Search Results
Results 1 - 50 of 1319
1 2 3 4 5 6 7 8 9 10 >
Acar Omer O Department of Urology, VKF American Hospital, Istanbul, - - 2014
The purpose of this study was to determine the blood-flow-enhancing effect of electroacupuncture (EA) in an experimental rat model of testicular torsion. At the first stage, 3D color Doppler ultrasound (3D-CDUS) scans were made to detect baseline perfusion of each testicle in 12 male albino Wistar rats. Then, the left ...
Fedorova Natalia N Department of Environmental Science, Policy and Management, University of California, Berkeley, CA 94720, USA; Alameda County Vector Control Services District, Alameda, CA 94502, USA. Electronic address: - - 2014
The diversity of Lyme disease (LD) and relapsing fever (RF)-group spirochetes in the metropolitan San Francisco Bay area in northern California is poorly understood. We tested Ixodes pacificus, I. spinipalpis, and small mammals for presence of borreliae in Alameda County in the eastern portion of San Francisco Bay between 2009 ...
Nishimuta Haruka H Dainippon Sumitomo Pharma - - 2014
Hydrolysis plays an important role in metabolic activation of prodrugs. In the current study, species and in vitro system differences in hepatic and extrahepatic hydrolysis were investigated for 11 prodrugs. Ten prodrugs in the dataset are predominantly hydrolyzed by carboxylesterases (CES), whereas olmesartan medoxomil is also metabolized by carboxymethylenebutenolidase (CMBL) ...
Reck José J Instituto de Pesquisas Veterinárias Desidério Finamor (IPVDF), Fundação Estadual de Pesquisa Agropecuária (FEPAGRO), Eldorado do Sul, RS, Brazil. Electronic address: - - 2014
Ornithodoros brasiliensis, also known as the mouro tick, is an argasid tick only found in the highlands of Southern Brazil. O. brasiliensis parasitism is associated with severe reactions in its hosts ranging from local pruritus and pain to systemic disturbances. Recently, the re-emergence of O. brasiliensis parasitism in humans and ...
Gu Yi Y Department of Clinical Pharmacology and DMPK, Hutchison MediPharma Limited, Building 4, 720 Cailun Road, Zhang-Jiang Hi-Tech Park, Shanghai, 201203, - - 2014
This study evaluated the preclinical pharmacokinetics (PK) and disposition of Fruquintinib (HMPL-013), a small molecule vascular endothelial growth factor receptors inhibitor. In vitro and in vivo PK/ADME assays were conducted. Allometry and PK modeling/simulation were conducted to predict human PK parameters and the time course profiles. HMPL-013 has high permeability ...
Kazui Miho M Daiichi Sankyo Co., - - 2014
Prasugrel, a thienopyridine anti-platelet drug, is converted in animals and humans to the pharmacologically active metabolite (R-138727, (2Z)-{1-[(1RS)-2-Cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4-sulfanylpiperidin-3-ylidene}ethanoic acid) that has 2 chiral centers, occurring as a mixture of 4 isomers. The RS- and RR-isomers are more active than the SS- and SR-isomers (RS > RR > SR = SS). ...
Harrill Alison H AH College of Public Health, The University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA; The Hamner-University of North Carolina Institute for Drug Safety Sciences, The Hamner Institutes for Health Sciences, Research Triangle Park, NC 27709, USA. Electronic address: - - 2014
NP260 was designed as a first-in-class selective antagonist of α4-subtype GABAA receptors that had promising efficacy in animal models of pain, epilepsy, psychosis, and anxiety. However, development of NP260 was complicated following a 28-day safety study in dogs in which pronounced elevations of serum aminotransferase levels were observed, although there ...
Melo Dunstana R - - 2014
Abstract Purpose: This manuscript compares the behavior of monomeric plutonium-239 (239)Pu(4+)-citrate injected intravenously in rats and dogs with a comparison of available humans data. Material and methods: The experimental design for these two studies consisted of eight groups sacrificed at predetermined time points post exposure. All organs and tissues as ...
Li Yan - - 2013
Aildenafil, 1-{[3-(6, 7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo [4, 3-d] primidin-5-yl)-4-ethoxyphenyl] sulfonyl}-cis-3, 5-dimethylpiperazine, a phosphodiesterase type V enzyme inhibitor (PDE5I), is under development for treatment of erectile dysfunction (ED). The purpose of this study was to elucidate metabolism of aildenafil in vivo in rats and in vitro in mouse, rat, dog, and human liver microsomes. ...
Yang Shuoye - - 2013
This study developed a radioisotope detection and tracing method to investigate the pharmacokinetic properties of calf thymus DNA (ctDNA) in rats and beagle dogs. The radioactivity labeling result was detected through gel electrophoresis analysis, and pharmacokinetic analytical methods for (3)H-ctDNA in rat and beagle dog plasma were developed, respectively. Full ...
Furukawa Takako - - 2013
Abstract 1.  Glucuronidation via UDP-glucuronosyltransferase (UGT) in the intestine has been reported to influence the pharmacokinetics (PK) of drugs; however, information concerning the differences in activity between species is limited. Here, we investigated the in vitro and in vivo activities of intestinal glucuronidation for 17 UGT substrates in humans, rats, ...
Li Ning - - 2013
Abstract 1. The aim was to evaluate the prodrug hypothesis by investigating the pharmacokinetics of ZJM-289 and its pharmacological metabolite 3-n-butylphthalide (NBP) in Sprague-Dawley rats and Beagle dogs following intravenous and intragastric administration of ZJM-289. The in vitro metabolic patterns in plasma and microsomal system were assessed to elucidate PK ...
Sekiguchi Kazutaka - - 2013
Abstract 1. The drug metabolism and pharmacokinetics of S-777469 were investigated in in vitro (rat, dog and human) and in in vivo (rats and dogs). 2. S-777469 was rapidly and well absorbed, with bioavailability values ranging from 50 to 70% in rats and dogs, almost all drug radioactivity was excreted into the ...
Nursyazana M T - - 2013
A study to determine the diversity and distribution of ectoparasites and endoparasites infesting wild rat population of Carey Island was carried out from June to December 2010. A total of 81 rats were captured from various locations on Carey Island. Four rat species were identified namely, Rattus tiomanicus (45.7%), Rattus ...
Lee Sangkyu - - 2013
β-Lapachone (3,4-dihydro-2,2-dimethyl-2H-naphthol[1,2-b]pyran-5,6-dione) is a natural compound extracted from the bark of the lapacho tree (Tabebuia avellanedae) and is undergoing phase II clinical trials as an antitumor drug candidate. The present study characterized in vitro metabolites of β-lapachone in mouse, rat, dog, monkey and human liver microsomes. β-Lapachone (10μM) was incubated ...
Tamayo Uria Ibon - - 2013
Urban Norway rats are challenging pests, posing significant health and economic threats. Implementing ecologically based integrated rodent management (EBIRM) programmes relies primarily on the understanding of ecological relationships between rodents and their environments, with emphasis on the processes influencing rodent populations in the target ecosystem. We investigated the temporal distribution ...
Takeuchi Toshiyuki - - 2013
Previous studies on the metabolic fate of resatorvid (TAK-242) have shown that species differences in the pharmacokinetics of 4-amino-3-chlorophenyl hydrogen sulfate (M-III), a metabolite of TAK-242, between rats and dogs are mainly attributable to the urinary excretion process. In the present study, the renal uptake mechanism of M-III was investigated ...
Moraru Gail Miriam - - 2013
BACKGROUND: Amblyomma maculatum is the primary vector for Rickettsia parkeri, a spotted fever group rickettsia (SFGR) and human pathogen. Cotton rats and quail are known hosts for larval and nymphal A. maculatum; however, the role of these hosts in the ecology of R. parkeri is unknown. METHODS: Cotton rats and ...
Fabio Karine M - - 2013
SRX246 is a potent, highly selective, orally bioavailable vasopressin 1a receptor antagonist that represents a novel mechanism of action for the treatment of mood disorders. The compound previously showed efficacy in animal models of mood disorders and excellent safety and tolerability in healthy volunteers in phase I clinical trials. In ...
Furuta Shinji - - 2013
The pharmacokinetic disposition of anagliptin, an orally active and highly selective dipeptidyl peptidase-4 (DPP-4) inhibitor was evaluated in male rats and dogs. Anagliptin was well absorbed in dogs (70.4 %) and moderately to well absorbed in rats ranging from 38.1 to 85.5 % depending on the dose. In situ testing indicated that ...
Zhang Donglu - - 2013
Abstract The study described here investigated the impact of intestinal excretion (IE, excretion of drug directly from circulation to intestinal lumen), enteroenteric recirculation (EER), and renal tubule recirculation (RTR) on apixaban pharmacokinetics and disposition. The experimental approaches involve integrating apixaban elimination pathways with pharmacokinetic profiles obtained from bile duct-cannulated (BDC) ...
Liu Hong - - 2013
Abstract 1. Metabolism of ABT-107 was investigated in in vitro hepatic systems, in rat and monkey receiving [(14)C]ABT-107, and in vivo plasma in rat, dog, monkey and human. 2. In in vitro hepatic systems, ABT-107 was primarily cleared via oxidative metabolism, and proceeded via two parallel pathways. Pathway 1, ABT-107 ...
Zamek-Gliszczynski Maciej J - - 2013
LY2090314 is an intravenous GSK-3 inhibitor in oncology trials. Drug disposition was characterized following IV infusion of [(14)C]LY2090314 to rats and dogs, and was related to available clinical data. LY2090314 exhibited high clearance (approximating hepatic blood flow) and a moderate volume of distribution (~1-2 L/kg) resulting in rapid elimination across ...
Morelli James K - - 2013
Dog and rat hepatocytes were treated with phospholipogenics to identify the more sensitive species and to determine whether lysosomal or mitochondrial changes were the primary cause of cytotoxicity. Endpoints included cell death, lysosome membrane integrity, mitochondrial membrane polarization, and fluorescent phospholipid (NBD-PE). Dog cells exhibited lower survival IC50 values than ...
Qiu Zhixia - - 2012
The objective of this investigation was to compare the efficiency of conversion to the active metabolite (AM) from clopidogrel and vicagrel, a novel antiplatelet agent, and support the drug design rationale in the view of the pharmacokinetics. Following intravenous administration to rats, vicagrel was rapidly converted to its thiolactone intermediate ...
Palmgren Anna-Pia - - 2012
1. The SureTran™ matrix is a novel method facilitating short-term maintenance of fresh primary hepatocyte cellular function and offers the potential use of primary cells "as fresh" for several days post isolation. In the study presented, the maintenance of several key phase I and II drug metabolizing enzyme and drug transporter ...
Kageyama Yuko Y Department of Clinical Laboratory Medicine, Graduate School of Medicine, The University of Tokyo, Tokyo, - - 2012
Sinusoidal vasoconstriction, in which hepatic stellate cells operate as contractile machinery, has been suggested to play a pivotal role in the pathophysiology of portal hypertension. We investigated whether sphingosine 1-phosphate (S1P) stimulates contractility of those cells and enhances portal vein pressure in isolated perfused rat livers with Rho activation by ...
- - 2012
The Norway rat (Rattus norvegicus) is a pervasive urban rodent that can carry a variety of pathogens transmissible to humans, bring stress to residents of infested neighborhoods, damage property, and cause financial loss. Several areas of New York City have experienced persistent rat infestation despite a longstanding rat control program ...
Li Austin C - - 2012
1. There has been a lack of in vivo metabolite profiling update of hydrocodone since the original report on species differences was published in 1978. As such, the mechanism for its analgesic activity in different species has been ambiguous. To address safety concern from regulatory agencies, hydrocodone metabolite profiles in ...
Huang Liyue - - 2012
This study was designed to characterize breast cancer resistance protein (Bcrp) knockout Abcg2(-/-) rats, and to assess the effect of Abcg2 deletion on the excretion and pharmacokinetic properties of probe substrates. Deletion of the target gene in the Abcg2(-/-) rats was confirmed, while gene expression was unaffected for most of ...
Han Jong-Min - - 2012
Cholestatic liver fibrosis, characterized by excessive accumulation of extracellular matrix (ECM) proteins, is associated with bile acid-induced oxidative stress and lipid peroxidation. We evaluated the therapeutic or protective effect of an aqueous extract of Artemisia iwayomogi Kitamura (WAI) in a rat bile duct ligation (BDL)-induced hepatic fibrogenesis model. After BDL, ...
Holm René - - 2012
The purpose of this study was to evaluate if a rat model, based upon co-administration of the anion-exchanging resin, cholestyramine, could replace surgery when evaluating the importance of bile on drug absorption. Two different formulations were used for the administration of halofantrine; polyethylene glycol 400 (PEG400) and PEG400/polysorbate 80 (50/50 ...
Zamek-Gliszczynski Maciej J - - 2012
Transporter gene knockout rats are practically advantageous over murine models for pharmacokinetic and excretion studies, but their phenotypic characterization is lacking. At present, relevant aspects of pharmacokinetics, metabolism, distribution, and excretion of transporter probes (P-gp: loperamide and paclitaxel, Bcrp: sulfasalazine, Mrp2: carboxydichlorofluorescein) were studied systematically across SAGE Mdr1a-, Bcrp-, and ...
Kudo Atsushi - - 2012
BACKGROUND: Severe macrosteatotic liver has been regarded as a donor contraindication for liver transplantation. However, it has not yet been determined whether hepatocytes lose function before cold ischemia. This study was designed to elucidate certain pathophysiological alterations and how to ameliorate such hepatic dysfunctions. MATERIALS AND METHODS: Wistar rats were ...
Varma Manthena V S - - 2012
Biliary excretion is a major elimination pathway, and its prediction is particularly important for optimization of systemic and/or target-site exposure of new molecular entities. The objective is to characterize the physicochemical space associated with hepato-biliary transport and rat biliary excretion (BE) and develop in silico models. BE of 123 in-house ...
Bahde Ralf - - 2012
Excretion of copper into bile requires the copper transporter Atp7b, which is deficient in Wilson disease. We hypothesized that a radiocopper-histidine complex would be effective for diagnosing Wilson disease by molecular imaging and tested this hypothesis in the Long-Evans cinnamon (LEC) rat model with Atp7b deficiency. We complexed (64)Cu to ...
Montenegro-Miranda Paula S PS Tytgat Institute for Intestinal and Liver Research, Academic Medical Center of the University of Amsterdam, The - - 2012
As recently demonstrated in patients with factor IX deficiency, adeno-associated virus (AAV)-mediated liver-directed therapy is a viable option for inherited metabolic liver disorders. Our aim is to treat Crigler-Najjar syndrome type I (CN I), an inherited severe unconjugated hyperbilirubinemia, as a rare recessive inherited disorder. Because the number of patients ...
Liu Tao - - 2012
The objective was to determine whether protective effects of JBP485 on biliary obstruction induced by alpha-naphthylisothiocyanate (ANIT) are mediated by the organic anion transporters Oat1, Oat3 and the multidrug resistance-associated protein Mrp2. The ANIT-induced increases in bilirubin (BIL), alanine aminotransferase (ALT) and aspartate transaminase (AST) in rat serum were inhibited ...
Holm René - - 2012
The bioavailability of the poorly soluble model drug halofantrine, dosed in a soy bean oil solution or in a self-nanoemulsifying drug delivery system (SNEDDS), at two levels of lipid, was assessed in rats. Three rat models were used: intact rats, sham-operated rats and bile duct cannulated rats. The study showed ...
Marion Tracy L - - 2012
Sandwich-cultured hepatocytes (SCH) are used commonly to investigate hepatic transport protein-mediated uptake and biliary excretion of substrates. However, little is known about the disposition of endogenous bile acids (BAs) in SCH. In this study, four endogenous conjugated BAs common to rats and humans [taurocholic acid (TCA), glycocholic acid (GCA), taurochenodeoxycholic ...
Du Jin-Xing - - 2012
Huangqi decoction was first described in Prescriptions of the Bureau of Taiping People's Welfare Pharmacy in Song Dynasty (AD 1078), and it is an effective recipe that is usually used to treat consumptive disease, anorexia, and chronic liver diseases. Transforming growth factor beta 1 (TGFβ1) plays a key role in ...
Wikramanayake T C TC Department of Dermatology and Cutaneous Surgery, University of Miami Miller School of Medicine, Miami, FL 33136, - - 2011
tert-butyl hydroperoxide (tBHP), an organic peroxide, has been shown to cause irreversible damage to keratinocytes in vitro with prolonged administration at high concentrations, and reversible damage with short-term administration at low concentrations. To investigate the effects of tBHP on keratinocytes in vivo, we analysed hair growth in tBHP-treated neonatal rats. ...
Klump Kelly L - - 2011
Ovarian hormones are associated with binge eating in women, however findings are limited by the lack of experimental control inherent in human studies. Animal research that manipulates ovarian hormone status and examines individual differences in extreme binge eating proneness is needed to model clinical phenotypes in humans and to confirm ...
Dimmock David - - 2011
Crigler-Najjar syndrome type I is a severe inborn error of bilirubin metabolism caused by a complete deficiency of uridine diphospho-glucuronosyl transferase 1A1 (UGT1A1) and results in life-threatening unconjugated hyperbilirubinemia. Lifelong correction of hyperbilirubinemia by liver-directed gene therapy using a helper-dependent adenoviral (HDAd) vector has been previously reported in the Gunn ...
Maillard Virginie - - 2011
Resistin, initially identified in adipose tissue and macrophages, was implicated in insulin resistance. Recently, its mRNA was found in hypothalamo-pituitary axis and rat testis, leading us to hypothesize that resistin may be expressed in ovary. Here, we determined in rat and cow: 1) the characterization of resistin in ovary by ...
Yang Guanghui - - 2011
The progression of wound healing is a complicated but well-known process involving many factors, yet there are few products on the market that enhance and accelerate wound healing. This is particularly problematic in veterinary medicine where multiple species must be treated and large animals heal slower, oftentimes with complicating factors ...
Morales-Ledesma Leticia - - 2011
In the present study we analyzed the existence of asymmetry in the secretion of steroid hormones in pre-pubertal female rats treated with unilateral ovariectomy (ULO) or unilateral perforation of the abdominal wall (sham-surgery). Treated rats were sacrificed at different times after surgery. Since sham-surgery had an apparent effect on the ...
Waldon Daniel J - - 2010
High-resolution accurate MS with an LTQ-Orbitrap was used to identify quinone imine metabolites derived from the 5-hydroxy (5-OH) and 4 prime-hydroxy (4'-OH) glutathione conjugates of diclofenac in rat bile. The initial quinone imine metabolites formed by oxidation of diclofenac have been postulated to be reactive intermediates potentially involved in diclofenac-mediated ...
Taketa Yoshikazu - - 2011
Ethylene glycol monomethyl ether (EGME) is a known reproductive toxicant that induces luteal hypertrophy in rat ovaries. In this study, we characterized the histopathological features of corpora lutea (CL) from EGME-treated rats and compared them with normal CL formation and regression. Normally cycling female Sprague-Dawley rats were treated with 5-bromo-2'-deoxyuridine ...
Zangeneh Farideh Zafari - - 2011
This study was conducted to evaluate the effect of interaction of sympathetic and opioid systems in the processing of polycystic ovary syndrome modeling in rat. Ninety adult female rats (7-8 weeks of age) were treated with EV for 60 days for induction of follicular cysts (PCO modeling). Clonidine and yohimbine were used ...
1 2 3 4 5 6 7 8 9 10 >