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https://www.readbyqxmd.com/read/28350454/structural-optimizations-of-thieno-3-2-b-pyrrole-derivatives-for-the-development-of-metabolically-stable-inhibitors-of-chikungunya-virus
#1
Kuan Chieh Ching, Thi Ngoc Quy Tran, Siti Naqiah Amrun, Yiu Wing Kam, Lisa F P Ng, Christina Li Lin Chai
Chikungunya virus (CHIKV) is a re-emerging vector-borne alphavirus and there is no approved effective antiviral treatment currently available for CHIKV. We previously reported the discovery of thieno[3,2-b]pyrrole 1b that displayed good antiviral activity against CHIKV infection in vitro. However, it has a short half-life in the presence of human liver microsomes (HLMs) (T1/2 = 2.91 min). Herein, we report further optimization studies in which potential metabolically labile sites on compound 1b were removed or modified, resulting in the identification of thieno[3,2-b]pyrrole 20 and pyrrolo[2,3-d]thiazole 23c possessing up to 17-fold increase in metabolic half-lives in HLMs and good in vivo pharmacokinetic properties...
March 28, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28346781/metabolism-of-ibuprofen-by-phragmites-australis-uptake-and-phytodegradation
#2
Yujie He, Alette A M Langenhoff, Nora B Sutton, Huub H M Rijnaarts, Marco H Blokland, Feiran Chen, Christian Huber, Peter Schröder
This study explores ibuprofen (IBP) uptake and transformation in the wetland plant species Phragmites australis and the underlying mechanisms. We grew P. australis in perlite under greenhouse conditions and treated plants with 60 µg/l of IBP. Roots and rhizomes (RR), stems and leaves (SL), and liquid samples were collected during 21 days of exposure. Results show that P. australis can take up, translocate, and degrade IBP. IBP was completely removed from the liquid medium after 21 days with a half-life of 2...
March 27, 2017: Environmental Science & Technology
https://www.readbyqxmd.com/read/28345998/pharmacokinetics-of-a-single-dose-of-voriconazole-administered-orally-with-and-without-food-to-red-tailed-hawks-buteo-jamaicensus
#3
Ruth A Parsley, Lisa A Tell, Ronette Gehring
OBJECTIVE To determine the pharmacokinetics of voriconazole administered PO with or without food to red-tailed hawks (Buteo jamaicensus) and whether any observed variability could be explained by measured covariates to inform dose adjustments. ANIMALS 7 adult red-tailed hawks. PROCEDURES In a crossover study design, hawks were randomly assigned to first receive voriconazole (15 mg/kg, PO) injected into a dead mouse (n = 3; fed birds) or without food (4; unfed birds). Sixteen days later, treatments were reversed...
April 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28345745/in-vitro-and-in-vivo-assessment-of-the-abuse-potential-of-pf614-a-novel-bio-md%C3%A2-prodrug-of-oxycodone
#4
D Lynn Kirkpatrick, William K Schmidt, Ricardo Morales, John Cremin, Julie Seroogy, Craig Husfeld, Thomas Jenkins
OBJECTIVE: The need for pain medication which will not lead to abuse is well recognized. Ensysce has designed prodrug analogs of the commonly used pain medications including hydromorphone, oxycodone (OC), hydrocodone, and morphine that limit their use to oral delivery, two of which are in clinical development. This study was undertaken to demonstrate that PF614, an extended-release prodrug of OC, allows the release of OC as designed when delivered orally, yet it resists ex vivo extraction with household chemicals and is pharmacologically inactive when administered by nonoral routes (nasal and parenteral), thereby substantially reducing its intravenous (IV) and intranasal abuse potential...
January 2017: Journal of Opioid Management
https://www.readbyqxmd.com/read/28344998/low-dose-liver-targeted-gene-therapy-for-pompe-disease-enhances-therapeutic-efficacy-of-ert-via-immune-tolerance-induction
#5
Sang-Oh Han, Giuseppe Ronzitti, Benjamin Arnson, Christian Leborgne, Songtao Li, Federico Mingozzi, Dwight Koeberl
Pompe disease results from acid α-glucosidase (GAA) deficiency, and enzyme replacement therapy (ERT) with recombinant human (rh) GAA has clinical benefits, although its limitations include the short half-life of GAA and the formation of antibody responses. The present study compared the efficacy of ERT against gene transfer with an adeno-associated viral (AAV) vector containing a liver-specific promoter. GAA knockout (KO) mice were administered either a weekly injection of rhGAA (20 mg/kg) or a single injection of AAV2/8-LSPhGAA (8 × 10(11) vector genomes [vg]/kg)...
March 17, 2017: Molecular Therapy. Methods & Clinical Development
https://www.readbyqxmd.com/read/28344481/stability-of-erythropoietin-repackaging-in-polypropylene-syringes-for-clinical-use
#6
Angela Marsili, Giorgia Puorro, Chiara Pane, Anna de Rosa, Giovanni Defazio, Carlo Casali, Antonio Cittadini, Giuseppe de Michele, Brunello Ettore Florio, Alessandro Filla, Francesco Saccà
Introduction: Epoetin alfa (Eprex®) is a subcutaneous, injectable formulation of short half-life recombinant human erythropoietin (rHuEPO). To current knowledge there are no published studies regarding the stability of rHuEPO once repackaging occurs (r-EPO) for clinical trial purposes. Materials and methods: We assessed EPO concentration in Eprex® and r-EPO syringes at 0, 60, 90, and 120 days after repackaging in polypropylene syringes. R-EPO was administered to 56 patients taking part in a clinical trial in Friedreich Ataxia...
February 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28343392/pharmacokinetic-and-biodistribution-studies-of-hpma-copolymer-conjugates-in-an-aseptic-implant-loosening-mouse-model
#7
Xin Wei, Fei Li, Gang Zhao, Yashpal Singh S Chhonker, Christine Elise Averill, Josselyn Galdamez, P Edward Purdue, Xiaoyan Wang, Edward V Fehringer, Kevin L Garvin, Steven R Goldring, Yazen Alnouti, Dong Wang
N-(2-Hydroxypropyl) methacrylamide (HPMA) copolymers were previously found to represent a versatile delivery platform for the early detection and intervention of orthopedic implant loosening. In this manuscript, we evaluated the impact of different structural parameters of the HPMA copolymeric system (e.g. molecular weight (MW), drug content) to its pharmacokinetics and biodistribution (PK/BD) profile. Using 125I, Alexa Fluor® 488 and IRDye® 800 CW-labeled HPMA copolymer-dexamethasone (P-Dex) conjugates with different MW and dexamethasone (Dex) contents, we found the MW to be the predominant impact factor on the PK/BD profiles of P-Dex, with Dex content as a secondary impact factor...
March 25, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28342666/stabilization-study-of-inactivated-foot-and-mouth-disease-virus-vaccine-by-size-exclusion-hplc-and-differential-scanning-calorimetry
#8
Yanli Yang, Qizu Zhao, Zhengjun Li, Lijing Sun, Guanghui Ma, Songping Zhang, Zhiguo Su
The inactivated foot and mouth disease virus (FMDV), which has a sedimentation coefficient of 146S, is crucial to the efficacy of vaccine preparations, but extremely unstable in vitro. It is prone to dissociate into smaller particles referred to as 12S with a concomitant decrease in immunogenicity; therefore, it is of great importance to find the best condition for stabilizing the FMDV. In the present work, the effects of solution pH and temperature on the dissociation of 146S was investigated and potential stabilizers were screened, with aid of high-performance size-exclusion chromatography (HPSEC) for rapid and quantitative determination of 146S, together with differential scanning calorimetry (DSC) technology for thermal stability analysis...
March 22, 2017: Vaccine
https://www.readbyqxmd.com/read/28342049/safety-assessment-of-chromafenozide-residue-level-with-decline-study-on-tomato-in-egypt
#9
Ehab Abdelraheem, Mohamed Arief, Somaia G Mohammad, Wayne Jiang
The objective of this study is to perform a safety assessment of chromafenozide residue level on tomato at the Egyptian national level. An open field decline study of chromafenozide on tomato was performed. The theoretical maximum daily intake (TMDI) of chromafenozide was calculated for assessing the chronic dietary exposure indicating that the ADI value of chromafenozide (0.27 mg/kg bw/day) was not exceeded. As a result, the safety assessment of chromafenozide residue levels was attained. A validated method of the QuEChERS approach followed by HPLC-DAD analysis was used to determine the chromafenozide residues...
April 2017: Environmental Monitoring and Assessment
https://www.readbyqxmd.com/read/28340139/assessment-of-acute-kidney-injury-in-rhabdomyolytic-mice-by-transcutaneous-measurement-of-sinistrin-excretion
#10
Aldo Moggio, Stefania Geraci, Alberto Boido, Carsten Sticht, Norbert Gretz, Benedetta Bussolati
Background: . Early and accurate assessment of renal function is required for the successful detection and treatment of acute kidney injury (AKI). However, only retention parameters such as plasma urea and creatinine, and the indirect estimation of glomerular filtration rate are commonly available. Methods.: Here, we measured the kinetics of plasma fluorescein isothiocyanate (FITC)-sinistrin excretion to detect alterations of renal function over time in a murine model of rhabdomyolysis-induced AKI...
February 27, 2017: Nephrology, Dialysis, Transplantation
https://www.readbyqxmd.com/read/28339766/higher-bioavailability-of-doxycycline-in-broiler-chickens-with-a-novel-in-feed-pharmaceutical-formulation
#11
Lilia Gutiérrez, Juan Zermeño, Yazmín Alcalá, Héctor Sumano
Bioavailability of a new, long-acting (LA) pharmaceutical preparation for administering doxycycline as in-feed medication to broiler chickens was compared to the standard in-feed administration of doxycycline. A commercial poultry house harboring Ross-308 broiler chickens, weighing 450 g, was divided into 7 sections as follows: doxy-FOLA group (n = 6,000 chickens divided into 3 replicates) medicated with 10% doxycyline, long-acting pellets at a dose of 400 g of doxycycline HCl/ton of food, resulting in a calculated dose of 48 mg/kg for 5 d; doxy-ref group (n = 6,000, divided into 3 replicates) medicated as for doxy-FOLA, but using a 20% commercial preparation of doxycycline...
February 23, 2017: Poultry Science
https://www.readbyqxmd.com/read/28339166/pharmacokinetics-pharmacodynamics-pharmacogenomics-safety-and-tolerability-of-avatrombopag-in-healthy-japanese-and-white-subjects
#12
Maiko Nomoto, Gina Pastino, Bhaskar Rege, Jagadeesh Aluri, Jim Ferry, David Han
Avatrombopag, an orally administered, small-molecule thrombopoietin receptor (c-Mpl) agonist, is currently in clinical development for the potential treatment of severe thrombocytopenia in patients with chronic liver disease undergoing an elective procedure. The objectives of this study were to characterize and compare the pharmacokinetics (including the food effect) and pharmacodynamics (platelet count) of avatrombopag following single doses in Japanese and white subjects. Following single dosing under fasted and fed conditions, mean peak concentrations occurred at 5 to 8 hours and subsequently declined with a half-life of 16 to 18 hours in Japanese and white subjects...
March 24, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28337282/chronic-intermittent-hypoxia-affects-endogenous-serotonergic-inputs-and-expression-of-synaptic-proteins-in-rat-hypoglossal-nucleus
#13
Xu Wu, Huan Lu, Lijuan Hu, Wankun Gong, Juan Wang, Cuiping Fu, Zilong Liu, Shanqun Li
Evidence has shown that hypoxic episodes elicit hypoglossal neuroplasticity which depends on elevated serotonin (5-HT), in contrast to the rationale of obstructive sleep apnea (OSA) that deficient serotonergic input to HMs fails to keep airway patency. Therefore, understanding of the 5-HT dynamic changes at hypoglossal nucleus (HN) during chronic intermittent hypoxia (CIH) will be essential to central pathogenic mechanism and pharmacological therapy of OSA. Moreover, the effect of CIH on BDNF-TrkB signaling proteins was quantified in an attempt to elucidate cellular cascades/synaptic mechanisms following 5-HT alteration...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28337188/influence-of-herbicide-triasulfuron-on-soil-microbial-community-in-an-unamended-soil-and-a-soil-amended-with-organic-residues
#14
Eva Pose-Juan, José M Igual, María J Sánchez-Martín, M S Rodríguez-Cruz
The effect of organic amendments and pesticides on a soil microbial community has garnered considerable interest due to the involvement of microorganisms in numerous soil conservation and maintenance reactions. The aim of this work was to assess the influence on a soil microbial community of the simultaneous application of the herbicide triasulfuron at three doses (2, 10, and 50 mg kg(-1)), with an organic amendment [sewage sludge (SS) or green compost (GC)]. Dissipation kinetics, soil microbial biomass, dehydrogenase activity (DHA) and respiration, and the profile of phospholipid fatty acids (PLFAs) extracted from the soil, were determined in unamended (S) soil and amended (S+SS and S+GC) ones...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28337087/medication-dosage-in-overweight-and-obese-children
#15
Kelly L Matson, Evan R Horton, Amanda C Capino
Approximately 31.8% of U.S. children ages 2 to 19 years are considered overweight or obese. This creates significant challenges to dosing medications that are primarily weight based (mg/kg) and in predicting pharmacokinetics parameters in pediatric patients. Obese individuals generally have a larger volume of distribution for lipophilic medications. Conversely, the Vd of hydrophilic medications may be increased or decreased due to increased lean body mass, blood volume, and decrease percentage of total body water...
January 2017: Journal of Pediatric Pharmacology and Therapeutics: JPPT: the Official Journal of PPAG
https://www.readbyqxmd.com/read/28337082/pharmacokinetics-of-peramivir-in-an-adolescent-patient-receiving-continuous-venovenous-hemodiafiltration
#16
Ryan C Dillon, Robert Witcher, Jeffrey J Cies, Wayne S Moore, Arun Chopra
Critically ill patients requiring renal replacement therapy commonly experience pharmacokinetic alterations. This case report describes the pharmacokinetics of peramivir (Rapivab, BioCryst Pharmaceuticals, Inc, Durham, NC), the first US Food and Drug Administration-approved intravenous neuraminidase inhibitor for the treatment of influenza, in an adolescent patient receiving continuous renal replacement therapy (CRRT). A 49.5-kg, 17-year-old Caucasian female presented with fever, cough, and persistent hypoxia...
January 2017: Journal of Pediatric Pharmacology and Therapeutics: JPPT: the Official Journal of PPAG
https://www.readbyqxmd.com/read/28336956/preclinical-development-of-a-humanized-neutralizing-antibody-targeting-hgf
#17
Hyori Kim, Sung Hee Hong, Jung Yong Kim, In-Chull Kim, Young-Whan Park, Song-Jae Lee, Seong-Won Song, Jung Ju Kim, Gunwoo Park, Tae Min Kim, Yun-Hee Kim, Jong Bae Park, Junho Chung, In-Hoo Kim
Hepatocyte growth factor (HGF) and its receptor, cMET, play critical roles in cell proliferation, angiogenesis and invasion in a wide variety of cancers. We therefore examined the anti-tumor activity of the humanized monoclonal anti-HGF antibody, YYB-101, in nude mice bearing human glioblastoma xenografts as a single agent or in combination with temozolomide. HGF neutralization, The extracellular signal-related kinases 1 and 2 (ERK1/2) phosphorylation, and HGF-induced scattering were assessed in HGF-expressing cell lines treated with YYB-101...
March 24, 2017: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/28336561/mice-lacking-the-inhibitory-collagen-receptor-lair-1-exhibit-a-mild-thrombocytosis-and-hyperactive-platelets
#18
Christopher W Smith, Steven G Thomas, Zaher Raslan, Pushpa Patel, Maxwell Byrne, Marie Lordkipanidzé, Danai Bem, Linde Meyaard, Yotis A Senis, Steve P Watson, Alexandra Mazharian
OBJECTIVE: Leukocyte-associated immunoglobulin-like receptor-1 (LAIR-1) is a collagen receptor that belongs to the inhibitory immunoreceptor tyrosine-based inhibition motif-containing receptor family. It is an inhibitor of signaling via the immunoreceptor tyrosine-based activation motif-containing collagen receptor complex, glycoprotein VI-FcRγ-chain. It is expressed on hematopoietic cells, including immature megakaryocytes, but is not detectable on platelets. Although the inhibitory function of LAIR-1 has been described in leukocytes, its physiological role in megakaryocytes and in particular in platelet formation has not been explored...
March 23, 2017: Arteriosclerosis, Thrombosis, and Vascular Biology
https://www.readbyqxmd.com/read/28335600/redox-potential-sensitive-n-acetyl-cysteine-prodrug-nanoparticles-inhibit-the-activation-of-microglia-and-improve-neuronal-survival
#19
Eleni Markoutsa, Peisheng Xu
One hallmark of neuroinflammation is the activation of microglia, which triggers the production and release of reactive oxygen species (ROS), nitrate, nitrite, and cytokines. N-acetyl cysteine (NAC) is a free radical scavenger that is involved in the intracellular and extracellular detoxification of ROS in the brain. However, the clinical application of NAC is limited by its low bioavailability and short half-life. Herein, NAC was conjugated to a polymer through disulfide bond to form a NAC-prodrug nanoparticle (NAC-NP)...
March 23, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28335469/comparison-of-the-pharmacokinetic-properties-of-hemoglobin-based-oxygen-carriers
#20
REVIEW
Kazuaki Taguchi, Keishi Yamasaki, Toru Maruyama, Masaki Otagiri
Hemoglobin (Hb) is an ideal material for use in the development of an oxygen carrier in view of its innate biological properties. However, the vascular retention of free Hb is too short to permit a full therapeutic effect because Hb is rapidly cleared from the kidney via glomerular filtration or from the liver via the haptogloblin-CD 163 pathway when free Hb is administered in the blood circulation. Attempts have been made to develop alternate acellular and cellular types of Hb based oxygen carriers (HBOCs), in which Hb is processed via various routes in order to regulate its pharmacokinetic properties...
March 18, 2017: Journal of Functional Biomaterials
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