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Showing 1-30 of 109 results for "T9652" within Papers
Jenny M Pedersen et al.
Journal of medicinal chemistry, 51(11), 3275-3287 (2008-05-07)
The chemical space of registered oral drugs was explored for inhibitors of the human multidrug-resistance associated protein 2 (MRP2; ABCC2), using a data set of 191 structurally diverse drugs and drug-like compounds. The data set included a new reference set
Zachary Barrett-O'Keefe et al.
Experimental physiology, 98(1), 268-277 (2012-08-01)
A sustained postexercise vasodilatation, which is histamine receptor mediated, has been observed following single bouts of whole-body exercise, but the mechanisms that regulate activation of histamine receptors following exercise are undefined. Exploration of vasodilatation after small muscle-mass dynamic or resistance
Lei Jia et al.
Bioorganic & medicinal chemistry, 16(11), 6252-6260 (2008-05-02)
Drug-induced long QT syndrome (LQTS) can cause critical cardiovascular side effects and has accounted for the withdrawal of several drugs from the market. Blockade of the potassium ion channel encoded by the human ether-a-go-go-related gene (hERG) has been identified as
Motoi Tobita et al.
Bioorganic & medicinal chemistry letters, 15(11), 2886-2890 (2005-05-25)
HERG attracts attention as a risk factor for arrhythmia, which might trigger torsade de pointes. A highly accurate classifier of chemical compounds for inhibition of the HERG potassium channel is constructed using support vector machine. For two test sets, our
Maria Zeniou et al.
PloS one, 10(8), e0134793-e0134793 (2015-08-14)
Cancer stem-like cells reside in hypoxic and slightly acidic tumor niches. Such microenvironments favor more aggressive undifferentiated phenotypes and a slow growing "quiescent state" which preserves them from chemotherapeutic agents that essentially target proliferating cells. Our objective was to identify
Aurélie Periat et al.
Journal of chromatography. A, 1356, 211-220 (2014-07-16)
In this study, the influence of electrospray ionization (ESI) source design on the overall sensitivity achieved in hydrophilic interaction chromatography (HILIC) and reversed phase liquid chromatography (RPLC), was investigated. State-of-the-art triple quadrupole mass analyzers from AB Sciex, Agilent Technologies and
Girish Hari Chaudhari et al.
Journal of pharmacological and toxicological methods, 67(2), 115-120 (2013-01-29)
Recent studies have shown the utility of adult zebrafish ECG (electrocardiogram) in assessing drug-induced QTc prolongation. While the method has significant advantages over current ECG animal models including ethical issues, low compound requirement and expense, adoption of the method into
Filomain Nguemo et al.
Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology, 29(5-6), 819-832 (2012-05-23)
Cardiac dysfunction is one of the main cause of drug candidate failures in the preclinical and/or clinical studies and responsible for the retraction of large number of drugs from the market. The prediction of arrhythmic risk based on preclinical trials
[Treatment with terfenadine and ketoconazole or itraconazole can cause torsades de pointes ventricular tachycardia].
S Pohjola-Sintonen
Duodecim; laaketieteellinen aikakauskirja, 109(2), 164-166 (1993-01-01)
Torsades de pointes induced by erythromycin and terfenadine.
D G Paris et al.
The American journal of emergency medicine, 12(6), 636-638 (1994-11-01)
Shigeru Hishinuma et al.
Biochemical pharmacology, 91(2), 231-241 (2014-07-30)
Differential binding sites for first- and second-generation antihistamines were indicated on the basis of the crystal structure of human histamine H1 receptors. In this study, we evaluated differences between the thermodynamic driving forces of first- and second-generation antihistamines for human
J N van den Anker et al.
Nederlands tijdschrift voor geneeskunde, 141(41), 1976-1978 (1998-04-29)
Doctors who prescribe drugs should be aware not only of potential drug-drug interactions, but also of potential food-drug interactions. In particular, the ingestion of grapefruit juice leads to enhanced systemic bioavailability of terfenadine and of several important and frequently prescribed
Minjoo Kim et al.
PloS one, 10(3), e0119519-e0119519 (2015-03-18)
Existing data on the association between being overweight and cardiovascular morbidity and mortality risk in adults are inconsistent. We prospectively and longitudinally investigated the effects of weight on arterial stiffness and plasma metabolites in middle-aged subjects (aged 40-55 years). A
Laurent Soulère et al.
Bioorganic & medicinal chemistry letters, 20(15), 4355-4358 (2010-07-10)
A virtual screening, involving flexible docking sequences within the LuxR, TraR and LasR binding sites, was used as a structural binding sites similarity filter to specifically target conserved residues in the proteins of the LuxR family (namely Tyr62, Trp66, Tyr70
Syed Mashhood Ali et al.
Magnetic resonance in chemistry : MRC, 50(4), 299-304 (2012-03-15)
Complexation of fexofenadine with α-cyclodextrin in aqueous medium was studied. The stoichiometry of the resulting inclusion complex was determined by (1) H NMR titration data. 2D ROESY data provided the evidence of formation of the complex by entry of the
Christel A S Bergström et al.
Journal of medicinal chemistry, 50(23), 5858-5862 (2007-10-13)
We determined the intrinsic aqueous solubility of 15 poorly soluble drugs with solubilities ranging from 2.9 nM to 1.1 microM. We then analyzed the data from a physicochemical perspective, using experimentally determined solid-state properties and easily interpretable two-dimensional molecular descriptors
Eunyoung Lee et al.
Drug metabolism and disposition: the biological fate of chemicals, 43(8), 1250-1253 (2015-06-07)
Cytochrome P450 2J2 (CYP2J2) is an enzyme responsible for the metabolism of endogenous substrates including arachidonic acid, as well as therapeutic drugs such as albendazole, astemizole, ebastine, and terfenadine. Selective inhibitors of CYP2J2 are essential for P450 reaction phenotyping studies.
Giulia Caron et al.
Journal of medicinal chemistry, 48(9), 3269-3279 (2005-04-29)
Growing interest in the use of both the logarithm of the partition coefficient of the neutral species in the alkane/water system (log P(N)(alk)) and the difference between log P(N)(oct) (the logarithm of the partition coefficient of the neutral species in
Reema Abu Khalaf et al.
European journal of medicinal chemistry, 45(4), 1598-1617 (2010-02-02)
Cholesteryl ester transfer protein (CETP) is involved in trafficking lipoprotein particles and neutral lipids between HDL and LDL and therefore is considered a valid target for treating dyslipidemic conditions and complications. Pharmacophore modeling and quantitative structure-activity relationship (QSAR) analysis were
David G Covell
PloS one, 7(10), e44631-e44631 (2012-10-12)
Studies into the genetic origins of tumor cell chemoactivity pose significant challenges to bioinformatic mining efforts. Connections between measures of gene expression and chemoactivity have the potential to identify clinical biomarkers of compound response, cellular pathways important to efficacy and
Johannes Kornhuber et al.
Journal of medicinal chemistry, 51(2), 219-237 (2007-11-22)
Some organic weak bases induce a detachment from inner lysosomal membranes and subsequent inactivation of acid sphingomyelinase (ASM) and thus work as functional ASM inhibitors. The aim of the present investigation was to develop a structure-property-activity relation (SPAR) model in
M Taglialatela et al.
Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology, 29 Suppl 3, 182-189 (1999-08-12)
Despite the enormous success of second generation antihistamines, in the mid-1980s, about 10 years after their introduction in the market, several reports appeared in the literature indicating the rare occurrence of a form of polymorphic ventricular dysrhythmia, the 'torsade de
Boram Lee et al.
Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association, 70, 94-99 (2014-05-03)
CYP2J2 enzyme is highly expressed in human tumors and carcinoma cell lines, and epoxyeicosatrienoic acids, CYP2J2-mediated metabolites, have been implicated in the pathologic development of human cancers. To identify a CYP2J2 inhibitor, 50 natural products obtained from plants were screened
Dipy M Vasa et al.
Journal of pharmaceutical sciences, 103(9), 2911-2923 (2014-05-16)
Fifteen model drugs were quenched from 3:1 (w/w) mixtures with polyethylene glycol 4000 (PEG4000). The resulting solids were characterized using powder X-ray diffraction (PXRD), analysis of pair distribution function-transformed PXRD data (where appropriate), hot-stage polarized light microscopy, and differential scanning
M K Church et al.
Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology, 42(10), 1423-1429 (2012-09-22)
Urticaria, and especially chronic spontaneous urticaria (CSU), is a difficult condition to treat. Consequently, clinicians need to use the best H(1)-antihistamines currently available and the pharmaceutical industries need to keep developing H(1)-antihistamines that are more effective than the ones we
Comment: the new macrolide antibiotics and terfenadine.
L M Cortese et al.
The Annals of pharmacotherapy, 26(7-8), 1019-1019 (1992-07-01)
Mercedes Segovia et al.
Cancer cell, 35(5), 767-781 (2019-05-16)
Although immune checkpoint blockers have yielded significant clinical benefits in patients with different malignancies, the efficacy of these therapies is still limited. Here, we show that disruption of transmembrane protein 176B (TMEM176B) contributes to CD8+ T cell-mediated tumor growth inhibition by
Toshikazu Yamaoka et al.
Journal of pharmacological and toxicological methods, 76, 83-95 (2015-09-01)
Glutathione (GSH) trapping assays are widely used to predict the post-marketing risk for idiosyncratic drug reactions (IDRs) in the pharmaceutical industry. Although several GSH derivatives have been introduced as trapping reagents for reactive intermediates, more sensitive and selective reagents are
L Endre et al.
Orvosi hetilap, 139(1), 11-15 (1998-02-07)
Authors treated 50 seasonal allergic rhinitis ragweed sensitive patients with a second generation antihistamine, terfenadine containing suspension given twice/day for two weeks in the weeds season of 1996. Nasal (rhinorrhoea, stuffed nose, sneezing, itching) and eye symptoms (hyperaemia, itching, tearing)
Jing Yuan et al.
Nature chemical biology, 5(10), 765-771 (2009-09-08)
Studies of gene function and molecular mechanisms in Plasmodium falciparum are hampered by difficulties in characterizing and measuring phenotypic differences between individual parasites. We screened seven parasite lines for differences in responses to 1,279 bioactive chemicals. Hundreds of compounds were
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