Abstract null null Erythropoiesis is a complex physiological process by which erythroid progenitors proliferate and differentiate into nonnucleated red blood cells. Several methods can be used to monitor in vitro the differentiation of erythroid precursors, and hence the toxic effects of drugs, chemicals, or pollutants. One of the most commonly available assay of erythropoiesis is the microscopic observation of differentiated cells after benzidine staining, which forms a blue complex with hemogl...
Abstract null null Allergic conjunctivitis is one of the most common immune diseases in the field of ophthalmology. The number of patients suffering from allergic conjunctivitis has been increasing, and there is still a strong need for development of therapeutic agents for this disease. In drug development, the utmost important point to improve the success probability is to accurately single out good compounds in the early stage of drug development. Therefore, drug efficacy evaluations in the no...
Last. Ikhlas A. Khan(University of Mississippi)H-Index: 51
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Abstract null null The high throughput method using dansyl cysteamine (HTS-DCYA™) is a sensitive and rapid in chemico approach to characterize skin sensitizers' thiol-reactivity. The direct quantification of fluorescent hapten-DCYA adducts facilitates the rapid testing of pure chemicals as well as mixtures. Poor solubility in acetonitrile was occasionally observed and can represent a limitation. To enable the range of solvent options compatible with the testing, the effect of binary solvent syst...
Abstract null null Introduction null For reliable identification of cardiac safety risk, compounds should be screened for activity on cardiac ion channels in addition to hERG, including NaV1.5 and CaV1.2. We identified different parameters that might affect IC50s of compounds on NaV1.5 peak and late currents recorded using automated patch clamp (APC) and suggest outlines for best practices. null null null Methods null APC instruments SyncroPatch 384 and Patchliner were used to record NaV1.5 peak...
Abstract null null Depressed right ventricular ejection fraction (RVEF) has clear prognostic significance in patients with pulmonary arterial hypertension (PAH). Accordingly, improvements in RVEF represent a desirable end-point in the development of PAH therapies. However, current methods for determination of RVEF require measurement of RV volume and are relatively complex and costly. Here, we validate a novel method for quantitative estimation of RVEF in rats based entirely upon analysis of rea...
Abstract null null A new approach is described for quantifying cholinergic receptor activation status human blood samples, based on M1 receptor-driven mobilization of intracellular calcium stores. The assay identifies anticholinergic as well as agonist cholinergic receptor activity. As a cell-based procedure, the assay shares the high efficiency of recently developed M1 receptor binding protocols, but differs from the latter in relying on fluorescence rather than radioactivity measurements. The ...
Abstract null null Opioid receptors are divided into the three classical types: MOP(μ:mu), DOP(δ:delta) and KOP(κ:kappa) that are naloxone-sensitive and an additional naloxone-insensitive nociceptin/orphanin FQ(N/OFQ) peptide receptor(NOP). Studies to determine opioid receptor location and turnover variably rely on; (i) measuring receptor mRNA, (ii) genetically tagging receptors, (iii) labelling receptors with radioligands, (iv) use of antibodies in immunohistochemistry/Western Blotting or (v) m...
Nasal drug administration has been identified as a potential alternative to oral drug administration, especially for systemic delivery of large molecular weight compounds. Major advantages of nasal drug delivery include high vascularity and permeability of the epithelial membranes as well as circumvention of first-pass metabolism. RPMI 2650 cell layers (in vitro cell model) and excised sheep nasal mucosal tissues (ex vivo sheep model) were evaluated with regard to epithelial thickness, selected ...
#1Süleyman Bodur(YTU: Yıldız Technical University)H-Index: 7
#2Sezin Erarpat(YTU: Yıldız Technical University)H-Index: 7
Last. Sezgin Bakırdere(TÜBA: Turkish Academy of Sciences)H-Index: 25
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Abstract null null In the present study, a novel analytical method for the determination of hydroxychloroquine sulfate in human serum and urine samples was established. One step derivatization and dispersive liquid-liquid microextraction (DLLME) was developed for quantitative determination of hydroxychloroquine sulfate in aqueous samples. Hydroxychloroquine sulfate was first hydrolyzed and converted to its benzoate derivative by adding benzoyl chloride in chloroform which also served as extracti...
#1Dhwanil A. Dalwadi(UNTHSC: University of North Texas Health Science Center)H-Index: 3
#2Stephanie Kim(UTMB: The University of Texas Medical Branch at Galveston)
Last. Seongcheol Kim(UNTHSC: University of North Texas Health Science Center)
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The Sigma-1 receptor (S1R) is an endoplasmic reticulum (ER) chaperone protein that has been implicated in attenuating inflammatory stress-mediated brain injuries. Selective S1R agonists represent a new class of therapeutic agent for treating neuropsychiatric and neurodegenerative disorders, however, to date, no S1R ligand has been approved for therapeutic purposes. We used three potential methods on known and potential S1R ligands to develop an unambiguous high-throughput cell screen for S1R act...
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