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https://www.readbyqxmd.com/read/29143287/lipoic-acid-stimulates-camp-production-in-healthy-control-and-secondary-progressive-ms-subjects
#1
Sarah E Fiedler, Vijayshree Yadav, Amelia R Kerns, Catherine Tsang, Sheila Markwardt, Edward Kim, Rebecca Spain, Dennis Bourdette, Sonemany Salinthone
Lipoic acid (LA) exhibits antioxidant and anti-inflammatory properties; supplementation reduces disease severity and T lymphocyte migration into the central nervous system in a murine model of multiple sclerosis (MS), and administration in secondary progressive MS (SPMS) subjects reduces brain atrophy compared to placebo. The mechanism of action (MOA) of LA's efficacy in suppression of MS pathology is incompletely understood. LA stimulates production of the immunomodulator cyclic AMP (cAMP) in vitro. To determine whether cAMP could be involved in the MOA of LA in vivo, we performed a clinical trial to examine whether LA stimulates cAMP production in healthy control and MS subjects, and whether there are differences in the bioavailability of LA between groups...
November 15, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/29134501/pharmacokinetic-properties-of-saffron-and-its-active-components
#2
Azar Hosseini, Bibi Marjan Razavi, Hossein Hosseinzadeh
Saffron as a medicinal plant has many therapeutic effects. Phytochemical studies have reported that saffron is composed of at least four active ingredients which include crocin, crocetin, picrocrocin and safranal. The carotenoids of saffron are sensitive to oxygen, light, heat and enzymatic oxidization. However, regulation of these factors is required for saffron quality. Some pharmacologic effects of saffron and its active compounds include cardioprotective, neuroprotective, memory enhancer, antidepressant and anxiolytic...
November 13, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29127904/pharmacokinetics-and-brain-uptake-study-of-novel-ampa-receptor-antagonist-perampanel-in-sd-rats-using-a-validated-uhplc-qtof-ms-method
#3
David Paul, Lingesh Allakonda, Amit Sahu, Shruti Surendran, Nanjappan Satheeshkumar
Perampanel (PER) is a novel AMPA receptor antagonist for antiepileptic therapy and is prospective for the treatment of other neurological disorders. A highly sensitive and rapid UHPLC-QTOF-MS method was developed for the quantification of PER in plasma/brain homogenate of SD rat with alogliptin as an internal standard (IS). Chromatographic separation was carried out on an Acquity UPLC HSS Cyano column (100mm×2.1mm, 1.8μm) using gradient mobile phase consisting of 0.1% formic acid and acetonitrile at a flow rate of 0...
November 8, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29126076/a-rapid-and-sensitive-chiral-lc-ms-ms-method-for-the-determination-of-ketamine-and-norketamine-in-mouse-plasma-brain-and-cerebrospinal-fluid-applicable-to-the-stereoselective-pharmacokinetic-study-of-ketamine
#4
Hidetoh Toki, Takuya Ichikawa, Akiko Mizuno-Yasuhira, Jun-Ichi Yamaguchi
A novel method for the rapid and sensitive chiral determination of ketamine and norketamine in mouse plasma, brain and cerebrospinal fluid (CSF) was developed using liquid chromatography-tandem mass spectrometry (LC-MS/MS). This method reduces the required matrix volume, compared with a previously reported chiral assay method for ketamine and norketamine. The method involves the deproteinization of a small amount of biological matrix (corresponding to 5μL of plasma, 10mg of brain, or 2.5μL of CSF) using a water-miscible organic solvent containing (2)H4-norketamine as an internal standard, the direct injection of the organic supernatant into an LC-MS/MS system, chiral separation on a CHIRALPAK AS-3R column (4...
October 7, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29113740/efficacy-of-pritelivir-and-acyclovir-in-the-treatment-of-herpes-simplex-virus-infections-in-a-mouse-model-of-herpes-simplex-encephalitis
#5
Debra C Quenelle, Alexander Birkmann, Thomas Goldner, Tamara Pfaff, Holger Zimmermann, Susanne Bonsmann, Deborah J Collins, Terri L Rice, Mark N Prichard
Pritelivir, a helicase-primase inhibitor, has excellent in vitro and in vivo activity against human herpes simplex virus (HSV). Mice lethally infected with HSV type 1 or 2, including acyclovir-resistant strains, were treated 72 h after infection for 7 days with pritelivir or acyclovir. Both drugs were administered orally twice daily either alone or in combination. Dosages of pritelivir from 0.3 to 30 mg/kg reduced mortality (P < 0.001) against HSV-1, E-377. With an acyclovir resistant HSV-1, 11360, pritelivir at 1 and 3 mg/kg increased survival (P < 0...
November 4, 2017: Antiviral Research
https://www.readbyqxmd.com/read/29109060/cannabinoid-1-receptor-neutral-antagonist-reduces-binge-like-alcohol-consumption-and-alcohol-induced-accumbal-dopaminergic-signaling
#6
Andrea Balla, Bin Dong, Borehalli M Shilpa, Kiran Vemuri, Alexandros Makriyannis, Subhash C Pandey, Henry Sershen, Raymond F Suckow, K Yaragudri Vinod
Binge alcohol (ethanol) drinking is associated with profound adverse effects on our health and society. Rimonabant (SR141716A), a CB1 receptor inverse agonist, was previously shown to be effective for nicotine cessation and obesity. However, studies using rimonabant were discontinued as it was associated with an increased risk of depression and anxiety. In the present study, we examined the pharmacokinetics and effects of AM4113, a novel CB1 receptor neutral antagonist on binge-like ethanol drinking in C57BL/6J mice using a two-bottle choice drinking-in-dark (DID) paradigm...
November 3, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/29106979/development-of-a-population-pharmacokinetic-model-to-predict-brain-distribution-and-dopamine-d2-receptor-occupancy-of-raclopride-in-non-anesthetized-rat
#7
Yin Cheong Wong, Trayana Ilkova, Rob C van Wijk, Robin Hartman, Elizabeth C M de Lange
BACKGROUND: Raclopride is a selective antagonist of the dopamine D2 receptor. It is one of the most frequently used in vivo D2 tracers (at low doses) for assessing drug-induced receptor occupancy (RO) in animals and humans. It is also commonly used as a pharmacological blocker (at high doses) to occupy the available D2 receptors and antagonize the action of dopamine or drugs on D2 in preclinical studies. The aims of this study were to comprehensively evaluate its pharmacokinetic (PK) profiles in different brain compartments and to establish a PK-RO model that could predict the brain distribution and RO of raclopride in the freely moving rat using a LC-MS based approach...
November 4, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29098835/-comparison-of-different-administration-routes-of-saikosaponin-in-plasma-pharmacokinetics-and-brain-pharmacokinetics
#8
Ya-Jie Dai, Xiao-Lan Chen, Hong-Yan Tang, Xian-Yi Deng, Lang Xie
To evaluate the optimum administration routes of saikosaponin in the treatment of epilepsy by comparing the plasma pharmacokinetics and the brain pharmacokinetics after different administration routes of saikosaponin. After receiving saikosaponin in different administration routes, the mice were sacrificed to collect the blood and brain tissues. The acetonitrile and methanol (9∶1) were used to precipitate the plasma protein. The concentration of the SSa in mice plasma and brain was determined by UPLC-MS/MS, and the pharmacokinetic parameters, bioavailability, the brain targeting coefficient (Re) and the brain drug targeting index (DTI) were calculated with Kinetica software...
July 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29089037/revisiting-atenolol-as-a-low-passive-permeability-marker
#9
Xiaomei Chen, Tim Slättengren, Elizabeth C M de Lange, David E Smith, Margareta Hammarlund-Udenaes
BACKGROUND: Atenolol, a hydrophilic beta blocker, has been used as a model drug for studying passive permeability of biological membranes such as the blood-brain barrier (BBB) and the intestinal epithelium. However, the extent of S-atenolol (the active enantiomer) distribution in brain has never been evaluated, at equilibrium, to confirm that no transporters are involved in its transport at the BBB. METHODS: To assess whether S-atenolol, in fact, depicts the characteristics of a low passive permeable drug at the BBB, a microdialysis study was performed in rats to monitor the unbound concentrations of S-atenolol in brain extracellular fluid (ECF) and plasma during and after intravenous infusion...
October 31, 2017: Fluids and Barriers of the CNS
https://www.readbyqxmd.com/read/29080240/design-synthesis-molecular-modeling-and-biological-evaluation-of-novel-amine-based-histone-deacetylase-inhibitors
#10
Pavel A Petukhov, Hazem Abdelkarim, Raghupathi Neelarapu, Antonett Madriaga, Irida Kastrati, Yue-Ting Wang, Aditya S Vaidya, Taha Y Taha, Gregory R J Thatcher, Jonna Frasor
Histone deacetylases (HDACs) are promising drug targets for a variety of therapeutic applications. Here we describe the design, synthesis, biological evaluation in cellular models of cancer, and preliminary drug metabolism and pharmacokinetic studies (DMPK) of a series of secondary and tertiary amine-based HDAC inhibitors. Introduction of an amino group with one or two surface binding groups (SBGs) yielded a successful strategy to develop novel and potent HDAC inhibitors. Secondary amines 2 were found to be generally more potent than the corresponding tertiary amines 3...
October 27, 2017: ChemMedChem
https://www.readbyqxmd.com/read/29079874/study-on-the-effect-of-emd386088-a-5-ht6-receptor-partial-agonist-in-enhancing-the-anti-immobility-action-of-some-antidepressants-in-rats
#11
Magdalena Jastrzębska-Więsek, Agata Siwek, Anna Partyka, Marcin Kołaczkowski, Maria Walczak, Magdalena Smolik, Gniewomir Latacz, Katarzyna Kieć-Kononowicz, Anna Wesołowska
The effect of some antidepressants co-administered with EMD386088 in the modified forced swim test in rats was investigated. Additionally, the pharmacokinetics, metabolic stability, and the effect of EMD386088 on P450 cytochromes were determined. Intraperitoneal (i.p.) coadministration of EMD386088 (2.5 mg/kg) and imipramine (15 mg/kg), reboxetine (5 mg/kg), moclobemide (10 mg/kg), or bupropion (10 mg/kg) evoked significant antidepressant-like activity, whereas no effect was observed after joint administration of EMD386088 with s-citalopram (10 mg/kg)...
October 27, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/29074633/comparison-between-the-prebolus-t1-measurement-and-the-fixed-t1-value-in-dynamic-contrast-enhanced-mr-imaging-for-the-differentiation-of-true-progression-from-pseudoprogression-in-glioblastoma-treated-with-concurrent-radiation-therapy-and-temozolomide-chemotherapy
#12
J G Nam, K M Kang, S H Choi, W H Lim, R-E Yoo, J-H Kim, T J Yun, C-H Sohn
BACKGROUND AND PURPOSE: Glioblastoma is the most common primary brain malignancy and differentiation of true progression from pseudoprogression is clinically important. Our purpose was to compare the diagnostic performance of dynamic contrast-enhanced pharmacokinetic parameters using the fixed T1 and measured T1 on differentiating true from pseudoprogression of glioblastoma after chemoradiation with temozolomide. MATERIALS AND METHODS: This retrospective study included 37 patients with histopathologically confirmed glioblastoma with new enhancing lesions after temozolomide chemoradiation defined as true progression (n = 15) or pseudoprogression (n = 22)...
October 26, 2017: AJNR. American Journal of Neuroradiology
https://www.readbyqxmd.com/read/29067789/the-new-acetylcholinesterase-inhibitors-pc-37-and-pc-48-7-meota-donepezil-like-compounds-characterization-of-their-metabolites-in-human-liver-microsomes-pharmacokinetics-and-in-vivo-formation-of-the-major-metabolites-in-rats
#13
Jana Zdarova Karasova, Martin Mzik, Milos Hroch, Jan Korabecny, Eugenie Nepovimova, Viktor Vorisek, Vladimir Palicka, Kamil Kuca
The objective of this study was to elucidate the pharmacokinetics and metabolite formation of newly developed non-selective AChE/BChE 7-MEOTA-donepezil-like inhibitors for potential therapeutic use in Alzheimer disease patients. The chemical structures of metabolites were defined during incubation with human liver microsomes, and subsequently the metabolization was verified in in vivo study. In vitro metabolic profiling revealed the formation of nine major metabolites in the case of PC-37 and eight metabolites of PC-48...
October 25, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29067345/ponezumab-in-mild-to-moderate-alzheimer-s-disease-randomized-phase-ii-pet-pib-study
#14
Jaren W Landen, Niels Andreasen, Carol L Cronenberger, Pamela F Schwartz, Anne Börjesson-Hanson, Henrik Östlund, Catherine A Sattler, Brendon Binneman, Martin M Bednar
INTRODUCTION: The safety, pharmacokinetics, and effect on peripheral and central amyloid β (Aβ) of multiple doses of ponezumab, an anti-Aβ monoclonal antibody, were characterized in subjects with mild-to-moderate Alzheimer's disease treated for 1 year. METHODS: Subjects were aged ≥50 years with Mini-Mental State Examination scores 16 to 26. Cohort Q was randomized to ponezumab 10 mg/kg (n = 12) or placebo (n = 6) quarterly. Cohort M was randomized to a loading dose of ponezumab 10 mg/kg or placebo, followed by monthly ponezumab 7...
September 2017: Alzheimer's & Dementia: Translational Research & Clinical Interventions
https://www.readbyqxmd.com/read/29066968/prediction-of-a-therapeutic-dose-for-buagafuran-a-potent-anxiolytic-agent-by-physiologically-based-pharmacokinetic-pharmacodynamic-modeling-starting-from-pharmacokinetics-in-rats-and-human
#15
Fen Yang, Baolian Wang, Zhihao Liu, Xuejun Xia, Weijun Wang, Dali Yin, Li Sheng, Yan Li
Physiologically based pharmacokinetic (PBPK)/pharmacodynamic (PD) models can contribute to animal-to-human extrapolation and therapeutic dose predictions. Buagafuran is a novel anxiolytic agent and phase I clinical trials of buagafuran have been completed. In this paper, a potentially effective dose for buagafuran of 30 mg t.i.d. in human was estimated based on the human brain concentration predicted by a PBPK/PD modeling. The software GastroPlus(TM) was used to build the PBPK/PD model for buagafuran in rat which related the brain tissue concentrations of buagafuran and the times of animals entering the open arms in the pharmacological model of elevated plus-maze...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29064811/-the-risk-of-epileptic-seizures-during-antibiotic-therapy
#16
Ewa Czapińska-Ciepiela
Numerous antibiotics may trigger epileptic seizures or status epilepticus by decreasing inhibitory transmission in the brain, thus lowering the seizure threshold. The most potent seizurogenic effect is exerted by penicillins, cephalosporins, fluorochinolons and carbapenems. Predisposing factors that facilitate development of epileptic seizures in the course of antibiotic therapy comprise all conditions accompanied by damage to the blood-brain barrier (including cerebral trauma and encephalitis), a high dose of an antibiotic or lack of adequate dose adjustment in patients with renal failure...
2017: Wiadomości Lekarskie: Organ Polskiego Towarzystwa Lekarskiego
https://www.readbyqxmd.com/read/29058298/pharmacokinetics-and-tolerability-of-oral-dosage-forms-of-huperzine-a-in-healthy-chinese-male-volunteers-a-randomized-single-dose-three-period-six-sequence-crossover-study
#17
San-Lan Wu, Jun Gan, Jing Rao, Si-Jie He, Wen-Wen Zhu, Ying Zhao, Yong-Ning Lv, Jian-Geng Huang, Ya-Ni Liu
Huperzine A is a potent, reversible, and blood-brain barrier permeable acetylcholinesterase inhibitor. The aim of this study was to compare the pharmacokinetics, tolerability, and bioavailability of two formulations with the established reference formulation of huperzine A in a fasting, healthy Chinese male population. This was a randomized, single-dose, 3-period, 6-sequence crossover study. The plasma concentrations of huperzine A were determined by liquid chromatography tandem mass spectrometry. Tolerability was assessed based on subject interview, vital sign monitoring, physical examination, and routine blood and urine tests...
October 2017: Journal of Huazhong University of Science and Technology. Medical Sciences
https://www.readbyqxmd.com/read/29031817/bcrp-abcg2-and-high-alert-medications-biochemical-pharmacokinetic-pharmacogenetic-and-clinical-implications
#18
REVIEW
Daiki Hira, Tomohiro Terada
The human breast cancer resistance protein (BCRP/ABCG2) is an ATP-binding cassette efflux transporter that uses ATP hydrolysis to expel xenobiotics from cells, including anti-cancer medications. It is expressed in the gastrointestinal tract, liver, kidney, and brain endothelium. Thus, ABCG2 functions as a tissue barrier to drug transport that strongly influences the pharmacokinetics of substrate medications. Genetic polymorphisms of ABCG2 are closely related to inter-individual variations in therapeutic performance...
October 13, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29019022/distribution-of-lacosamide-in-the-rat-brain-assessed-by-in-vitro-slice-technique
#19
Zsolt Gáll, Szende Vancea
Lacosamide is a newer anticonvulsant and is the only one that enhances the slow inactivation of voltage gated sodium channels. It is also claimed to have disease-modifying potential, but its pharmacokinetic properties have been much less discussed in the literature. In rats, lacosamide shows restricted distribution to tissues, and the brain-to-plasma partition coefficient (Kp) is only 0.553. In this study, the brain disposition of lacosamide was evaluated in rat brains, and its neuropharmacokinetic parameters (i...
October 10, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28980221/cardiopulmonary-bypass-in-the-newborn-effects-of-circulatory-cell-free-hemoglobin-and-hyperoxia-evaluated-in-a-novel-rat-pup-model
#20
Åsa Jungner, Suvi Vallius, Matteo Bruschettini, Olga Romantsik, Magnus Gram, David Ley
BACKGROUND: Infants with congenital heart defects (CHD) are at risk for white matter brain injury. This novel rat pup model characterizes the systemic effects of intravasal cell-free hemoglobin and hyperoxia, hypothesizing that immature endogenous scavenging systems relate to increased vulnerability to conditions present during cardiopulmonary bypass (CPB). METHODS: Plasma pharmacokinetics of cell-free human hemoglobin (Hb) was determined after intraperitoneal (i...
October 4, 2017: Intensive Care Medicine Experimental
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