Search results for " intestine"
showing 10 items of 132 documents
Synthesis and evaluation of fluorine-18 labeled glyburide analogs as β-cell imaging agents
2003
Glyburide is a prescribed hypoglycemic drug for the treatment of type 2 diabetic patients. We have synthesized two of its analogs, namely N-[4-[beta-(2-(2'-fluoroethoxy)-5-chlorobenzenecarboxamido)ethyl]benzenesulfonyl]-N'-cyclohexylurea (2-fluoroethoxyglyburide, 8b) and N-[4-[beta-(2-(2'-fluoroethoxy)-5-iodobenzenecarboxamido)ethyl]benzenesulfonyl]-N'-cyclohexylurea (2-fluoroethoxy-5-deschloro-5-iodoglyburide, 8a), and their fluorine-18 labeled analogs as beta-cell imaging agents. Both F-18 labeled compound 8a and compound 8b were synthesized by alkylation of the corresponding multistep synthesized hydroxy precursor 4a and 4b with 2-[(18)F]fluoroethyl tosylate in DMSO at 120 degrees C for …
Absolute volume of the rectum and AUC from rectal DVH between 25Gy and 50Gy predict acute gastrointestinal toxicity with IG-IMRT in prostate cancer
2016
International audience; Background: To determine whether dose/volume specific endpoints (DVSE) or Area under the rectal DVH curve (rAUC) better predict acute gastrointestinal (GI) toxicity in prostate cancer patients treated with IMRT in the era of daily image guidance (IG-IMRT). Methods: A set of DVSE was recorded from V25 to V75 (increments of 5Gy) (both in % and in cc) for 180 men. The rAUC was calculated for doses ranging between 25Gy and 50Gy (rAUC(25-50)). Univariate and multivariate logistic regressions were performed to determine the relationship between DVSE or rAUC(25-50) and the appearance of any acute GI toxicity. Results: The rates of acute grade 1 (G1), G2 and G3 GI toxicities…
Clinical Translation and First In-Human Use of [44Sc]Sc-PSMA-617 for PET Imaging of Metastasized Castrate-Resistant Prostate Cancer
2017
Background: Various trivalent radiometals are well suited for labeling of DOTA-conjugated variants of Glu-ureido-based prostate-specific membrane antigen (PSMA) inhibitors. The DOTA-conjugate PSMA-617 has proven high potential in PSMA radioligand therapy (PSMA-RLT) of prostate cancer as well as PET imaging when labeled with lutetium-177 and gallium-68 respectively. Considering the relatively short physical half-life of gallium-68 this positron emitter precludes prolonged acquisition periods, as required for pre-therapeutic dosimetry or intraoperative applications. In this context, the positron emitter scandium-44 is an attractive alternative for PET imaging. We report the synthesis of [44Sc…
Chirurgische Therapie bei Karzinoiden des Gastrointestinaltraktes
2001
More than 70% of all carcinoids are localized in the gastrointestinal tract. Carcinoids of the upper, middle and lower intestines have to be distinguished ontogenetically. The classification according to Capella takes into account the size of the tumor ( 2 cm), the grade of invasion of other structures, the grade of angioinvasion, the biologic behaviour, the grade of differentiation and the hormonal activity of the tumor. A carcinoid-syndrome is rarely found. Carcinoids of the small intestine occur multiple in 30-50% and in 20-30% a second malignant tumor is seen. In carcinoids of the colon this percentage is even higher (25-40%). The therapy of carcinoids depends on the size of the tumor a…
La teneur en lipides du régime affecte les capacitésd'absorption intestinale et la triglycéridémie postprandiale: contribution du récepteur nucléaire…
2007
The dietary long chain fatty acid have crucial functions into the organism such as energysource, eicosanoïdes synthesis, gene regulation). The fat disposal is essential and depend onintestinal barrier. It is well known that intestinal fat absorption is efficient. However, we don'tif the high triglycerides bioavailability of gut is attributable to inborn properties or to acquiredproperties. To answer this question, mice were subjected to a high-fat diet (40%, w/w) during21 days. We have shown that high-fat induces : 1) intestinal LCFA uptake, 2) intestinalmitotic index which leads to an increase of intestinal relative mass, 3) expression of genesinvolved in fatty uptake (Fatty Acid Transport…
Nitric oxide synthase in the enteric nervous system of the guinea-pig: a quantitative description
1994
The distribution and abundance of nitric oxide synthase (NOS)-containing neurons and their terminals in the gastrointestinal tract of the guinea-pig were examined in detail using NADPH diaphorase histochemistry and NOS immunohistochemistry. NOS-containing cell bodies were found in the myenteric plexus throughout the gastrointestinal tract and in the submucous plexus of the stomach, colon and rectum. NOS-containing neurons comprised between 12% (in the duodenum) and 54% (in the esophagus) of total myenteric neurons. In the ileum, NOS neurons represented 19% of total myenteric neurons. Most of the NOS neurons throughout the gastrointestinal tract possessed lamellar dendrites and a single axon…
Improvement of trospium-specific absorption models for fasted and fed states in humans
2014
The purpose of this study was to mechanistically interpret the oral absorption pattern of trospium in fasted and fed states by means of gastrointestinal simulation technology. A drug absorption model was built on the basis of experimental data. According to the generated model, low permeability across the intestinal epithelium, delayed gastric emptying time and a prolonged residence time in the small intestine are the key factors governing trospium absorption in the fasted state. Furthermore, in silico modelling provided a plausible explanation of the pronounced reduction in the oral bioavailability of trospium when administered with food. The simulation results support the decreased dissol…
In Situ Study of the Effect of Naringin, Talinolol and Protein-Energy Undernutrition on Intestinal Absorption of Saquinavir in Rats
2011
To study the potential interactions of naringin (NAR), talinolol (TAL) and protein-energy undernutrition (PEU) in the absorption process of saquinavir (SQV), perfusion experiments were performed in the small intestine of rats at different SQV concentrations. The results obtained demonstrated that SQV intestinal absorption was described by simultaneous passive diffusion (kdif = 3.44 hr) and saturable absorption (Vma = 127.31 lM ⁄ hr; Kma =1 0.50lM) together with a capacity-limited efflux (Vms = 270.53 lM ⁄ hr; Kms =2 3.44lM). The competitive inhibition constants of NAR on the SQV input and efflux processes were (IC50)a =3 .98l Ma nd(IC50)s = 5.00 lM, respectively. NAR significantly decreased…
Synthese, Verteilung und Ausscheidung von 14C markiertem 2-Phenyl-3-methyl-tetrahydro-1,4-oxazin (Preludin)
1958
A radioactive preludin preparation, C14 labelled on the 2-carbon of the tetrahydrooxazine ring, was injected into mice in doses of 100 mg/kg s.c. and rats in doses of 10 mg/kg i.v. The radioactivity of the tissues and excreta was followed for 48 hours. An activity concentration surpassing the average body concentration was obtained for a short time in the lungs and for a longer time in kidneys, liver and in the wall of stomach and small intestine. 95–99% of the total activity is found in the urine. The kidney excretion is virtually finished at the end of 8 hours; 1–5% appear after the 8th hour in faeces. No radioactivity was obtained from the expired CO2. The main excretion organs are kidne…
Colorectal Cancer Stem Cells: From the Crypt to the Clinic
2014
Since their first discovery, investigations of colorectal cancer stem cells (CSCs) have revealed some unexpected properties, including a high degree of heterogeneity and plasticity. By exploiting a combination of genetic, epigenetic, and microenvironmental factors, colorectal CSCs metastasize, resist chemotherapy, and continually adapt to a changing microenvironment, representing a formidable challenge to cancer eradication. Here, we review the current understanding of colorectal CSCs, including their origin, relationship to stem cells of the intestine, phenotypic characterization, and underlying regulatory mechanisms. We also discuss limitations to current preclinical models of colorectal …