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PubMed Journals Articles About "Sigma Pharmaceuticals Limited" RSS

11:28 EDT 17th July 2018 | BioPortfolio

Sigma Pharmaceuticals Limited PubMed articles on BioPortfolio. Our PubMed references draw on over 21 million records from the medical literature. Here you can see the latest Sigma Pharmaceuticals Limited articles that have been published worldwide.

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Showing "Sigma Pharmaceuticals Limited" PubMed Articles 1–25 of 423

Synthesis and pharmacological evaluation of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives as sigma-2 receptor ligands.

Increasing evidences have implicated that sigma-2 receptor is a biomarker and significantly over-expressed in many proliferative cancer cells with no or low expression in normal cells. Sigma-2 receptor selective ligands have been successfully used as valuable tools to study its pharmacological functions, tumor imaging, and cancer therapeutics or adjuvants. 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinolinylalkyl benzamides are among a few categories of structures that have demonstrated high affinities and selecti...


Performance specifications and six sigma theory: Clinical chemistry and industry compared.

Analytical performance specifications are crucial in test development and quality control. Although consensus has been reached on the use of biological variation to derive these specifications, no consensus has been reached which model should be preferred. The Six Sigma concept is widely applied in industry for quality specifications of products and can well be compared with Six Sigma models in clinical chemistry. However, the models for measurement specifications differ considerably between both fields: wh...

Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties.

Substituted norbenzomorphans are known to display high affinity and selectivity for the two sigma receptor (σR) subtypes. In order to study the effects of simplifying the structures of these compounds, a scaffold hopping strategy was used to design several novel sets of substituted isoindolines, tetrahydroisoquinolines and tetrahydro-2-benzazepines. The binding affinities of these new compounds for the sigma 1 (σ1R) and sigma 2 (σ2R) receptors were determined, and some analogs were identified that exhibi...


Sigma 1 receptor mediated HMGB1 expression in spinal cord is involved in the development of diabetic neuropathic pain.

No study has been conducted to examine the interactions of sigma-1 receptor (Sigma-1R) and high mobility group box 1 protein (HMGB1) in the development of diabetic peripheral neuropathy. Thus, we examined the effects of streptozotocin (STZ) treatment on expression of HMGB1 in subcellular levels in the dorsal root ganglion (DRG) in both wild-type and Sigma-1R-/- mice and evaluated the effects of repeated intrathecal administrations of selective Sigma-1R antagonists BD1047, agonist PRE-084, or HMGB1 inhibitor...

Autoverification process improvement by Six Sigma approach: Clinical chemistry & immunoassay.

This study examines effectiveness of a project to enhance an autoverification (AV) system through application of Six Sigma (DMAIC) process improvement strategies.

Letter--Incorporating Real-World Evidence and Patient Value Criteria into Value-Based Frameworks for Relapsed/Refractory Multiple Myeloma.

Orlowski has received research funding from Amgen, BioTheryX, Bristol-Myers Squibb, Celgene Corporation, and Takeda Pharmaceuticals; honoraria from Amgen, Bristol-Myers Squibb, Celgene Corporation, Janssen, Millennium Pharmaceuticals, and Onyx Pharmaceuticals; and is a member of advisory boards for Amgen, Bristol-Myers Squibb, Celgene Corporation, Incyte, Kite, Legend Biotech, Sanofi-Aventis, and Takeda Pharmaceuticals.

Development of a novel radiobromine-labeled sigma-1 receptor imaging probe.

Sigma-1 receptor is a target for tumor imaging. In a previous study, we synthesized a vesamicol analog, (+)-2-[4-(4-bromophenyl)piperidino]cyclohexanol [(+)-pBrV], with a high affinity for sigma-1 receptor, and synthesized radiobrominated (+)-pBrV. This radiobrominated (+)-pBrV showed high tumor uptake in tumor-bearing mice; however, radioactivity accumulation in normal tissues, such as the liver, was high. We assumed that the accumulation of (+)-pBrV in the non-target tissues was partially derived from its...

A sigma factor toolbox for orthogonal gene expression in Escherichia coli.

Synthetic genetic sensors and circuits enable programmable control over timing and conditions of gene expression and, as a result, are increasingly incorporated into the control of complex and multi-gene pathways. Size and complexity of genetic circuits are growing, but stay limited by a shortage of regulatory parts that can be used without interference. Therefore, orthogonal expression and regulation systems are needed to minimize undesired crosstalk and allow for dynamic control of separate modules. This ...

Genetics of familial hypercholesterolemia: a tool for development of novel lipid lowering pharmaceuticals?

Familial hypercholesterolemia is characterized by high LDL cholesterol and an elevated risk to develop coronary heart disease. Mutations in LDL receptor-mediated cholesterol uptake are the main cause of familial hypercholesterolemia. However, multiple mutations in various other genes are also associated with high LDL cholesterol and even familial hypercholesterolemia. Thus, pharmaceuticals that target these genes and proteins might be attractive treatment options to reduce LDL cholesterol. This review provi...

Long story short: an introduction to the short-term and long-term Six Sigma quality and its importance in the laboratory medicine for the management of extra-analytical processes.

There is a compelling need for quality tools that enable effective control of the extra-analytical phase. In this regard, Six Sigma seems to offer a valid methodological and conceptual opportunity, and in recent times, the International Federation of Clinical Chemistry and Laboratory Medicine has adopted it for indicating the performance requirements for non-analytical laboratory processes. However, the Six Sigma implies a distinction between short-term and long-term quality that is based on the dynamics of...

Post-production handling and administration of protein pharmaceuticals and potential instability issues.

The safety and efficacy of protein pharmaceuticals depend not only on biological activity, but also on purity levels. Impurities may be process related due to limitations in manufacturing, or product related caused by protein degradation occurring throughout the life history of a product. Although the pharmaceutical biotechnology industry has made great progress in improving bulk and drug product manufacturing as well as company-controlled storage and transportation conditions to minimize the level of degra...

Reference Values for Spirometry Derived Using Lambda, Mu, Sigma (LMS) Method in Korean Adults: in Comparison with Previous References.

The present study aimed to update the prediction equations for spirometry and their lower limits of normal (LLN) by using the lambda, mu, sigma (LMS) method and to compare the outcomes with the values of previous spirometric reference equations.

Impact of Pharmaceuticals on the Environment: Risk Assessment Using QSAR Modeling Approach.

An extensive use of pharmaceuticals and the widespread practices of their erroneous disposal measures have made these products contaminants of emerging concern (CEC). Especially, active pharmaceutical ingredients (APIs) are ubiquitously detected in surface water and soil, mainly in the aquatic compartment, where they do affect the living systems. Unfortunately, there is a huge gap in the availability of ecotoxicological data on pharmaceuticals' environmental behavior and ecotoxicity which force EMEA (Europe...

A General Strategy for Site-Selective Incorporation of Deuterium and Tritium into Pyridines, Diazines and Pharmaceuticals.

Methods to incorporate deuterium and tritium atoms into organic molecules are valuable for medicinal chemistry. The prevalence of pyridines and diazines in pharmaceuticals means that new ways to label these heterocycles will present opportunities in drug design and facilitate absorption, distribution, metabolism and excretion (ADME) studies. A broadly applicable protocol is presented wherein pyridines, diazines and pharmaceuticals are converted into heterocyclic phosphonium salts and then isotopically label...

Environmental concentrations of pharmaceuticals directly affect phytoplankton and effects propagate through trophic interactions.

Pharmaceuticals are found in freshwater ecosystems where even low concentrations in the range of ng Lmay affect aquatic organisms. In the current study, we investigated the effects of chronic exposure to three pharmaceuticals on two microalgae, a potential modulation of the effects by additional inorganic phosphorus (P) limitation, and a potential propagation of the pharmaceuticals' effect across a trophic interaction. The latter considers that pharmaceuticals are bioaccumulated by algae, potentially metabo...

Point of Care 2.0: Coagulation Monitoring Using Rotem® Sigma and Teg® 6S.

New-generation methods for point of care based coagulation monitoring enable fully automated viscoelastic analyses for the assessment of particular parts of hemostasis. Contrary to the measuring techniques of former models, the viscoelastic ROTEM sigma and TEG 6s analyses are performed in single-use test cartridges without time- and personnel-intensive pre-analytical procedures. This review highlights methodical strengths and limitations of the devices and meets concerns associated with their integration in...

New toxicogenetic insights and ranking of the selected pharmaceuticals belong to the three different classes: A toxicity estimation to confirmation approach.

Tetracycline hydrochloride (TH), indomethacin (IM), and bezafibrate (BF) belong to the three different important classes of pharmaceuticals, which are well known for their toxicity and environmental concerns. However, studies are still elusive to highlight the mechanistic toxicity of these pharmaceuticals and rank them using both, the toxicity prediction and confirmation approaches. Therefore, we employed the next generation toxicity testing in 21st century (TOX21) tools and estimated the in vitro/vivo toxi...

Spatial patterns of pharmaceuticals and wastewater tracers in the Hudson River Estuary.

The widespread use of pharmaceuticals by human populations results in their sustained discharge to surface waters via wastewater treatment plants (WWTPs). In this study, 16 highly prescribed pharmaceuticals were quantified along a 250 km transect of the Hudson River Estuary and New York Harbor to describe their sources and spatial patterns. Sampling was conducted over two dry weather periods in May and July 2016, at 72 sites which included mid-channel and nearshore sites, as well as locations influenced b...

AF710B, an M1/sigma-1 receptor agonist with long-lasting disease-modifying properties in a transgenic rat model of Alzheimer's disease.

AF710B (aka ANAVEX 3-71) is a novel selective allosteric M1 muscarinic and sigma-1 receptor agonist. In 3×Tg-AD mice, AF710B attenuates cognitive deficits and decreases Alzheimer-like hallmarks. We now report on the long-lasting disease-modifying properties of AF710B in McGill-R-Thy1-APP transgenic (Tg) rats.

The Electronic Structure of OsSi Calculated by MS-NEVPT2 with Inclusion of the Relativistic Effects.

The electronic states of \ce{OsSi} are calculated by Multi-State N-Electron Valence State Second Order Perturbation Theory (MS-NEVPT2) with all-electron basis sets. The relativistic effects are considered comprehensively that allows us to identify the $X^{3}\Sigma^-_{0^+}$ ground state. The theoretical equilibrium bond length 2.103 {\AA} is close to the experimental measurement of 2.1207 {\AA} while the vibrational frequency 466 cm$^{-1}$ is smaller than the experimental value of 516 cm$^{-1}$. Two excited ...

Urbanization gradient of selected pharmaceuticals in surface water at a watershed scale.

Ubiquitous detection of pharmaceuticals in the aquatic environment around the world raises a great public concern. Aquatic residuals of pharmaceuticals have been assumed to relate to land use patterns and various human activities within a catchment or watershed. This study generated a gradient of human activity in the Jiulong River watershed, southeastern China by urban land use percentage in 20 research subwatersheds. Thirty-three compounds from three-category pharmaceuticals [26 compounds of 5 antibiotic ...

Advanced oxidation process-mediated removal of pharmaceuticals from water: A review.

Pharmaceuticals, which are frequently detected in natural and wastewater bodies as well as drinking water have attracted considerable attention, because they do not readily biodegrade and may persist and remain toxic. As a result, pharmaceutical residues pose on-going and potential health and environmental risks. To tackle these emerging contaminants, advanced oxidation processes (AOPs) such as photo-Fenton, sonolysis, electrochemical oxidation, radiation and ozonation etc. have been applied to remove pharm...

Pediatric Poisonings: The Risk of Over-the-Counter Pharmaceuticals.

Every week in the United States, 56% of children younger than age 18 years and 82% of adults take at least one medication. Nonprescription medications, including acetaminophen and ibuprofen, are among the most commonly used pharmaceuticals across all age groups. Use of nonprescription medications, traditionally available over-the-counter, has become ubiquitous. Unfortunately, with such abundant use there is an associated risk for therapeutic misuse, intentional misuse, and even abuse. [Pediatr Ann. 2017;46(...

Oxygen uptake rate in alginate producer (algU+) and non-producer (algU-) strains of Azotobacter vinelandii under nitrogen-fixation conditions.

The sigma E (AlgU) in Azotobacter vinelandii has been shown to control the expression of cydR gene, a repressor of genes of the alternative respiratory chain, and alginate has been considered a barrier for oxygen diffusion. Therefore, the aim of the present study was to compare the respiratory activity of an alginate non-producing strain, lacking the sigma factor E (algU-), and polymer producing strains (algU+) of A. vinelandii under diazotrophic conditions at different aeration conditions.

Unveiling the important roles of coexisting contaminants on photochemical transformations of pharmaceuticals: Fibrate drugs as a case study.

Pharmaceuticals are a group of ubiquitous emerging pollutants, many of which have been shown to undergo efficient photolysis in the environment. Photochemically produced reactive intermediates (PPRIs) sensitized by the pharmaceuticals in sunlit natural waters may induce photodegradation of coexisting compounds. In this study, the roles of coexisting contaminants on the phototransformation of pharmaceuticals were unveiled with the fibrate drugs gemfibrozil (GMF), fenofibrate (FNF), and fenofibric acid (FNFA)...


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