. METHODS: Adult male mice (C57BL/6N, 22-25g, 9-10weeks; implanted n=26, intact n=45) were evaluated during week-long tests, conducted three and eight weeks after surgical implantation of the PA-C10 blood pressure probe...
May 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28167229/population-pharmacokinetics-model-of-thc-used-by-pulmonary-route-in-occasional-cannabis-smokers
#20
A Marsot, C Audebert, L Attolini, B Lacarelle, J Micallef, O Blin
Cannabis is the most widely used illegal drug in the world. Delta-9-tetrahydrocannabinol (THC) is the main source of the pharmacological effect. Some studies have been carried out and showed significant variability in the described models as the values of the estimated pharmacokinetic parameters. The objective of this study was to develop a population pharmacokinetic model for THC in occasional cannabis smokers. Twelve male volunteers (age: 20-28years, body weight: 62.5-91.0kg), tobacco (3-8 cigarette per day) and cannabis occasional smokers were recruited from the local community...
May 2017: Journal of Pharmacological and Toxicological Methods
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