keyword
MENU ▼
Read by QxMD icon Read
search

half-life

keyword
https://www.readbyqxmd.com/read/28449232/safety-pharmacokinetics-and-pharmacologic-effects-of-the-selective-androgen-receptor-modulator-gsk2881078-in-healthy-men-and-postmenopausal-women
#1
Richard V Clark, Ann C Walker, Susan Andrews, Philip Turnbull, Jeffrey A Wald, Mindy H Magee
AIM: Selective androgen receptor modulators (SARMs) induce anabolic effects on muscle without the adverse effects of androgenic steroids. In this first-in-human study, we report safety, tolerability, pharmacokinetics (PK), and pharmacodynamics of the SARM GSK2881078. METHODS: In Part A, healthy young men (n = 10) received a single dose of study drug (0 mg, 0.05 mg, 0.1 mg, 0.2 mg GSK2881078 or matching-placebo). In Part B, repeat-dose cohorts in men (n = 65) were 0...
April 27, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28449192/anti-inflammatory-effects-of-pegylated-human-adrenomedullin-in-a-mouse-dss-induced-colitis-model
#2
Sayaka Nagata, Motoo Yamasaki, Kazuo Kitamura
Preclinical Research Human adrenomedullin (hAM), a hypotensive peptide, also has anti-inflammatory effects. hAM can reduce the severity of the dextran sulphate sodium (DSS)- and 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis in animal models. Furthermore, in a clinical study, hAM treatment reduced the Disease Activity Index in ulcerative colitis. However, these therapeutic effects required continuous administration of hAM as the half-life of native hAM is quite short in blood. To resolve this problem, hAM N-terminal was conjugated with two kinds of polyethylene glycol (PEG); 5 kDa PEG or 60 kDa PEG (5 kDa PEG-hAM and 60 kDa PEG-hAM respectively)...
April 27, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28449038/real-time-imaging-of-single-neuronal-cell-apoptosis-in-patients-with-glaucoma
#3
Maria F Cordeiro, Eduardo M Normando, M Jorge Cardoso, Serge Miodragovic, Seham Jeylani, Benjamin M Davis, Li Guo, Sebastien Ourselin, Roger A'Hern, Philip A Bloom
Retinal cell apoptosis occurs in many ocular neurodegenerative conditions including glaucoma-the major cause of irreversible blindness worldwide. Using a new imaging technique that we have called DARC (detection of apoptosing retinal cells), which until now has only been demonstrated in animal models, we assessed if annexin 5 labelled with fluorescent dye DY-776 (ANX776) could be used safely in humans to identify retinal cell apoptosis. Eight patients with glaucomatous neurodegeneration and evidence of progressive disease, and eight healthy subjects were randomly assigned to intravenous ANX776 doses of 0...
April 26, 2017: Brain: a Journal of Neurology
https://www.readbyqxmd.com/read/28449002/purification-and-biochemical-and-kinetic-properties-of-an-endo-polygalacturonase-from-the-industrial-fungus-aspergillus-sojae
#4
Dante Fratebianchi, Ivana Alejandra Cavello, Sebastián Fernando Cavalitto
An endo-polygalacturonase secreted by Aspergillus sojae was characterized after being purified to homogeneity from submerged cultures with orange peel as the sole carbon source by gel filtration and ion-exchange chromatographies. According to SDS-PAGE and analytical isoelectric focusing analyses, the enzyme presents a molecular weight of 47 kDa and pI value of 4.2. This enzyme exhibits considerable stability under highly acidic to neutral conditions (pH 1.5-6.5) and presents a half-life of 2 h at 50°C. Besides its activity towards pectin and polygalacturonic acid, the enzyme displays pectin-releasing activity, acting best in a pH range of 3...
April 28, 2017: Journal of Molecular Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28448818/pegylated-bilirubin-nanoparticle-as-an-anti-oxidative-and-anti-inflammatory-demulcent-in-pancreatic-islet-xenotransplantation
#5
Min Jun Kim, Yonghyun Lee, Sangyong Jon, Dong Yun Lee
Transplanted islets suffer hypoxic stress, which leads to nonspecific inflammation. This is the major cause of islet graft failure during the early stage of intrahepatic islet transplantation. Although bilirubin has shown potent anti-oxidative and anti-inflammatory functions, its clinical applications have been limited due to its insolubility and short half-life. To overcome this problem, novel amphiphilic bilirubin nanoparticles are designed. Hydrophilic poly(ethylene glycol) (PEG) is conjugated to the hydrophobic bilirubin molecule...
April 18, 2017: Biomaterials
https://www.readbyqxmd.com/read/28447858/risk-prediction-of-hepatotoxicity-in-paracetamol-poisoning
#6
Anselm Wong, Andis Graudins
CONTEXT: Paracetamol (acetaminophen) poisoning is the most common cause of acute liver failure in the developed world. A paracetamol treatment nomogram has been used for over four decades to help determine whether patients will develop hepatotoxicity without acetylcysteine treatment, and thus indicates those needing treatment. Despite this, a small proportion of patients still develop hepatotoxicity. More accurate risk predictors would be useful to increase the early detection of patients with the potential to develop hepatotoxicity despite acetylcysteine treatment...
April 27, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28446744/levetiracetam-pharmacokinetics-in-a-patient-with-intracranial-hemorrhage-undergoing-continuous-veno-venous-hemofiltration
#7
Edward T Van Matre, Scott W Mueller, Douglas N Fish, Robert MacLaren, Luis F Cava, Robert T Neumann, Tyree H Kiser
BACKGROUND Levetiracetam is an antiepileptic drug frequently used in critically ill patients. Levetiracetam is primarily eliminated as a parent compound via glomerular filtration and requires dose adjustment in renal insufficiency, but the literature on patients receiving continuous veno-venous hemofiltration (CVVH) is scant. CASE REPORT We report the levetiracetam pharmacokinetic profile of a patient being treated with levetiracetam 1000 mg intravenously every 12 h who required continuous veno-venous hemofiltration (CVVH)...
April 27, 2017: American Journal of Case Reports
https://www.readbyqxmd.com/read/28446540/human-prostate-luminal-cell-differentiation-requires-notch3-induction-by-p38-mapk-and-myc
#8
Sander B Frank, Penny L Berger, Mats Ljungman, Cindy K Miranti
Many pathways dysregulated in prostate cancer are also involved in epithelial differentiation. To better understand prostate tumor initiation, we sought to investigate specific genes and mechanisms required for normal basal to luminal cell differentiation. Utilizing human prostate basal epithelial cells and an in vitro differentiation model, we tested the hypothesis that p38-MAPK regulation of NOTCH3, via MYC, is required for luminal differentiation. Inhibition (SB202190, BIRB796) or knockdown of p38α and/or p38δ prevented proper differentiation...
April 26, 2017: Journal of Cell Science
https://www.readbyqxmd.com/read/28446517/a-novel-%C3%AE-calcitonin-gene-related-peptide-analogue-protects-against-end-organ-damage-in-experimental-hypertension-cardiac-hypertrophy-and-heart-failure
#9
Aisah A Aubdool, Pratish Thakore, Fulye Argunhan, Sarah-Jane Smillie, Moritz Schnelle, Salil Srivastava, Khadija M Alawi, Elena Wilde, Jennifer Mitchell, Keith Farrell-Dillon, Daniel A Richards, Giuseppe Maltese, Richard C Siow, Manasi Nandi, James E Clark, Ajay M Shah, Anette Sams, Susan D Brain
Background -Research into the therapeutic potential of α-calcitonin gene-related peptide (α-CGRP) has been limited due to its peptide nature and short half-life. Here, we evaluate whether a novel potent and long lasting (t½ ≥ 7h) acylated α-CGRP analogue (αAnalogue) could alleviate and reverse cardiovascular disease in two distinct murine models of hypertension and heart failure in vivoMethods -The ability of the αAnalogue to act selectively via the CGRP pathway was shown in skin using a CGRP receptor antagonist...
April 26, 2017: Circulation
https://www.readbyqxmd.com/read/28446512/molecular-mechanisms-facilitating-the-initial-kinetochore-encounter-with-spindle-microtubules
#10
Vanya Vasileva, Marek Gierlinski, Zuojun Yue, Nicola O'Reilly, Etsushi Kitamura, Tomoyuki U Tanaka
The initial kinetochore (KT) encounter with a spindle microtubule (MT; KT capture) is one of the rate-limiting steps in establishing proper KT-MT interaction during mitosis. KT capture is facilitated by multiple factors, such as MT extension in various directions, KT diffusion, and MT pivoting. In addition, KTs generate short MTs, which subsequently interact with a spindle MT. KT-derived MTs may facilitate KT capture, but their contribution is elusive. In this study, we find that Stu1 recruits Stu2 to budding yeast KTs, which promotes MT generation there...
April 26, 2017: Journal of Cell Biology
https://www.readbyqxmd.com/read/28445610/population-pharmacokinetics-of-liposomal-irinotecan-in-patients-with-cancer
#11
Bambang Adiwijaya, Jaeyeon Kim, Istvan Lang, Tibor Csõszi, Antonio Cubillo, Jen-Shi Chen, Mark Wong, Joon Oh Park, Jun Suk Kim, Kun Ming Rau, Bohuslav Melichar, Javier Gallego, Jonathan Fitzgerald, Bruce Belanger, Istvan Molnar, Wen Wee Ma
nal-IRI is a liposomal formulation of irinotecan with a longer half-life (t1/2 ), higher plasma total irinotecan (tIRI), and lower SN-38 maximum concentration (Cmax ) compared with non-liposomal irinotecan. Population pharmacokinetic (PK) analysis of nal-IRI was performed for tIRI and total SN-38 (tSN38) using patient samples from 6 studies. PK-safety association was evaluated for neutropenia and diarrhea in 353 patients. PK-efficacy association was evaluated from a phase 3 study in pancreatic cancer NAPOLI1...
April 26, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28445495/pharmacokinetic-and-pharmacodynamic-modelling-after-subcutaneous-intravenous-and-buccal-administration-of-a-high-concentration-formulation-of-buprenorphine-in-conscious-cats
#12
Graeme M Doodnaught, Beatriz P Monteiro, Javier Benito, Daniel Edge, Francis Beaudry, Ludovic Pelligand, Paulo Steagall
BACKGROUND: The aim of this study was to describe the joint pharmacokinetic-pharmacodynamic model and evaluate thermal antinociception of a high-concentration formulation of buprenorphine (Simbadol™) in cats. METHODS: Six healthy cats (4.9 ± 0.7 kg) were included in a prospective, randomized, blinded, crossover study. Simbadol™ (1.8 mg mL-1) was administered by the subcutaneous (SC; 0.24 mg kg-1), intravenous (IV; 0.12 mg kg-1) or buccal (OTM; 0.12 mg kg-1) route of administration and thermal thresholds (TT) were compared with a saline group (SAL)...
2017: PloS One
https://www.readbyqxmd.com/read/28444959/controlling-and-monitoring-intracellular-delivery-of-anticancer-polymer-nanomedicines
#13
REVIEW
Claudia Battistella, Harm-Anton Klok
Polymer nanomedicines are very attractive to improve the delivery of chemotherapeutics. Polymer conjugates and other polymer-based nanocarriers allow to increase plasma half-life and drug bioavailability and can also be guided toward tumors using passive and active targeting strategies. Since many chemotherapeutics act on targets that are located in well-defined subcellular compartments, other important factors that contribute to an efficient therapy include cellular internalization and subsequent intracellular trafficking of the polymer nanomedicines and/or its payload to the appropriate organelle in the cytoplasm...
April 26, 2017: Macromolecular Bioscience
https://www.readbyqxmd.com/read/28444856/pharmacokinetics-after-a-single-dose-of-naloxone-administered-as-a-nasal-spray-in-healthy-volunteers
#14
E Vanky, L Hellmundt, U Bondesson, S Eksborg, S Lundeberg
BACKGROUND: There is increasing interest in the use of intranasal naloxone to reverse adverse opioid effects during management of procedural pain in children and in adults after overdose. There are limited data on the pharmacokinetics of intranasal naloxone so in this study we aimed to detail the pharmacokinetic profile of the commercially marketed injectable solution of naloxone 0.4 mg/ml when administered as an intranasal spray. METHODS: Twenty healthy volunteers received naloxone as an intranasal spray at a dose of 10 μg/kg...
April 25, 2017: Acta Anaesthesiologica Scandinavica
https://www.readbyqxmd.com/read/28444664/endocrine-complications-of-surgical-treatment-of-thyroid-cancer-an-update
#15
Pedro Iglesias, Juan José Díez
Postoperative hypoparathyroidism (HypoPT) and hypothyroidism (HypoT) are the main endocrine complications after the surgical treatment for thyroid cancer. Postsurgical HypoPT can be transient, protracted or permanent. Its frequency varies according to the underlying cervical pathology, surgical technique, and mainly the experience of the surgeon. Risk factors for HypoPT include aggressiveness of the tumor, extent of surgery, the presence of parathyroid gland in the pathologic specimen, and surgeon experience...
April 25, 2017: Experimental and Clinical Endocrinology & Diabetes
https://www.readbyqxmd.com/read/28444597/biodegradation-of-pyrene-and-benzo-a-pyrene-in-the-liquid-matrix-and-soil-by-a-newly-identified-raoultella-planticola-strain
#16
Lifeng Ping, Qian Guo, Xiaoyang Chen, Xiaoli Yuan, Chunrong Zhang, Hua Zhao
In the current study, the PL7 strain was isolated from soil and identified as Raoultella planticola based on its physiological characteristics and 16S rDNA sequence. By the 10th day, the PL7 strain degraded 52.0% of the pyrene (PYR) content and 50.8% of the benzo[a]pyrene (BaP) content in 20 mg L(-1) PYR and 10 mg L(-1) BaP in the liquid matrix. The half-life of PYR and BaP by PL7 degradation was 8.59 and 9.46 days, respectively. At pH 8.0, the degradation rates of PYR and BaP by PL7 were significantly higher at 30 °C than at 20 and 40 °C...
May 2017: 3 Biotech
https://www.readbyqxmd.com/read/28444357/coordinated-regulations-of-mrna-synthesis-and-decay-during-cold-acclimation-in-arabidopsis-cells
#17
Toshihiro Arae, Shiori Isai, Akira Sakai, Katsuhiko Mineta, Masami Yokota Hirai, Yuya Suzuki, Shigehiko Kanaya, Junji Yamaguchi, Satoshi Naito, Yukako Chiba
Plants possess a cold acclimation system to acquire freezing tolerance through pre-exposure to non-freezing low temperatures. The transcriptional cascade of C-repeat binding factors (CBFs)/dehydration response element-binding factors (DREBs) is considered a major transcriptional regulatory pathway during cold acclimation. However, little is known regarding the functional significance of mRNA stability regulation in the response of gene expression to cold stress. The actual level of individual mRNAs is determined by a balance between mRNA synthesis and degradation...
April 21, 2017: Plant & Cell Physiology
https://www.readbyqxmd.com/read/28443689/recent-achievements-in-tc-99m-radiopharmaceutical-direct-production-by-medical-cyclotrons
#18
Alessandra Boschi, Petra Martini, Micol Pasquali, Licia Uccelli
(99m)Tc is the most commonly used radionuclide in the field of diagnostic imaging, a noninvasive method intended to diagnose a disease, assess the disease state and monitor the effects of treatments. Annually, the use of (99m)Tc, covers about 85% of nuclear medicine applications. This isotope releases gamma rays at about the same wavelength as conventional X-ray diagnostic equipment, and owing to its short half-life (t½ = 6 hours) is ideal for diagnostic nuclear imaging. A patient can be injected with a small amount of (99m)Tc and within 24 hours almost 94% of the injected radionuclide would have decayed and left the body, limiting the patient's radiation exposure...
April 26, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28443255/glucagon-like-peptide-1-and-glucagon-like-peptide-1-receptor-agonists-in-the-treatment-of-type-2-diabetes
#19
REVIEW
Seungah Lee, Dong Yun Lee
The prevalence of type 2 diabetes (T2D) is increasing worldwide. Patients with T2D suffer from various diabetes-related complications. Since there are many patients with T2D that cannot be controlled by previously developed drugs, it has been necessary to develop new drugs, one of which is a glucagon-like peptide-1 (GLP-1) based therapy. GLP-1 has been shown to ameliorate diabetes-related conditions by augmenting pancreatic β-cell insulin secretion and having the low risk of causing hypoglycemia. Because of a very short half-life of GLP-1, many researches have been focused on the development of GLP-1 receptor (GLP-1R) agonists with long half-lives such as exenatide and dulaglutide...
March 2017: Annals of Pediatric Endocrinology & Metabolism
https://www.readbyqxmd.com/read/28442331/non-covalent-conjugation-of-cutinase-from-fusarium-sp-ict-sac1-with-pectin-for-enhanced-stability-process-minutiae-kinetics-thermodynamics-and-structural-study
#20
Abhijeet B Muley, Sandeep A Chaudhari, Rekha S Singhal
Cutinase, a member of α/β-fold hydrolase family possess potentially diverse applications in several industrial processes and products. The present work aims towards thermo-stabilization of cutinase from novel source Fusarium sp. ICT SAC1 via non-covalent interaction with polysaccharides. Although all six polysaccharides chosen for study enhanced the thermal stability, pectin was found to be most promising. The interaction protocol for cutinase with pectin was optimized sequentially with respect to the ratio of enzyme to pectin, solution pH, and buffer strength...
April 22, 2017: International Journal of Biological Macromolecules
keyword
keyword
91311
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"