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pharmacokinetics, rat

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https://www.readbyqxmd.com/read/28429212/experimental-study-of-a-radiopharmaceutical-agent-based-on-modified-fatty-acid-labeled-with-technetium-99m
#1
S I Sazonova, Yu N Il'yushenkova, Yu B Lishmanov, S V Tsibul'nikov, V S Skuridin, E A Nesterov, N V Varlamova, E A Il'ina, V D Filimonov, M V Belyanin, E V Stepanova, S M Minin
Using rat model of coronary occlusion, we studied pharmacokinetics and the efficiency of a new radiopharmaceutical agent (99m)Tc-PDA-DTPA intended for diagnostics of changes in myocardial metabolism and its analogue (123)I-PMPDA. (99m)Tc-PDA-DTPA was eliminated mostly by the kidneys and maximal concentration in the heart was attained within 60 min after intravenous injection; no accumulation in the area of myocardial infarction was observed. The studied substance was inferior to its analogue 123I-PMPDA by the quality of scintigraphic visualization of the heart...
April 20, 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28426176/uhplc-ms-ms-method-for-the-simultaneous-quantitation-of-five-anthraquinones-and-gallic-acid-in-rat-plasma-after-oral-administration-of-prepared-rhubarb-decoction-and-its-application-to-a-pharmacokinetic-study-in-normal-and-acute-blood-stasis-rats
#2
Hui Zhu, Xiao Liu, Ting Ting Zhu, Xiao Li Wang, Kun Ming Qin, Ke Pei, Bao Chang Cai
Prepared rhubarb, as one of the main processed products of rhubarb, has a good effect on promoting blood circulation. This paper described a rapid, sensitive and selective ultra-fast liquid chromatography with tandem mass spectrometry method for simultaneous quantification of five anthraquinones (rhein, aloe-emodin, chrysophanol, emodin and physcion) and gallic acid in plasma. Chromatographic separation was performed on an Extend C18 column at the temperature of 30°C using the mobile phase consisted of 0.1% aqueous formic acid and acetonitrile...
April 20, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28422508/nitrile-in-the-hole-discovery-of-a-small-auxiliary-pocket-in-neuronal-nitric-oxide-synthase-leading-to-the-development-of-potent-and-selective-2-aminoquinoline-inhibitors
#3
Maris A Cinelli, Huiying Li, Georges Chreifi, Thomas L Poulos, Richard B Silverman
Neuronal nitric oxide synthase (nNOS) inhibition is a promising strategy to treat neurodegenerative disorders, but the development of nNOS inhibitors is often hindered by poor pharmacokinetics. We previously developed a class of membrane-permeable 2-aminoquinoline inhibitors and later rearranged the scaffold to decrease off-target binding. However, the resulting compounds had decreased permeability, low human nNOS activity, and low selectivity versus human eNOS. In this study, 5-substituted phenyl ether-linked aminoquinolines and derivatives were synthesized and assayed against purified NOS isoforms...
April 19, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28421119/influences-of-realgar-indigo-naturalis-a-traditional-chinese-medicine-formula-on-the-main-cyp450-activities-in-rats-using-a-cocktail-method
#4
Huan-Hua Xu, Fei-Ran Hao, Mei-Xi Wang, Si-Jia Ren, Ming Li, Hong-Ling Tan, Yu-Guang Wang, Xiang-Lin Tang, Cheng-Rong Xiao, Qian-De Liang, Yue Gao, Zeng-Chun Ma
The purpose of this work was to study the influences of Realgar-Indigo naturalis (RIF) and its principal element realgar on 4 main cytochrome P450 enzymes activities in rats. A simple and efficient cocktail method was developed to detect the four probe drugs simultaneously. In this study, Wistar rats were administered intragastric RIF and realgar for 14 days; mixed probe drugs were injected into rats by caudal vein. Through analyzing the pharmacokinetic parameter of mixed probe drugs in rats, we can calculate the CYPs activities...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/28419964/effects-of-paeonia-emodi-on-hepatic-cytochrome-p450-cyp3a2-and-cyp2c11-expression-and-pharmacokinetics-of-carbamazepine-in-rats
#5
Mohammad Raish, Ajaz Ahmad, Khalid M Alkharfy, Basit L Jan, Kazi Mohsin, Abdul Ahad, Fahad I Al-Jenoobi, Abdullah M Al-Mohizea
Herbal medicines, dietary supplements, and other foods may pharmacokinetically and/or pharmacodynamically interact with carbamazepine (CBZ), which could lead to potential clinical consequences. Paeonia emodi (PE) is one of the herbs used as complementary therapy in the treatment of epileptic patients in some cultures, and may also be co-administered with CBZ. This study evaluates the effects of PE on the pharmacokinetics of CBZ and determines a possible mechanism of interaction. Rats were administered vehicle saline or PE (200mg/kg, p...
April 15, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28418637/development-and-application-of-an-msall-based-approach-for-the-quantitative-analysis-of-linear-polyethylene-glycols-in-rat-plasma-by-liquid-chromatography-triple-quadrupole-time-of-flight-mass-spectrometry
#6
Xiaotong Zhou, Xiangjun Meng, Longmei Cheng, Chong Su, Yantong Sun, Lingxia Sun, Zhaohui Tang, John Paul Fawcett, Yan Yang, Jingkai Gu
Polyethylene glycols (PEGs) are synthetic polymers composed of repeating ethylene oxide subunits. They display excellent biocompatibility and are widely used as pharmaceutical excipients. To fully understand the biological fate of PEGs requires accurate and sensitive analytical methods for their quantitation. Application of conventional liquid chromatography-tandem mass spectrometry (LC-MS/MS) is difficult because PEGs have polydisperse molecular weights (MWs) and tend to produce multicharged ions in-source resulting in innumerable precursor ions...
April 18, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28416614/modeling-combined-immunosuppressive-and-anti-inflammatory-effects-of-dexamethasone-and-naproxen-in-rats-predicts-the-steroid-sparing-potential-of-naproxen
#7
Xiaonan Li, Debra C DuBois, Dawei Song, Richard R Almon, William J Jusko, Xijing Chen
Dexamethasone (DEX), a widely prescribed corticosteroid (CS), has long been the cornerstone for the treatment of inflammation and immunological dysfunctions in Rheumatoid Arthritis (RA). The CS are frequently used in combination with other anti-rheumatic agents such as nonsteroidal anti-inflammatory drugs (NSAIDs) and disease-modifying anti-rheumatic drugs (DMARDs) to mitigate disease symptoms and minimize unwanted effects. The steroid dose-sparing potential of the NSAID naproxen (NPX) was explored with in vitro and in vivo studies...
April 17, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28415449/complementary-approaches-for-the-evaluation-of-biocompatibility-of-90-y-labeled-superparamagnetic-citric-acid-fe-er-3o4-coated-nanoparticles
#8
Bratislav Antic, Marko Boskovic, Jasmina Nikodinovic-Runic, Yue Ming, Hongguo Zhang, Emil S Bozin, Drina Janković, Vojislav Spasojevic, Sanja Vranjes-Djuric
Magnetic nanoparticles (MNPs) are of immense interest for diagnostic and therapeutic applications in medicine. Design and development of new iron oxide-based MNPs for such applications is of rather limited breadth without reliable and sensitive methods to determine their levels in body tissues. Commonly used methods, such as ICP, are quite problematic, due to the inability to decipher the origin of the detected iron, i.e. whether it originates from the MNPs or endogenous from tissues and bodily fluids. One of the approaches to overcome this problem and to increase reliability of tracing MNPs is to partially substitute iron ions in the MNPs with Er...
June 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
https://www.readbyqxmd.com/read/28415020/simultaneous-determination-of-ten-bioactive-constituents-of-sanjie-zhentong-capsule-in-rat-plasma-by-ultra-high-performance-liquid-chromatography-tandem-mass-spectrometry-and-its-application-to-a-pharmacokinetic-study
#9
Jiachun Li, Dongpo Li, Youzhi Pan, Jun-Hua Hu, Wenzhe Huang, Zhen-Zhong Wang, Wei Xiao, Yu Wang
Sanjie Zhentong capsule, a well-known traditional Chinese medicine prescription, are used for the treatment of endometriosis-related diseases. In this study, a simple, rapid and sensitive ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method was developed for the simultaneous determination of ten bioactive constituents, including peimine, peiminine, peimisine, loureirin A, loureirin B, 7,4'-dihydroxyflavone, pterostilbene, ginsenoside Rg1, ginsenoside Rb1, and notoginsenoside R1 in rat plasma after oral administration of Sanjie Zhentong capsule...
March 9, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28413326/effect-of-b-complex-vitamins-on-the-antifatigue-activity-and-bioavailability-of-ginsenoside-re-after-oral-administration
#10
Yin Bin Chen, Yu Fang Wang, Wei Hou, Ying Ping Wang, Sheng Yuan Xiao, Yang Yang Fu, Jia Wang, Si Wen Zheng, Pei He Zheng
BACKGROUND: Both ginsenoside Re and B-complex vitamins are widely used as nutritional supplements. They are often taken together so as to fully utilize their antifatigue and refreshing effects, respectively. Whether actually a drug-nutrient interaction exists between ginsenoside Re and B-complex vitamins is still unknown. The objective of this study was to simultaneously investigate the effect of B-complex vitamins on the antifatigue activity and bioavailability of ginsenoside Re after their oral administration...
April 2017: Journal of Ginseng Research
https://www.readbyqxmd.com/read/28412296/impact-of-higher-order-heme-degradation-products-on-hepatic-function-and-hemodynamics
#11
Raphael A Seidel, Thierry Claudel, Franziska A Schleser, Navin K Ojha, Matthias Westerhausen, Sandor Nietzsche, Christoph Sponholz, Frans Cuperus, Sina M Coldewey, Stefan H Heinemann, Georg Pohnert, Michael Trauner, Michael Bauer
BACKGROUND& AIMS: While, traditionally, biliverdin and bilirubin are considered end products of heme catabolism, there is evidence for further degradation to diverse bioactive products. As such, Z-BOX A and Z-BOX B arise upon oxidation with unknown implications for hepatocellular function and integrity. We studied the impact of Z-BOX A and B on hepatic functions and explored their alterations in health and cholestatic conditions. METHODS: Functional implications and mechanisms were investigated in rats, hepatocytic HepG2 and HepaRG cells, human immortalized hepatocytes, and isolated perfused livers...
April 12, 2017: Journal of Hepatology
https://www.readbyqxmd.com/read/28411632/an-ultra-specific-and-sensitive-sandwich-elisa-for-imatinib-using-two-anti-imatinib-antibodies
#12
Tetsuya Saita, Yuta Yamamoto, Kazuhisa Hosoya, Yutaro Yamamoto, Sakiko Kimura, Yutaka Narisawa, Masashi Shin
The development of an immunoassay for a low-molecular-weight drug first requires the identification of specific antibodies that do not cross-react with the drug's metabolites. If two antibodies can simultaneously recognize the entire structure of the drug, we can then utilize them to establish an ultra-specific sandwich ELISA, free from interference due to the metabolic products of the drug. This paper reports an ultra-specific and sensitive sandwich ELISA for determination of the tyrosine kinase inhibitor imatinib using two anti-imatinib antibodies...
May 29, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/28411455/identification-of-3-substituted-6-1-1h-1-2-3-triazolo-4-5-b-pyrazin-1-yl-ethyl-quinoline-derivatives-as-highly-potent-and-selective-mesenchymal-epithelial-transition-factor-c-met-inhibitors-via-metabolite-profiling-based-structural-optimization
#13
Fei Zhao, Le-Duo Zhang, Yu Hao, Na Chen, Rui Bai, Yu-Ji Wang, Chun-Chun Zhang, Gong-Sheng Li, Li-Jun Hao, Chen Shi, Jing Zhang, Yu Mao, Yi Fan, Guang-Xin Xia, Jian-Xin Yu, Yan-Jun Liu
c-Met/HGF signaling pathway plays an important role in cancer progression, and it was considered to be related to poor prognosis and drug resistance. Based on metabolite profiling of (S)-7-fluoro-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-1H-imidazo[4,5-b]pyrazin-1-yl)ethyl)quinoline (1), a series of 2-substituted or 3-substituted-6-(1-(1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)ethyl)quinoline derivatives was rationally designed and evaluated. Most of the 3-substituted derivatives not only exhibited potent activities in both enzymatic and cellular assays, but also were stable in liver microsomes among different species (human, rat and monkey)...
April 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28411279/characterization-and-interspecies-scaling-of-rhtnf-%C3%AE-pharmacokinetics-with-minimal-physiologically-based-pharmacokinetic-mpbpk-models
#14
Xi Chen, Debra C DuBois, Richard R Almon, William J Jusko
Tumor necrosis factor-α (TNF-α) is a soluble cytokine and target of specific monoclonal antibodies (mAbs) and other biological agents used for the treatment of inflammatory diseases. These biologics exert their pharmacological effects through binding and neutralizing TNF-α, and thus prevent TNF-α from interacting with its cell surface receptors. The magnitude of pharmacological effects is governed not only by the pharmacokinetics of mAbs, but also the kinetic fate of TNF-α. We have examined the pharmacokinetics of rhTNF-α in rats at low doses and quantitatively characterized its pharmacokinetic features with a minimal physiologically-based pharmacokinetic (mPBPK) model...
April 14, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28408153/refinement-of-the-oral-exposure-description-in-the-cyclic-siloxane-pbpk-model-for-rats-and-humans-implications-for-exposure-assessment
#15
Jerry L Campbell, Melvin E Andersen, Cynthia Van Landingham, Robinan Gentry, Elke Jensen, Jean Y Domoradzki, Harvey J Clewell
The multi-compound, and multi-dose (MC-MD) route physiologically based pharmacokinetic (PBPK) model for cyclic siloxanes reported by McMullin et al. (2016) brought together the series of models for octamethylcyclotetrasiloxane (D4) and decamethylcyclopentasiloxane (D5) in rat and human into a unified code structure that would allow simulation of both compounds following the inhalation and dermal routes of exposure. The refined MC-MD PBPK model presented here expands upon this effort to include representation of rat kinetic data in plasma, tissues and exhaled breath for the parent compounds after oral bolus administration...
April 10, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28406043/cardioprotective-effect-of-magnetic-hydrogel-nanocomposite-loaded-n-%C3%AE-l-rhamnopyranosyl-vincosamide-isolated-from-moringa-oleifera-leaves-against-doxorubicin-induced-cardiac-toxicity-in-rats-in-vitro-and-in-vivo-studies
#16
Mostafa Cheraghi, Mehrdad Namdari, Hadis Daraee, Babak Negahdari, Hammed T Aiyelabegan
Cardioprotective effect of N, α-L-rhamnopyranosyl vincosamide (VR), isolated from the leaves of Moringa oleifera plant in doxorubicin-induced cardiac toxicity rats was evaluated. Twelve (12) rats were randomly selected into 3 groups; 2 rats received distilled water in the control group, 5 rats in group I received varying concentration of VR treatment, and group II containing 5 rats received varying concentration of VR-loaded magnetic hydrogel nanocomposite. Malondialdehyde (MDA), glutathione peroxidase (GSH) and superoxide dismutase (SOD) enzymes activities level were analysed after two weeks...
April 13, 2017: Journal of Microencapsulation
https://www.readbyqxmd.com/read/28404688/brain-disposition-of-cis-para-methyl-4-methylaminorex-cis-4-4-dmar-and-its-potential-metabolites-after-acute-and-chronic-treatment-in-rats-correlation-with-central-behavioral-effects
#17
Jacopo Lucchetti, Claudio Marcello Marzo, Alice Passoni, Angelo Di Clemente, Federico Moro, Renzo Bagnati, Marco Gobbi, Luigi Cervo
Para-methyl-4-methylaminorex (4,4'-DMAR) is a phenethylamine derivative with psychostimulant activity, whose abuse has been associated with several deaths and a wide range of adverse effects. We recently validated an HPLC-MS/MS method to measure the compound's concentrations in plasma, and applied it to describe the pharmacokinetic properties after single dose in rats. In this study we investigated the brain disposition and metabolism of cis-4,4'-DMAR after intraperitoneal injection, and its central behavioral effects...
April 12, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28403743/nonclinical-profile-of-blz-100-a-tumor-targeting-fluorescent-imaging-agent
#18
Julia Parrish-Novak, Kelly Byrnes-Blake, Narine Lalayeva, Stefanie Burleson, Janean Fidel, Rhonda Gilmore, Pamela Gayheart-Walsten, Gregory A Bricker, William J Crumb, K S Tarlo, Stacey Hansen, Valorie Wiss, Errol Malta, William S Dernell, James M Olson, Dennis M Miller
BLZ-100 is a single intravenous use, fluorescent imaging agent that labels tumor tissue to enable more complete and precise surgical resection. It is composed of a chlorotoxin peptide covalently bound to the near-infrared fluorophore indocyanine green. BLZ-100 is in clinical development for intraoperative visualization of human tumors. The nonclinical safety and pharmacokinetic (PK) profile of BLZ-100 was evaluated in mice, rats, canines, and nonhuman primates (NHP). Single bolus intravenous administration of BLZ-100 was well tolerated, and no adverse changes were observed in cardiovascular safety pharmacology, PK, and toxicology studies in rats and NHP...
March 2017: International Journal of Toxicology
https://www.readbyqxmd.com/read/28403574/determination-of-artemisitene-in-rat-plasma-by-uplc-ms-ms-and-its-application-in-pharmacokinetics
#19
Lilan Wu, Yunshan Wu, Weiying Chen, Wen Zhou, Lipeng Tang, Ben Li, Bo Liu
RATIONALE: Artemisitene showed a wide variety of pharmacological activities, such as antioxidant protection in vitro and in vivo. It has been identified as a novel Nrf2 inducer. However, there is no report on an UPLC-MS/MS method to quantitate artemisitene in rat plasma and its application on pharmacokinetic profile study. METHODS: An ACQUITY UPLC(TM) BEH Symmetry ShieldRP18 column (1.7 µm, 2.1 mm × 100 mm) was used with a flow rate of 0.3 mL · min(-1) ...
April 12, 2017: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/28402755/distribution-of-fcrn-across-species-and-tissues
#20
Sari Latvala, Bjoern Jacobsen, Michael B Otteneder, Annika Herrmann, Sven Kronenberg
The neonatal Fc receptor (FcRn) is a major histocompatibility complex class I type molecule that binds to, transports, and recycles immunoglobulin G (IgG) and albumin, thereby protecting them from lysosomal degradation. Therefore, besides the knowledge of FcRn affinity, FcRn protein expression is critical in understanding the pharmacokinetic behavior of Fc-containing biotherapeutics such as monoclonal antibodies. The goal of this investigation was to achieve for the first time a comparative assessment of FcRn distribution across a variety of tissues and species...
April 1, 2017: Journal of Histochemistry and Cytochemistry: Official Journal of the Histochemistry Society
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