نتایج جستجو برای: unbound aggregate

تعداد نتایج: 49655  

Journal: :The Journal of pharmacology and experimental therapeutics 2011
Yasuo Uchida Sumio Ohtsuki Junichi Kamiie Tetsuya Terasaki

The purpose of this study was to examine whether in vivo drug distribution to the brain can be reconstructed by integrating P-glycoprotein (P-gp)/mdr1a expression levels, P-gp in vitro activity, and drug unbound fractions in mouse plasma and brain. For 11 P-gp substrates, in vitro P-gp transport activities were determined by measuring transcellular transport across monolayers of mouse P-gp-tran...

Journal: :Antimicrobial agents and chemotherapy 2017
Catherine J Byrne Jason A Roberts Brett McWhinney Jerome P Fennell Philomena O'Byrne Evelyn Deasy Sean Egan Ronan Desmond Helen Enright Sheila A Ryder Deirdre M D'Arcy Johnny McHugh

The objective of this study was to explore the following aspects of teicoplanin use in patients with hematological malignancy: early attainment of target trough concentrations with current high-dose teicoplanin regimens, variability in unbound teicoplanin fractions, factors associated with observed total and unbound trough concentrations, efficacy and toxicity, and renal function estimation. Th...

2011
Patricia M. LoRusso Antonio Jimeno Grace Dy Alex Adjei Jordan Berlin Lawrence Leichman Jennifer A. Low Dawn Colburn Ilsung Chang Sravanthi Cheeti Jin Y. Jin Richard A. Graham

Purpose: This study was designed to evaluate whether less frequent dosing [three times per week (TIW) or once weekly (QW)] of 150 mg vismodegib following a loading dose [150 mg once daily (QD) for 11 days] would result in similar safety, tolerability, and steady-state levels of total and unbound vismodegib as continuous QD dosing. Experimental Design: Sixty-seven patients with advanced solid tu...

2012
Michael Knott Robert B. Best

Intrinsically disordered proteins play an important role in cellular signalling, mediated by their interactions with other biomolecules. A key question concerns the nature of their binding mechanism, and whether the bound structure is induced only by proximity to the binding partner. This is difficult to answer through experiment alone because of the very heterogeneous nature of the unbound ens...

Journal: :Drug metabolism and disposition: the biological fate of chemicals 2017
Julia Riede Birk Poller Jörg Huwyler Gian Camenisch

Inhibition of the bile salt export pump (BSEP) has been recognized as a key factor in the development of drug-induced cholestasis (DIC). The risk of DIC in humans has been previously assessed using in vitro BSEP inhibition data (IC50) and unbound systemic drug exposure under assumption of the "free drug hypothesis." This concept, however, is unlikely valid, as unbound intrahepatic drug concentr...

Journal: :Journal of clinical pharmacology 2014
Cecile A Delille Sarah T Pruett Vincent C Marconi Jeffrey L Lennox Wendy S Armstrong Richard F Arrendale Anandi N Sheth Kirk A Easley Edward P Acosta Aswani Vunnava Ighovwerha Ofotokun

HIV-1 protease inhibitors (PIs) exhibit different protein binding affinities and achieve variable plasma and tissue concentrations. Degree of plasma protein binding may impact central nervous system penetration. This cross-sectional study assessed cerebrospinal fluid (CSF) unbound PI concentrations, HIV-1 RNA, and neopterin levels in subjects receiving either ritonavir-boosted darunavir (DRV), ...

ژورنال: آبخیزداری ایران 2020
Sahandi, Khadijeh, Vaezi, Ali Reza,

This study was carried out to investigate the role of soil structure in splash erosion in semi-arid soils. Splash erosion was measured in four soil textures (silty clay loam, sandy clay loam, silt loam and sandy loam) with two soil structure conditions (with natural structure and under aggregate breakdown) using a simulated rainfall with 50 mmh-1 in intensity for 30 min in splash caps with 10-c...

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