T9652

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Showing 1-30 of 109 results for "T9652" within Papers

Quantitative benefit-risk assessment using only qualitative information on utilities.

Ola Caster et al.

Medical decision making : an international journal of the Society for Medical Decision Making, 32(6), E1-15 (2012-09-01)

Utilities of pertinent clinical outcomes are crucial variables for assessing the benefits and risks of drugs, but numerical data on utilities may be unreliable or altogether missing. We propose a method to incorporate qualitative information into a probabilistic decision analysis

H(1)-antihistamines and urticaria: how can we predict the best drug for our patient?

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

Effect of coadministration of single and multiple doses of rifampicin on the pharmacokinetics of fexofenadine enantiomers in healthy subjects.

Hiroyuki Kusuhara et al.

Drug metabolism and disposition: the biological fate of chemicals, 41(1), 206-213 (2012-11-02)

The effect of rifampicin on the pharmacokinetics of fexofenadine enantiomers was examined in healthy subjects who received fexofenadine alone or with single or multiple doses of rifampicin (600 mg). A single coadministered dose of rifampicin significantly decreased the oral clearance

Development and validation of an ultra-performance liquid chromatography method for simultaneous analysis of 20 antihistaminics in dietary supplements.

Jung Yeon Kim et al.

Biomedical chromatography : BMC, 29(3), 465-474 (2014-08-01)

The purpose of this study was to develop and validate an ultra-performance liquid chromatography method for simultaneous analysis of 20 antihistamines (illegal additives) in dietary supplements. The limits of detection and quantitation of the method ranged from 1.5 to 2.5

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

Zhichao Liu et al.

PLoS computational biology, 7(12), e1002310-e1002310 (2011-12-24)

Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI types (hepatotoxic side effects) seen in the clinic can be translated

H1-antihistamines exacerbate high-fat diet-induced hepatic steatosis in wild-type but not in apolipoprotein E knockout mice.

Vineesh V Raveendran et al.

American journal of physiology. Gastrointestinal and liver physiology, 307(2), G219-G228 (2014-05-24)

We examined the effects of two over-the-counter H1-antihistamines on the progression of fatty liver disease in male C57Bl/6 wild-type and apolipoprotein E (ApoE)-/- mice. Mice were fed a high-fat diet (HFD) for 3 mo, together with administration of either cetirizine

Comment: the new macrolide antibiotics and terfenadine.

L M Cortese et al.

The Annals of pharmacotherapy, 26(7-8), 1019-1019 (1992-07-01)

Antihistamines modulate the integrin signaling pathway in h9c2 rat cardiomyocytes: Possible association with cardiotoxicity.

J S Yun et al.

Human & experimental toxicology, 34(8), 796-807 (2014-11-27)

The identification of biomarkers for toxicity prediction is crucial for drug development and safety evaluation. The selective and specific biomarkers for antihistamines-induced cardiotoxicity is not well identified yet. In order to evaluate the mechanism of the life-threatening effects caused by

A pharmacophore hypothesis for P-glycoprotein substrate recognition using GRIND-based 3D-QSAR.

Giovanni Cianchetta et al.

Journal of medicinal chemistry, 48(8), 2927-2935 (2005-04-15)

Trying to understand the complex interactions that substrates and inhibitors have with the efflux transporter P-glycoprotein has been the subject of various publications. In this work, we have confined our study to substrates by picking a diverse set of 129

Adenylate kinase release as a high-throughput-screening-compatible reporter of bacterial lysis for identification of antibacterial agents.

Anna C Jacobs et al.

Antimicrobial agents and chemotherapy, 57(1), 26-36 (2012-10-03)

Adenylate kinase (AK) is a ubiquitous intracellular enzyme that is released into the extracellular space upon cell lysis. We have shown that AK release serves as a useful reporter of bactericidal agent activity and can be exploited for antimicrobial screening

Enhanced systemic exposure of fexofenadine via the intranasal administration of chitosan-coated liposome.

Fu Qiang et al.

International journal of pharmaceutics, 430(1-2), 161-166 (2012-04-25)

The present study aimed to develop the intranasal delivery system of fexofenadine for the prolonged drug release via the preparation of mucoadhesive liposome. By using thin layer film hydration method, liposome of fexofenadine was prepared with DPPC/DPPG, resulting in the

Terfenadine

McTavish D, et al.

Drugs, 39, 552-574 (1990)

Characterization of a highly sensitive and selective novel trapping reagent, stable isotope labeled glutathione ethyl ester, for the detection of reactive metabolites.

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

Targeting TMEM176B Enhances Antitumor Immunity and Augments the Efficacy of Immune Checkpoint Blockers by Unleashing Inflammasome Activation.

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

Inhibitory effects of the antihistamines epinastine, terfenadine, and ebastine on potassium currents in rat ventricular myocytes.

H Ohtani et al.

The Journal of pharmacy and pharmacology, 51(9), 1059-1063 (1999-10-21)

We examined and compared the inhibitory effects of three non-sedating antihistamines, terfenadine, ebastine, and epinastine, on delayed rectifier potassium current (IK) and transient outward potassium current (Ito) of rat isolated ventricular myocytes, using a patch clamp technique. Terfenadine, ebastine and

Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.

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

[Multicenter studies of terfenadine-containing suspensions in children with hayfever].

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)

[Long QT interval. Interaction of terfenadine and itraconazole].

Cornelia Rufke et al.

Medizinische Monatsschrift fur Pharmazeuten, 29(1), 22-24 (2006-02-09)

Development of recombinant cell line co-expressing mutated Nav1.5, Kir2.1, and hERG for the safety assay of drug candidates.

Masato Fujii et al.

Journal of biomolecular screening, 17(6), 773-784 (2012-04-14)

To provide a high-throughput screening method for human ether-a-go-go-gene-related gene (hERG) K(+) channel inhibition, a new recombinant cell line, in which single action potential (AP)-induced cell death was produced by gene transfection. Mutated human cardiac Na(+) channel Nav1.5 (IFM/Q3), which

Poorly soluble marketed drugs display solvation limited solubility.

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

Differential thermodynamic driving force of first- and second-generation antihistamines to determine their binding affinity for human H1 receptors.

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

Different effects of the selective serotonin reuptake inhibitors fluvoxamine, paroxetine, and sertraline on the pharmacokinetics of fexofenadine in healthy volunteers.

Junji Saruwatari et al.

Journal of clinical psychopharmacology, 32(2), 195-199 (2012-03-01)

Although the interaction between selective serotonin reuptake inhibitors (SSRIs) and other drugs is important in the treatment of depression, there have been few studies of SSRIs concerning transporter-mediated interactions in humans. The objective of this study was to evaluate the

Comparative effects of terfenadine and loratadine in the treatment of hay fever.

G Ciprandi et al.

Journal of investigational allergology & clinical immunology, 1(6), 368-372 (1991-12-01)

This double-blind, double-dummy, parallel-group study was undertaken in 40 patients with seasonal allergic rhinoconjunctivitis during the 1990 hay fever season. The patients were randomized and treated for seven days with either 120 mg terfenadine or 10 mg loratadine, each drug

Involvement of unique mechanisms in the induction of scratching behavior in BALB/c mice by compound 48/80.

Naoki Inagaki et al.

European journal of pharmacology, 448(2-3), 175-183 (2002-07-30)

Compound 48/80 induced scratching behavior in BALB/c mice, and the role of mast cell mediators in this behavior was examined. Mouse scratching behavior was detected and evaluated using a new apparatus, MicroAct. Compound 48/80 increased the incidence of scratching behavior

Comparison of nasal steroid with antihistamine in prophylactic treatment against pollinosis using an environmental challenge chamber.

Heizaburo Yamamoto et al.

Allergy and asthma proceedings, 33(5), 397-403 (2012-10-03)

Environmental challenge chambers (ECC) have been used to expose people to pollen allergens within a stable atmosphere and to examine the efficacy of treatment. Although pollinosis is one of the typical IgE-mediated type I allergic diseases, allergic inflammation is thought

Effect of terfenadine on nasal provocation.

R Jankowski et al.

International archives of allergy and immunology, 101(3), 311-317 (1993-01-01)

The effect of premedication with terfenadine, an H1 antagonist, on nasal challenge with antigen, histamine and methacholine was evaluated. A single dose of terfenadine had no effect on the response to a localized challenge with methacholine but completely blocked the

Hypaconitine-induced QT prolongation mediated through inhibition of KCNH2 (hERG) potassium channels in conscious dogs.

Shuilin Xie et al.

Journal of ethnopharmacology, 166, 375-379 (2015-03-25)

Hypaconitine is one of the main aconitum alkaloids in traditional Chinese medicines prepared with herbs from the genus Acotinum. These herbs are widely used for the treatment of cardiac insufficiency and arrhythmias. However, Acotinum alkaloids are known for their toxicity

Terfenadine, a nonsedating antihistamine.

C A Carter et al.

Drug intelligence & clinical pharmacy, 19(11), 812-817 (1985-11-01)

Terfenadine is an antihistamine recently approved for use in the U.S. Terfenadine possesses a unique chemical structure when compared with other antihistamines. It is a selective inhibitor of H1-receptors with little or no anticholinergic, antiserotoninergic, or antiadrenergic effects. Comparative studies

Phase separation in coamorphous systems: in silico prediction and the experimental challenge of detection.

Katja Pajula et al.

Molecular pharmaceutics, 11(7), 2271-2279 (2014-05-16)

Combinatorial chemistry has enabled the production of very potent drugs that might otherwise suffer from poor solubility and low oral bioavailability. One approach to increase solubility is to make the drug amorphous, which leads to problems associated with drug stability.

Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).

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

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