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https://www.readbyqxmd.com/read/28213761/psychomotor-effect-differences-between-l-methamphetamine-and-d-methamphetamine-are-independent-of-murine-plasma-and-brain-pharmacokinetics-profiles
#1
Tetsuya Nishimura, Kazue Takahata, Yuri Kosugi, Takaaki Tanabe, Shizuko Muraoka
l-Methamphetamine has been occasionally referred to as a stimulant similar to d-methamphetamine, probably owing to insufficient comparative studies. Here, we directly compared psychomotor efficacies and pharmacokinetics of methamphetamine enantiomers in mice. Only d-methamphetamine, but not l-methamphetamine, induced stereotypy and sensitization at 1-10 mg/kg. However, plasma pharmacokinetic parameters of 10 mg/kg l-methamphetamine were ≥tenfold those of 1 mg/kg d-methamphetamine. These results clearly indicate that differential psychomotor efficacies of methamphetamine enantiomers are independent of their pharmacokinetic profiles...
February 17, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28213295/determination-of-imm-h004-a-novel-neuroprotective-agent-in-rat-plasma-and-brain-tissue-by-liquid-chromatography-tandem-mass-spectrometry
#2
Ziqian Zhang, Xiangmeng Wu, Manman Zhao, Yakun Yang, Yan Wang, Jinping Hu, Baolian Wang, Li Sheng, Yan Li
A rapid and sensitive liquid chromatography-tandem mass spectrometry method for determination of IMM-H004, a novel neuroprotective agent, in rat plasma and brain was developed. Plasma and brain tissue homogenate samples containing IMM-H004 and propranolol (internal standard, IS) were prepared by using a direct protein precipitation of acetonitrile. Separation was carried out in Zorbax SB-C18 column at a flow rate of 0.3mL/min utilizing acetonitrile/water as mobile phases which contain 0.5% formic acid (v/v)...
February 6, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28199114/curcumin-loaded-blood-stable-polymeric-micelles-for-enhancing-therapeutic-effect-on-erythroleukemia
#3
Feirong Gong, Dan Chen, Xin Teng, Junhua Ge, Xianfeng Ning, Ya-Ling Shen, Jian Li, Shanfeng Wang
Curcumin has high potential in suppressing many types of cancer and overcoming multi-drug resistance in a multi-faceted manner by targeting diverse molecular targets. However, the rather low systemic bioavailability resulted from its extremely low aqueous solubility and rapid metabolism and excretion in vivo has hampered its application in cancer therapy. With the primary aim to increase the aqueous solubility of curcumin while retaining its stability in the blood circulation before it accesses the tumor site, here we report preparation of curcumin-loaded N-(tert-butoxycarbonyl)-L-phenylalanine end-capped methoxy-poly(ethylene glycol)-block-poly(ε-caprolactone) (mPEG-PCL-Phe(Boc)) micelles with high stability both in vitro and in vivo and anti-tumor efficacy...
February 15, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28193520/mdr1a-plays-a-crucial-role-in-regulating-the-analgesic-effect-and-toxicity-of-aconitine-by-altering-its-pharmacokinetic-characteristics
#4
Lijun Zhu, Jinjun Wu, Min Zhao, Wenjie Song, Xiaoxiao Qi, Ying Wang, Linlin Lu, Zhongqiu Liu
Aconitine (AC) is the primary bioactive/toxic alkaloid in plants of the Aconitum species. Our previous study demonstrated that Mdr1 was involved in efflux of AC. However, the mechanism by which Mdr1 regulates the efficacy/toxicity of AC in vivo remains unclear. The present study aimed to determine the effects of Mdr1a on the efficacy/toxicity and pharmacokinetics of AC in wild-type and Mdr1a(-/-) FVB mice. After oral administration of AC, significantly higher analgesic effect was observed in Mdr1a(-/-) mice (49% to 105%) compared to wild-type mice (P<0...
February 11, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28192085/influence-of-peptide-transporter-2-pept2-on-the-distribution-of-cefadroxil-in-mouse-brain-a-microdialysis-study
#5
Xiaomei Chen, Richard F Keep, Yan Liang, Hao-Jie Zhu, Margareta Hammarlund-Udenaes, Yongjun Hu, David E Smith
Peptide transporter 2 (PEPT2) is a high-affinity low-capacity transporter belonging to the proton-coupled oligopeptide transporter family. Although many aspects of PEPT2 structure-function are known, including its localization in choroid plexus and neurons, its regional activity in brain, especially extracellular fluid (ECF), is uncertain. In this study, the pharmacokinetics and regional brain distribution of cefadroxil, a ß-lactam antibiotic and PEPT2 substrate, were investigated in wildtype and Pept2 null mice using in vivo intracerebral microdialysis...
February 10, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28190755/quantitative-prediction-of-histamine-h1-receptor-occupancy-by-the-sedative-and-non-sedative-antagonists-in-the-human-central-nervous-system-based-on-systemic-exposure-and-preclinical-data
#6
Kayoko Kanamitsu, Yoshitane Nozaki, Yoko Nagaya, Yuichi Sugiyama, Hiroyuki Kusuhara
Significant histamine H1 receptor occupation in the central nervous system (CNS) is associated with sedation. Here we examined the time profiles of the H1 receptor occupancy (RO) in the CNS using sedative (diphenhydramine and ketotifen) and non-sedative (bepotastine and olopatadine) antagonists at their therapeutic doses by integrating in vitro and animal data. A pharmacokinetic model was constructed to associate plasma concentrations and receptor binding in the brain. Dissociation and association rate constants with the H1 receptor and plasma and brain unbound fractions were determined in vitro...
November 18, 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28178362/determination-of-the-neuropharmacological-drug-nodakenin-in-rat-plasma-and-brain-tissues-by-liquid-chromatography-tandem-mass-spectrometry-application-to-pharmacokinetic-studies
#7
Yingshi Song, Huiyu Yan, Jingbo Xu, Hongxi Ma
A rapid and sensitive liquid chromatography tandem mass spectrometry detection using SRM in positive ionization mode was developed and validated for the quantification of nodakenin in rat plasma and brain. Pareruptorin A was used as internal standard. A single step liquid-liquid extraction was used for plasma and brain sample preparation. The method was validated with respect to selectivity, precision, accuracy, linearity, limit of quantification, recovery, matrix effect and stability. Lower limit of quantification of nodakenin was 2...
February 8, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28167558/pharmacokinetic-and-tissue-distribution-of-benznidazole-after-oral-administration-in-mice
#8
Luísa Perin, Rodrigo Moreira da Silva, Kátia da Silva Fonseca, Jamille Mirelle de Oliveira Cardoso, Fernando Augusto Siqueira Mathias, Levi Eduardo Soares Reis, Israel Molina, Rodrigo Correa-Oliveira, Paula Melo de Abreu Vieira, Cláudia Martins Carneiro
Specific chemotherapy using Benznidazole (BNZ) for Chagas disease during the chronic stage is controversial due to its limited efficacy and toxic effects. Although BNZ has been used to treat Chagas disease since the 1970s, few studies about the biodistribution of this drug exist. In this study, BNZ tissue biodistribution in a murine model and its pharmacokinetic profile in plasma were monitored. A bioanalytical high-performance liquid chromatography with an ultraviolet detector (HPLC-UV) method was developed and validated according to the European Medicines Agency for quantification of BNZ in organs and plasma samples prepared by liquid-liquid extraction using ethyl acetate...
February 6, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28165806/enhancing-both-oral-bioavailability-and-brain-penetration-of-puerarin-using-borneol-in-combination-with-preparation-technologies
#9
Tao Yi, Dandan Tang, Fan Wang, Jiqiong Zhang, Jiao Zhang, Jirui Wang, Xiaoyu Xu, Jifen Zhang
Now there are few good oral preparations of puerarin used in cerebrovascular diseases because of its poor oral absorption caused by the low water solubility and the poor penetration into brain. In this study, three oral formulations of puerarin, nanocrystals suspension (NCS), inclusion compounds solution (ICS) and self-microemulsifying drug delivery system (SMEDDS) were prepared with borneol as an oral brain-targeting enhancer. A rat syngeneic in vitro model of the brain-blood barrier (BBB) was established to investigate effects of borneol on the permeability of puerarin across the BBB...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28140519/structural-insights-into-anticancer-activity-of-d-ring-modified-estrone-derivatives-using-their-lipophilicity-in-estimation-of-sar-and-molecular-docking-studies
#10
Jovana Trifunović, Vladan Borčić, Saša Vukmirovic, Momir Mikov
PURPOSE: Many forms of breast carcinoma are hormone-dependent and therefore development of novel aromatase inhibitors is of particular interest. Since brain metastases are frequent in patients with advanced breast carcinoma, one of the goals of modern drug development is the discovery of drugs with specific pharmacokinetic profile. METHODS: HPTLC is often used to determine lipophilicity of the molecules based on their retention constant. As a predictive analysis, multiple linear regression method was performed in order to connect pharmacokinetic dependent parameters with independent physicochemical properties such are: RM(0) , TPSA and Mw of fourteen D-ring modified estrone derivatives...
January 31, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28139838/rolapitant-absolute-bioavailability-and-pet-imaging-studies-in-healthy-adult-volunteers
#11
X Wang, Z Y Zhang, D Powers, J Wang, S Lu, V Kansra
Rolapitant, a selective, long-acting neurokinin-1 (NK-1) receptor antagonist, demonstrated efficacy in preventing chemotherapy-induced nausea and vomiting (CINV) in patients receiving highly or moderately emetogenic chemotherapy. Two studies in healthy volunteers evaluated 1) absolute bioavailability and 2) NK-1 receptor occupancy of oral rolapitant. Absolute bioavailability, determined by the ratio of dose-normalized exposure following a 180-mg oral dose vs. an intravenous microdose, was approximately 100%...
January 31, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28137817/pharmacokinetics-of-the-novel-echinocandin-cd101-in-multiple-animal-species
#12
Voon Ong, Kenneth D James, Steven Smith, B Radha Krishnan
CD101 is a novel semi-synthetic echinocandin with antifungal activity against Candida and Aspergillus spp. The PK of CD101 administered intravenously to mice, rats, dogs, cynomolgus monkeys, and chimpanzees are presented. CD101 consistently exhibited very low clearance, modest volume of distribution, and long half-life across all species tested. In mouse, rat, dog, cynomolgus monkey, and chimpanzee, CD101 clearance [mL/min/kg] was 0.10, 0.47, 0.30, 0.41, and 0.06; Vss [mL/kg] was 206, 1390, not determined, 597, and 400; and t1/2 [h] was 25, 39, 53, 40, and 81, respectively...
January 30, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28129817/-dalbavancin-pharmacokinetic-and-pharmacodynamic-parameters
#13
José Ramón Azanza, Belén Sádaba, Joana Reis
Dalbavancin is a new lipoglycopeptide antibiotic whose structure influences its pharmacokinetic profile. It is not absorbed after oral administration and is therefore administered intravenously. It is distributed through intracellular fluid, reaching adequate concentrations in the skin, bone, blister fluid and synovial fluid. Plasma protein binding is very high. Concentrations in brain tissue and cerebrospinal fluid (CSF) are inadequate. Excretion is through non-microsomal metabolism with inactive metabolites and through the kidneys by glomerular filtration...
January 2017: Enfermedades Infecciosas y Microbiología Clínica
https://www.readbyqxmd.com/read/28127624/oxycodone-self-administration-in-male-and-female-rats
#14
Maria Mavrikaki, Marco Pravetoni, Sarah Page, David Potter, Elena Chartoff
RATIONALE: Oxycodone is one of the most widely prescribed painkillers in the USA. However, its use is complicated by high abuse potential. As sex differences have been described in drug addiction, the present study tested for sex differences in intravenous oxycodone self-administration in rats. METHODS: Male and female Sprague-Dawley rats were implanted with jugular vein catheters and trained to self-administer oxycodone (0.03 mg/kg/infusion) under fixed ratio 1 (FR1), FR2, and FR5 schedules of reinforcement followed by a dose-response study to assess sensitivity to the reinforcing effects of oxycodone...
January 27, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28120486/a-phase-i-randomized-proof-of-clinical-mechanism-study-assessing-the-pharmacokinetics-and-pharmacodynamics-of-the-oral-pde9a-inhibitor-bi-409306-in-healthy-male-volunteers
#15
Katja Boland, Viktoria Moschetti, Chantaratsamon Dansirikul, Solen Pichereau, Lien Gheyle, Frank Runge, Heike Zimdahl-Gelling, Michael Sand
OBJECTIVE: Cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase (PDE) inhibitors are hypothesized to improve cognition in schizophrenia and Alzheimer disease by increasing cGMP levels in certain brain regions. This phase I, randomized, parallel-group, double-blind, placebo-controlled study provides proof-of-mechanism evidence for BI 409306, a novel, oral PDE9A inhibitor. METHODS: In healthy males, exposure of BI 409306 (25-, 50-, 100-, and 200-mg single dose) and placebo was assessed in plasma and cerebrospinal fluid (CSF)...
January 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28100102/pharmacokinetics-and-tissue-distribution-of-crotonoside
#16
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
#17
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...
February 2017: Epilepsia
https://www.readbyqxmd.com/read/28097866/pharmacokinetics-and-biodistribution-of-the-illegal-food-colorant-rhodamine-b-in-rats
#18
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 30, 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
#19
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
#20
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
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