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https://www.readbyqxmd.com/read/28100102/pharmacokinetics-and-tissue-distribution-of-crotonoside
#1
Peiao Yan, Lan Zhang, Cheng Peng, Ruoqi Zhang
1. Crotonoside is a bioactive ingredient from Croton Herba with a strong antitumour activity. This study aimed to develop a highly sensitive and selective high-performance liquid chromatography (HPLC) method to quantify crotonoside in biological samples for pharmacokinetics and distribution studies. 2. Protein precipitation by perchloric acid was used to separate crotonoside from the biological samples, and the recovery rates for crotonoside and the internal standard (luteoloside) were  >80%. All calibration curves examining the crotonoside levels in plasma and tissues were linear (all correlation coefficients > 0...
January 19, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28098336/preclinical-evaluation-of-intravenous-nax-810-2-a-novel-galr2-preferring-analog-for-anticonvulsant-efficacy-and-pharmacokinetics
#2
Cameron S Metcalf, Brian D Klein, Daniel R McDougle, Liuyin Zhang, Dan Kaufmann, Grzegorz Bulaj, H Steve White
OBJECTIVE: Potential clinical utility of galanin or peptidic analogs has been hindered by poor metabolic stability, lack of brain penetration, and hyperglycemia due to galanin receptor subtype 1 (GalR1) activation. NAX 810-2, a galanin receptor subtype 2 (GalR2)-preferring galanin analog, possesses 15-fold greater affinity for GalR2 over GalR1 and protects against seizures in the mouse 6 Hz, corneal kindling, and Frings audiogenic seizure models. The purpose of these studies was to further evaluate the preclinical efficacy and pharmacokinetics of NAX 810-2 in mice...
January 18, 2017: Epilepsia
https://www.readbyqxmd.com/read/28097866/pharmacokinetics-and-biodistribution-of-the-illegal-food-colorant-rhodamine-b-in-rats
#3
Yung-Yi Cheng, Tung-Hu Tsai
The International Agency for Research on Cancer (IARC) demonstrated rhodamine B as a potential carcinogen in 1978. Nevertheless, rhodamine B has been illegally used as a colorant in food in many countries. Few pharmacokinetic and toxicological investigations have been performed since the first pharmacokinetic study on rhodamine B in 1961. The aims of this study were to develop a simple and sensitive high performance liquid chromatography method with fluorescence detection for the quantitative detection of rhodamine B in the plasma and organs of rats and to estimate its pharmacokinetics and biodistribution...
January 18, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28092695/absorption-distribution-and-excretion-of-the-anti-tuberculosis-drug-delamanid-in-rats-extensive-tissue-distribution-suggests-potential-therapeutic-value-for-extrapulmonary-tuberculosis
#4
Masakazu Shibata, Yoshihiko Shimokawa, Katsunori Sasahara, Noriaki Yoda, Hiroyuki Sasabe, Mitsunari Suzuki, Ken Umehara
Delamanid (OPC-67683, Deltyba(TM) , nitro-dihydro-imidazooxazoles derivative) is approved for the treatment of adult pulmonary multidrug-resistant tuberculosis. The absorption, distribution, and excretion of delamanid-derived radioactivity were investigated after a single oral administration of (14) C-delamanid at 3 mg/kg to rats. In both male and female rats, radioactivity in blood and all tissues reached peak levels by 8 or 24 hours postdose, and thereafter decreased slowly. Radioactivity levels were 3- to 5-fold higher in lung tissue at time to maximum concentration compared with plasma...
January 16, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28070719/sunitinib-paracetamol-sex-divergent-pharmacokinetics-and-tissue-distribution-drug-drug-interaction-in-mice
#5
Ming Hui Liew, Salby Ng, Chii Chii Chew, Teng Wai Koo, Yun Lee Chee, Evelyn Li-Ching Chee, Pilar Modamio, Cecilia Fernández, Eduardo L Mariño, Ignacio Segarra
The sex-divergent pharmacokinetics and interaction of tyrosine kinase inhibitor sunitinib with paracetamol was evaluated in male and female mice. Mice (control groups) were administered 60 mg/kg PO sunitinib alone or with 200 mg/kg PO paracetamol (study groups). Sunitinib concentration in plasma, brain, kidney and liver were determined and non-compartmental pharmacokinetic analysis performed. Female control mice showed 36% higher plasma sunitinib AUC0→∞, 31% and 27% lower liver and kidney AUC0→∞ and 2...
January 9, 2017: Investigational New Drugs
https://www.readbyqxmd.com/read/28065587/ffpm-a-pde4-inhibitor-reverses-learning-and-memory-deficits-in-app-ps1-transgenic-mice-via-camp-pka-creb-signaling-and-anti-inflammatory-effects
#6
Haibiao Guo, Yufang Cheng, Canmao Wang, Jingang Wu, Zhengqiang Zou, Bo Niu, Hui Yu, Haitao Wang, Jiangping Xu
Thus far, phosphodiesterase-4 (PDE4) inhibitors have not been approved for application in Alzheimer's disease (AD) in a clinical setting due to severe side effects, such as nausea and vomiting. In this study, we investigated the effect of FFPM, a novel PDE4 inhibitor, on learning and memory abilities, as well as the underlying mechanism in the APP/PS1 mouse model of AD. Pharmacokinetic studies have revealed that FFPM efficiently permeates into the brain, and reached peak values in plasma 2 h after orally dosing...
January 6, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28012176/selection-and-early-clinical-evaluation-of-the-brain-penetrant-11%C3%AE-hydroxysteroid-dehydrogenase-type-1-11%C3%AE-hsd1-inhibitor-ue2343-xanamem-tm
#7
Scott P Webster, Andrew McBride, Margaret Binnie, Karen Sooy, Jonathan R Seckl, Ruth Andrew, T David Pallin, Hazel J Hunt, Trevor R Perrior, Vincent S Ruffles, J William Ketelbey, Alan Boyd, Brian R Walker
BACKGROUND AND PURPOSE: Reducing glucocorticoid exposure in the brain via intracellular inhibition of the cortisol-regenerating enzyme 11β-hydroxysteroid dehydrogenase (11β-HSD1) has emerged as a therapeutic strategy to treat cognitive impairment in early Alzheimer's disease (AD). We sought to discover novel, brain-penetrant 11β-HSD1 inhibitors as potential medicines for the treatment of AD. EXPERIMENTAL APPROACH: Medicinal chemistry optimisation of a series of amido-thiophene analogues was performed to identify potent and selective 11β-HSD1 inhibitors with optimised oral pharmacokinetics able to access the brain...
December 23, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27992940/pharmacokinetics-of-a-standardized-extract-of-centella-asiatica-eca-233-in-rats
#8
Tosapol Anukunwithaya, Mayuree H Tantisira, Boonyong Tantisira, Phisit Khemawoot
ECa 233, a standardized extract of Centella asiatica, has been found to exhibit various positive neurological effects and to have a good safety profile. The present study aimed to explore the disposition kinetics of ECa 233, containing madecassoside (53.1 %) and asiaticoside (32.3 %), in rats. The extract was intravenously or orally administered at doses from 50 to 200 mg/kg. Plasma, tissues, urine, and feces were collected at time points from 0 to 48 h after dosing. The levels of madecassoside and asiaticoside, as well as their postulated triterpenic metabolites, madecassic acid and asiatic acid, in biological samples, were simultaneously measured by liquid chromatography-tandem mass spectrometry...
December 19, 2016: Planta Medica
https://www.readbyqxmd.com/read/27984094/selegiline-induces-a-wake-promoting-effect-in-rats-which-is-related-to-formation-of-its-active-metabolites
#9
Christoffer Bundgaard, Liliana P Montezinho, Neil Anderson, Christian Thomsen, Arne Mørk
The goal of the present work was to characterise the effects of selegiline on the rat sleep pattern. Furthermore, for comparative purposes, the pharmacokinetics of selegiline and its metabolites in brain and plasma were investigated, and microdialysis experiments were performed to examine the resulting effect on dopamine, noradrenaline and serotonin levels. Selegiline (1, 5, 10 and 30mg/kg) was found to dose-dependently increase the time spent awake following acute dosing. The pharmacokinetic assessment of selegiline showed that, following an oral dose of 5mg/kg, low circulating levels of the parent compound were found relative to those of biotransformed l-methamphetamine and l-amphetamine...
October 28, 2016: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/27936965/avp-786-for-the-treatment-of-agitation-in-dementia-of-the-alzheimer-s-type
#10
Ricardo P Garay, George T Grossberg
Agitation is common and distressing in patients with Alzheimer-type dementia, but safe, effective treatments remain elusive. Psychological treatments are first-line options, but they have limited efficacy. Off-label psychotropic medications are frequently used, but they also have limited effectiveness, and their use may have harmful side effects, including death. Areas covered: This review discusses the history leading to the conception of AVP-786 (deuterated (d6)-dextromethorphan/quinidine), its pharmacokinetic and pharmacodynamic profiles and safety issues, together with an overview of recent clinical trials...
January 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/27928655/in-vivo-pharmacokinetics-of-puerarin-via-different-drug-administration-routes-based-on-middle-cerebral-artery-occlusion-model
#11
Pengyue Li, Jie Bai, Boyu Dong, Yang Lu, Shengwei Zhang, Shuang Guo, Ning Tan, Mengdi Zhao, Shouying Du, Puning Cao
BACKGROUND AND OBJECTIVES: Pueraria labata has traditionally been applied in the treatment of stroke in Chinese clinics. Puerarin is the key ingredient in it for brain protection effect. To find a superior administration route for puerarin in the treatment of ischemic cerebrovascular disease, the pharmacokinetics of puerarin based on the middle cerebral artery occlusion (MCAO) rat via different administration routes were studied and compared. METHODS: Ten rats (MCAO model) divided into two groups were treated with puerarin via intravenous and intranasal routes...
December 7, 2016: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27864744/a-generic-multi-compartmental-cns-distribution-model-structure-for-9-drugs-allows-prediction-of-human-brain-target-site-concentrations
#12
Yumi Yamamoto, Pyry A Välitalo, Dirk-Jan van den Berg, Robin Hartman, Willem van den Brink, Yin Cheong Wong, Dymphy R Huntjens, Johannes H Proost, An Vermeulen, Walter Krauwinkel, Suruchi Bakshi, Vincent Aranzana-Climent, Sandrine Marchand, Claire Dahyot-Fizelier, William Couet, Meindert Danhof, Johan G C van Hasselt, Elizabeth C M de Lange
PURPOSE: Predicting target site drug concentration in the brain is of key importance for the successful development of drugs acting on the central nervous system. We propose a generic mathematical model to describe the pharmacokinetics in brain compartments, and apply this model to predict human brain disposition. METHODS: A mathematical model consisting of several physiological brain compartments in the rat was developed using rich concentration-time profiles from nine structurally diverse drugs in plasma, brain extracellular fluid, and two cerebrospinal fluid compartments...
November 18, 2016: Pharmaceutical Research
https://www.readbyqxmd.com/read/27845049/a-novel-role-for-pht1-in-the-disposition-of-l-histidine-in-brain-in-vitro-slice-and-in-vivo-pharmacokinetic-studies-in-wildtype-and-pht1-null-mice
#13
Xiao-Xing Wang, Yongjun Hu, Richard F Keep, Noriko Toyama-Sorimachi, David E Smith
PHT1 (SLC15A4) is responsible for translocating l-histidine (l-His), di/tripeptides and peptide-like drugs across biological membranes. Previous studies have indicated that PHT1 is located in brain parenchyma, however, its role and significance in brain along with effect on the biodistribution of substrates is unknown. In this study, adult gender-matched Pht1-competent (wildtype) and Pht1-deficient (null) mice were used to investigate the effect of PHT1 on l-His brain disposition via in vitro slice and in vivo pharmacokinetic approaches...
January 15, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27836941/target-site-investigation-for-the-plasma-prolactin-response-mechanism-based-pharmacokinetic-pharmacodynamic-analysis-of-risperidone-and-paliperidone-in-the-rat
#14
Shinji Shimizu, Sandra M den Hoedt, Victor Mangas Sanjuan, Sinziana Cristea, Jana K Geuer, Dirk-Jan van den Berg, Robin Hartman, Francisco Bellanti, Elizabeth C M de Lange
In order to understand the drivers in the biological system response to dopamine D2 receptor antagonists, a mechanistic semi-physiologically-based (PB) pharmacokinetic-pharmacodymanic (PKPD) model was developed to describe prolactin responses to risperidone (RIS) and its active metabolite paliperidone (PAL). A microdialysis study in rats was performed to obtain detailed plasma, brain extracellular fluid (brainECF), and cerebrospinal fluid (CSF) concentrations of PAL and RIS. To assess the impact of P-gp functioning on brain distribution, experiments were performed in absence or presence of the P-glycoprotein (P-gp) inhibitor tariquidar (TQD)...
November 11, 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/27830575/neuropharmacology-of-3-4-methylenedioxypyrovalerone-mdpv-its-metabolites-and-related-analogs
#15
Michael H Baumann, Mohammad O Bukhari, Kurt R Lehner, Sebastien Anizan, Kenner C Rice, Marta Concheiro, Marilyn A Huestis
3,4-Methylenedioxypyrovalerone (MDPV) is a psychoactive component of so-called bath salts products that has caused serious medical consequences in humans. In this chapter, we review the neuropharmacology of MDPV and related analogs, and supplement the discussion with new results from our preclinical experiments. MDPV acts as a potent uptake inhibitor at plasma membrane transporters for dopamine (DAT) and norepinephrine (NET) in nervous tissue. The MDPV formulation in bath salts is a racemic mixture, and the S isomer is much more potent than the R isomer at blocking DAT and producing abuse-related effects...
November 10, 2016: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/27810560/intranasal-delivery-of-ciprofloxacin-to-rats-a-topical-approach-using-a-thermoreversible-in-situ-gel
#16
Joana Sousa, Gilberto Alves, Paula Oliveira, Ana Fortuna, Amílcar Falcão
Intranasal administration of antibiotics is an alternative and attractive delivery approach in the treatment of local infections such as chronic rhinosinusitis. This topical route has the advantage of delivering high drug concentrations directly to the site of infection when trying to eradicate the highly resistant bacterial biofilms. The purpose of this study was to assess and compare the pharmacokinetic parameters of ciprofloxacin following intranasal and intravenous administrations to rats in plasma, olfactory bulb and nasal mucosa of two different nasal regions...
January 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27803466/comparative-physicochemical-and-pharmacokinetic-properties-of-quetiapine-and-its-active-metabolite-norquetiapine
#17
Dong-Wook Kim, Kwon-Yeon Weon, Eon-Pyo Hong, Eun Kyoung Chung, Kyung-Tae Lee
Quetiapine (QTP) is an atypical antipsychotic drug commonly used to treat several psychiatric disorders and is metabolized into the active metabolite norquetiapine (NQTP). This study was designed to evaluate and compare the physicochemical properties, metabolic stability, brain distribution, and pharmacokinetics of QTP and NQTP. Compared to QTP, NQTP had a higher pKa, solubility, and rat liver microsomal stability, optimal log D and similar log P values. For pharmacokinetic evaluation, QTP and NQTP were administered orally and intravenously to rats at various doses...
2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27799216/efavirenz-is-predicted-to-accumulate-in-brain-tissue-an-in-silico-in-vitro-and-in-vivo-investigation
#18
Paul Curley, Rajith K R Rajoli, Darren M Moss, Neill J Liptrott, Scott Letendre, Andrew Owen, Marco Siccardi
Adequate concentrations of efavirenz in the central nervous system (CNS) are necessary to suppress viral replication, but high concentrations may increase the likelihood of CNS adverse drug reactions. The aim of this investigation was to evaluate the efavirenz distribution in the cerebrospinal fluid (CSF) and the brain by using a physiologically based pharmacokinetic (PBPK) simulation for comparison with rodent and human data. The efavirenz CNS distribution was calculated using a permeability-limited model on a virtual cohort of 100 patients receiving efavirenz (600 mg once daily)...
January 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27785749/revealing-the-neuroendocrine-response-after-remoxipride-treatment-using-multi-biomarker-discovery-and-quantifying-it-by-pk-pd-modeling
#19
Willem J van den Brink, Yin C Wong, Berfin Gülave, Piet H van der Graaf, Elizatbeth C M de Lange
To reveal unknown and potentially important mechanisms of drug action, multi-biomarker discovery approaches are increasingly used. Time-course relationships between drug action and multi-biomarker profiles, however, are typically missing, while such relationships will provide increased insight in the underlying body processes. The aim of this study was to investigate the effect of the dopamine D2 antagonist remoxipride on the neuroendocrine system. Different doses of remoxipride (0, 0.7, 5.2, or 14 mg/kg) were administered to rats by intravenous infusion...
January 2017: AAPS Journal
https://www.readbyqxmd.com/read/27775094/pharmacokinetic-comparison-between-quercetin-and-quercetin-3-o-%C3%AE-glucuronide-in-rats-by-uhplc-ms-ms
#20
Le-Le Yang, Na Xiao, Xiao-Wei Li, Yong Fan, Raphael N Alolga, Xiao-Yue Sun, Shi-Lei Wang, Ping Li, Lian-Wen Qi
Quercetin is a natural flavonoid widely distributed in human diet and functional foods. Quercetin 3-O-β-glucuronide (Q3G) is present in wine and some medicinal plants. Quercetin and Q3G may be metabolized from each other in vivo. While quercetin has been the subject of many studies, the pharmacokinetic profiles of quercetin and Q3G (in animals) have not yet been compared. Herein, we prepared a column-based method for rapid isolation of Q3G from Nelumbo nucifera. Then, we developed an UHPLC-MS/MS method to compare the pharmacokinetics of quercetin and Q3G...
October 24, 2016: Scientific Reports
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