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https://www.readbyqxmd.com/read/29786965/l-and-d-threo-ethylphenidate-concentrations-pharmacokinetics-and-pharmacodynamics-in-horses
#1
Heather K Knych, Dan S McKemie, Kelsey Seminoff, Petra Hartmann, Lynn Hovda, Dionne Benson
Ethylphenidate is a psychostimulant and analogue of the commonly prescribed compound, methylphenidate (Ritalin®). There are a limited number of studies describing the disposition and pharmacologic/toxicological effects of ethylphenidate in any species. The abuse potential in equine athletes along with the limited data available regarding administration in horses necessitates further study. The objectives of the current study were to describe drug concentrations, develop an analytical method that could be used to regulate its use and describe the pharmacodynamic effects of ethylphenidate in horses...
May 22, 2018: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29786960/the-atomic-resolution-structure-of-a-class-c-%C3%AE-lactamase-and-of-its-complex-with-avibactam
#2
Stefano Mangani, Cecilia Pozzi, Flavio Di Pisa, Filomena De Luca, Manuela Benvenuti, Jean-Denis Docquier
β-lactamases (BLs) are important antibiotic resistance determinants that significantly compromise the efficacy of valuable β-lactam antibacterial drugs. For that reason, combinations with β-lactamase inhibitor were developed. Avibactam is the first non-β-lactam BL inhibitor introduced in clinical practice. Ceftazidime-avibactam represents one of the few last-resort antibiotics available for the treatment of infections caused by near pandrug-resistant bacteria. TRU-1 is a chromosomally-encoded AmpC-type BL of Aeromonas enteropelogenes, related to the FOX-type BLs and constitutes a good model for class C BLs...
May 22, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29786944/design-synthesis-and-evaluation-of-a-novel-series-of-inhibitors-reversing-p-glycoprotein-mediated-multidrug-resistance
#3
Hesham Ghaleb, Huilan Li, Mutta Kairuki, Qianqian Qiu, Xinzhou Bi, Chunxia Liu, Chen Liao, Jieming Li, Kamal Hezam, Wenlong Huang, Hai Qian
Multidrug resistance (MDR) is still the main barrier to attaining effective results with chemotherapy. Discovery of new chemo-reversal agents is needed to overcome MDR. Our study focused on a better way to obtain novel drugs with triazole rings that have an MDR-reversal ability through click chemistry. Among 20 developed compounds, compound 19 had a minimal cytotoxic effect compared to tariquidar and verapamil (VRP) and showed a higher reversal activity than VRP through increased accumulation in K562/A02 cells...
May 22, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29786873/in-vivo-profiling-of-four-centrally-administered-opioids-for-antinociception-constipation-and-respiratory-depression-between-colony-differences-in-sprague-dawley-rats
#4
A Kuo, M T Smith
Outbred rodent stocks including Sprague Dawley rats, are known for their genetic diversity and so they are often used to develop animal models of human disease. Although between-colony differences in pharmaco-behavioural studies have been published previously, a direct head-to-head comparison study, whereby all research was performed in the same laboratory by the same experimenter utilising the supraspinal route of drug administration in the same strain of rat, is lacking. Herein, we report our head-to-head comparison study, involving assessment of antinociception, constipation and respiratory depression evoked by single bolus intracerebroventricular (ICV) doses of morphine, buprenorphine, DPDPE and U69,593 using male Sprague Dawley rats sourced from a different breeding colony (BC2) from that (BC1) used by us previously...
May 22, 2018: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/29786857/effect-of-oatp1b1-1b3-inhibitor-gdc-0810-on-the-pharmacokinetics-of-pravastatin-and-coproporphyrin-i-iii-in-healthy-female-subjects
#5
Lichuan Liu, Sravanthi Cheeti, Kenta Yoshida, Edna Choo, Eugene Chen, Buyun Chen, Mary Gates, Stina Singel, Roland Morley, Joseph Ware, Srikumar Sahasranaman
Developed as an oral anticancer drug to treat estrogen receptor-positive breast cancer, GDC-0810 was shown to be a potent inhibitor of organic anion-transporting polypeptide 1B1 and 1B3 (OATP1B1/1B3) from an in vitro assay. A clinical study was conducted to assess the drug-drug interaction potential between GDC-0810 and pravastatin, which is a relatively selective and sensitive OATP1B1/1B3 substrate. Fifteen healthy female subjects of non-childbearing potential were enrolled in the study. On day 1 in period 1, a single 10-mg dose of pravastatin was administered to all subjects...
May 22, 2018: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29786853/cysteamine-modified-gold-nanoparticles-as-a-colorimetric-sensor-for-the-rapid-detection-of-gentamicin
#6
Joshua C Gukowsky, Chen Tan, Zexiang Han, Lili He
A simple, rapid, and specific colorimetric method for gentamicin detection using cysteamine-modified gold nanoparticles (cys-AuNPs) has been developed. The maximum residue limits of gentamicin allowed in foods are typically below 100 nM, so an effective detection method for low concentrations of the drug is required. The aggregation of gold nanoparticles (AuNPs) was used as the basis for this method, and adding cysteamine to the AuNPs helped to enhance their aggregative abilities. The cys-AuNPs are capable of detecting gentamicin concentrations as low as 12...
May 22, 2018: Journal of Food Science
https://www.readbyqxmd.com/read/29786852/evolution-of-lobar-abnormalities-of-cerebral-glucose-metabolism-in-41-children-with-drug-resistant-epilepsy
#7
Tuhina Govil-Dalela, Ajay Kumar, Michael E Behen, Harry T Chugani, Csaba Juhász
OBJECTIVE: We analyzed long-term changes of lobar glucose metabolic abnormalities in relation to clinical seizure variables and development in a large group of children with medically refractory epilepsy. METHODS: Forty-one children (25 males) with drug-resistant epilepsy had a baseline positron emission tomography (PET) scan at a median age of 4.7 years; the scans were repeated after a median of 4.3 years. Children with progressive neurological disorders or space-occupying lesion-related epilepsy and those who had undergone epilepsy surgery were excluded...
May 22, 2018: Epilepsia
https://www.readbyqxmd.com/read/29786784/generation-of-prostate-cancer-patient-derived-xenografts-to-investigate-mechanisms-of-novel-treatments-and-treatment-resistance
#8
Hung-Ming Lam, Holly M Nguyen, Eva Corey
Treatment advances lead to survival benefits of patients with advanced prostate cancer. These treatments are highly efficacious in a subset of patients; however, similarly to other cancers, after initial responses the tumors develop resistance (acquired resistance) and the patients succumb to the disease. Furthermore, there is a subset of patients who do not respond to the treatment at all (de novo resistance). Preclinical testing using patient-derived xenografts (PDXs) has led to successful drug development, and PDXs will continue to provide valuable resources to generate clinically relevant data with translational potential...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/29786768/risk-prediction-score-for-hiv-infection-development-and-internal-validation-with-cross-sectional-data-from-men-who-have-sex-with-men-in-china
#9
Lu Yin, Yuejuan Zhao, Meridith Blevins Peratikos, Liang Song, Xiangjun Zhang, Ruolei Xin, Zheya Sun, Yunan Xu, Li Zhang, Yifei Hu, Chun Hao, Yuhua Ruan, Yiming Shao, Sten H Vermund, Han-Zhu Qian
Receptive anal intercourse, multiple partners, condomless sex, sexually transmitted infections (STIs), and drug/alcohol addiction are familiar factors that correlate with increased human immunodeficiency virus (HIV) risk among men who have sex with men (MSM). To improve estimation to HIV acquisition, we created a composite score using questions from routine survey of 3588 MSM in Beijing, China. The HIV prevalence was 13.4%. A risk scoring tool using penalized maximum likelihood multivariable logistic regression modeling was developed, deploying backward step-down variable selection to obtain a reduced-form model...
May 21, 2018: AIDS and Behavior
https://www.readbyqxmd.com/read/29786662/study-on-the-discrimination-between-citri-reticulatae-pericarpium-varieties-based-on-hs-spme-gc-ms-combined-with-multivariate-statistical-analyses
#10
Yuying Zheng, Xuan Zeng, Wei Peng, Zhong Wu, Weiwei Su
Citri reticulatae pericarpium (CRP), the dried pericarps of Citrus reticulata Blanco and its cultivars, has been widely used in drugs and foods in China for centuries. In this study, an accurate and feasible analytical method based on HS-SPME-GC-MS coupled with multivariate statistical analyses was developed to comprehensively compare volatile compounds of pericarps derived from Citrus reticulata "Chachi" ("Guangchenpi" in Chinese, GCP) and other cultivars of Citrus reticulata Blanco ("Chenpi" in Chinese, CP)...
May 22, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29786660/molecular-targets-of-active-anticancer-compounds-derived-from-marine-sources
#11
REVIEW
Xiaoping Song, Ying Xiong, Xin Qi, Wei Tang, Jiajia Dai, Qianqun Gu, Jing Li
Over the past decades, a number of novel compounds, which are produced in the marine environment, have been found to exhibit the anticancer effects. This review focuses on molecular targets of marine-derived anticancer candidates in clinical and preclinical studies. They are kinases, transcription factors, histone deacetylase, the ubiquitin-proteasome system, and so on. Specific emphasis of this review paper is to provide information on the optimization of new target compounds for future research and development of anticancer drugs, based on the identification of structures of these target molecules and parallel compounds...
May 22, 2018: Marine Drugs
https://www.readbyqxmd.com/read/29786643/controlled-deactivation-cb1-receptor-ligands-as-a-novel-strategy-to-lower-intraocular-pressure
#12
Sally Miller, Shashank Kulkarni, Alex Ciesielski, Spyros P Nikas, Ken Mackie, Alexandros Makriyannis, Alex Straiker
Nearly half a century has passed since the demonstration that cannabis and its chief psychoactive component Δ⁸-THC lowers intraocular pressure (IOP). Elevated IOP remains the chief hallmark and therapeutic target for glaucoma, a condition that places millions at risk of blindness. It is likely that Δ⁸-THC exerts much of its IOP-lowering effects via the activation of CB1 cannabinoid receptors. However, the initial promise of CB1 as a target for treating glaucoma has not thus far translated into a credible therapeutic strategy...
May 22, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29786560/microfabrication-of-liver-and-heart-tissues-for-drug-development
#13
REVIEW
Grace E Brown, Salman R Khetani
Drug-induced liver- and cardiotoxicity remain among the leading causes of preclinical and clinical drug attrition, marketplace drug withdrawals and black-box warnings on marketed drugs. Unfortunately, animal testing has proven to be insufficient for accurately predicting drug-induced liver- and cardiotoxicity across many drug classes, likely due to significant differences in tissue functions across species. Thus, the field of in vitro human tissue engineering has gained increasing importance over the last 10 years...
July 5, 2018: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/29786559/three-dimensional-bioprinting-of-stem-cell-derived-tissues-for-human-regenerative-medicine
#14
REVIEW
Gregor Skeldon, Baltasar Lucendo-Villarin, Wenmiao Shu
Stem cell technology in regenerative medicine has the potential to provide an unlimited supply of cells for drug testing, medical transplantation and academic research. In order to engineer a realistic tissue model using stem cells as an alternative to human tissue, it is essential to create artificial stem cell microenvironment or niches. Three-dimensional (3D) bioprinting is a promising tissue engineering field that offers new opportunities to precisely place stem cells within their niches layer-by-layer...
July 5, 2018: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/29786558/new-substrates-for-stem-cell-control
#15
REVIEW
Sara Schmidt, Annamaria Lilienkampf, Mark Bradley
The capacity to culture stem cells in a controllable, robust and scalable manner is necessary in order to develop successful strategies for the generation of cellular and tissue platforms for drug screening, toxicity testing, tissue engineering and regenerative medicine. Creating substrates that support the expansion, maintenance or directional differentiation of stem cells would greatly aid these efforts. Optimally, the substrates used should be chemically defined and synthetically scalable, allowing growth under defined, serum-free culture conditions...
July 5, 2018: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/29786552/intestinal-organoids-for-modelling-intestinal-development-and-disease
#16
REVIEW
Kathryn L Fair, Jennifer Colquhoun, Nicholas R F Hannan
Gastrointestinal diseases are becoming increasingly prevalent in developed countries. Immortalized cells and animal models have delivered important but limited insight into the mechanisms that initiate and propagate these diseases. Human-specific models of intestinal development and disease are desperately needed that can recapitulate structure and function of the gut in vitro Advances in pluripotent stem cells and primary tissue culture techniques have made it possible to culture intestinal epithelial cells in three dimensions that self-assemble to form 'intestinal organoids'...
July 5, 2018: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/29786551/three-dimensional-cell-culture-from-evolution-to-revolution
#17
REVIEW
Sharmin Alhaque, Michael Themis, Hassan Rashidi
Recent advances in the isolation of tissue-resident adult stem cells and the identification of inductive factors that efficiently direct differentiation of human pluripotent stem cells along specific lineages have facilitated the development of high-fidelity modelling of several tissues in vitro Many of the novel approaches have employed self-organizing three-dimensional (3D) culturing of organoids, which offer several advantages over conventional two-dimensional platforms. Organoid technologies hold great promise for modelling diseases and predicting the outcome of drug responses in vitro Here, we outline the historical background and some of the recent advances in the field of three-dimensional organoids...
July 5, 2018: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/29786508/-use-of-the-evalobs-%C3%A2-adherence-scale-in-an-unselected-french-population-of-treated-subjects-with-antihypertensive-hypolipemiants-or-oral-antidiabetics-medications-the-flahs-2017-adherence-survey
#18
X Girerd, O Hanon, B Vaïsse
OBJECTIVE: A Visual Analog Scale (VAS) is useful for diagnosing medication nonadherence and its validity has been evaluated using electronic pillbox as the gold standard. We have developed the EvaLobs® scale for use on paper or on smartphone and the aim of the study was to administrate the scale among FLAHS 2017 participants treated for an hypertension, a dyslipidemia or diabetes. In subjects treated with antihypertensive medications, participants completed the 6-item Girerd Scale and EvaLobs® ...
May 18, 2018: Annales de Cardiologie et D'angéiologie
https://www.readbyqxmd.com/read/29786430/galaxygpcrloop-template-based-and-ab-initio-structure-sampling-of-the-extracellular-loops-of-g-protein-coupled-receptors
#19
Jonghun Won, Gyu Rie Lee, Hahnbeom Park, Chaok Seok
The second extracellular loops (ECL2s) of G-protein-coupled receptors (GPCRs) are often involved in GPCR functions, and their structures have important implications in drug discovery. However, structure prediction of ECL2 is difficult because of its long length and the structural diversity among different GPCRs. In this study, a new ECL2 conformational sampling method involving both template-based and ab initio sampling was developed. Inspired by observation of similar ECL2 structures of closely related GPCRs, a template-based sampling method employing loop structure templates selected from the structure database was developed...
May 22, 2018: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/29786423/electrochemical-determination-of-tnt-dnt-rdx-and-hmx-with-gold-nanoparticles-poly-carbazole-aniline-film-modified-glassy-carbon-sensor-electrodes-imprinted-for-molecular-recognition-of-nitroaromatics-and-nitramines
#20
Şener Sağlam, Ayşem Üzer, Erol Erçağ, Reşat Apak
Since nitroaromatic and nitramine type energetic materials, mostly arising from military activities, are persistent pollutants in soil and groundwater, on-site sensing of these hazardous chemicals has gained importance. A novel electrochemical sensor was designed for detecting nitroaromatic and nitramine type energetic materials, relying on gold nanoparticles (Aunano ) -modified glassy carbon (GC) electrode coated with nitro-energetic memory poly(carbazole-aniline) copolymer (Cz- co-ANI) film (e.g., TNT memory-GC/P(Cz- co-ANI)-Aunano modified electrode)...
May 22, 2018: Analytical Chemistry
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