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91.
92.
Lundin Pål D. P. Lundin Stefan Olsson Håkan Karlsson Börje W. Weström Björn R. Pierzynowski Stefan G. 《Pharmaceutical research》1995,12(10):1478-1482
Purpose. The present investigation was done to study the intestinal absorption of three oxytocin peptide analogues and to elucidate the role of pancreatic juice on their absorption.
Methods. In conscious chronically catheterized pigs (6–8 weeks of age) plasma concentration of the peptides, [Mpa1, D-Tyr(Ethyl)2, Thr4, Orn8]-oxytocin (F314), [Mpa1, D-Tyr(Ethyl)2, Val4, D-Arg8]-oxytocin (CAT), and [Mpa1, D-Tyr(Ethyl)2, Thr4, Orn8, desGly9, carba6]-oxytocin (F327) after intraduodenal administration, during presence or diversion of the pancreatic juice via a pancreatic duct catheter, were determined by radioimmunoassay. The stability of the peptides to degradation was determined in vitro by incubation with activated pancreatic juice, chymotrypsin or trypsin, followed by reversed phase HPLC analyses.
Results. All peptides were absorbed with a bioavailability of about 0.5% in the presence of pancreatic juice, but increased to 1.0%, 2.1%, and 13.5% for F314, CAT, and F327, respectively, when the pancreatic juice was diverted from the intestine. After incubation with pancreatic juice 95% of F314, 98% of F327, and 100% of CAT was found intact. When incubated with trypsin CAT remained intact while F314 and F327 were degraded by 54% and 46%, respectively. Incubation with purified chymotrypsin did not degrade the test peptides.
Conclusions. The results indicate that the increased absorption of peptides observed under conditions of diverted pancreatic juice cannot only be explained by the absence of pancreatic enzymes, but also by changed absorptive properties in the gastrointestinal tract. 相似文献
93.
Christian Foged Christer Halldin Christian Loc’h Bernard Mazière Stefan Pauli Mariannick Maziére Holger C. Hansen Tetsuya Suhara Carl-Gunnar Swahn Per Karlsson Lars Farde 《European journal of nuclear medicine and molecular imaging》1997,24(10):1261-1267
NNC 13-8241 has recently been labelled with iodine-123 and developed as a metabolically stable benzodiazepine receptor ligand
for single-photon emission computed tomography (SPECT) in monkeys and man. NNC 13-8199 is a bromo-analogue of NNC 13-8241.
This partial agonist binds selectively and with subnanomolar affinity to the benzodiazepine receptors. We prepared 76Br labelled NNC 13-8199 from the trimethyltin precursor by the chloramine-T method. Carbon-11 labelled NNC 13-8199 was synthesised
by N-alkylation of the nitrogen of the amide group with [11C]methyl iodide. Positron emission tomography (PET) examination with the two radioligands in monkeys demonstrated a high uptake
of radioactivity in the occipital, temporal and frontal cortex. In the study with [76Br]NNC 13-8199, the monkey brain uptake continued to increase until the time of displacement with flumazenil at 215 min after
injection. For both radioligands the radioactivity in the cortical brain regions was markedly reduced after displacement with
flumazenil. More than 98% of the radioactivity in monkey plasma represented unchanged radioligand 40 min after injection.
The low degree of metabolism indicates that NNC 13-8199 is metabolically much more stable than hitherto developed PET radioligands
for imaging of benzodiazepine receptors in the primate brain. [76Br]NNC 13-8199 has potential as a radioligand in human PET studies using models where a slow metabolism is an advantage.
Received 19 April and in revised form 10 June 1997 相似文献
94.
95.
Dao Yin Xie Stefan Hassenstein Martin Oberhoff Hartmut Hanke Andreas Baumbach Kristian Hohla Karl Konstantin Haase Karl Rüdiger Karsch 《Lasers in surgery and medicine》1993,13(6):618-624
A modified exeimer laser energy delivery system was used to irradiate 100 segments of normal and fibrous aorta in vitro. The laser beam was scanned into 8 fiber bundles consisting of 50 fibers each resulting in a reduction of the applied pulse energy. The total repetition rate was increased to 150 Hz in order to keep the repetition rate per fiber bundle close to 20 Hz and to minimize thermal injury. The results demonstrate that effective ablation (etch rate per 8 pulses > 2.0 μm) occurred at an energy fluency of 50 mJ/mm2 in both normal and fibrous aorta. Tissue damage (carbonization, tissue separation, fissures, cracks, and vacuolization) was in a range of 100 ± 28 to 152 ± 30 μm for normal aorta and in a range of 57 ± 35 to 110 ± 39 μm for fibrous aorta. We conclude that effective ablation of normal and fibrous human aorta can be achieved by the application of smooth excimer laser coronary angioplasty. This improvement of excimer laser technology may result in a reduction of shock wave- and cavitation-induced damage leading to a reduction of tissue injury. However, this awaits further in vitro and in vivo confirmation. © 1993 Wiley-Liss, Inc. 相似文献
96.
Danuta Knapikowa Zbigniew Andreasik Stefan Kwiatkowski Marek Okrojek Roman Smolik Krzysztof Szczerba 《International archives of occupational and environmental health》1988,60(5):351-353
Summary We examined 81 men exposed for a long time to carbon disulphide (CS2) and tested the possible electrocardiographic (ECG) changes of ischemic heart disease (I.H.D.). The subjects were examined twice in two years. In order to make the ECG evaluation more objective, the Minnesota Code was applied. Two obligatory ECG examinations and only one submaximal effort test were carried out. For comparative evaluation, the control group was examined once. We proved that, in spite of the accepted opinion concerning the atheromatous action of CS2, this compound does not cause ECG symptoms of I.H.D. in a higher percentage of exposed persons. It also does not cause any significant increase in I.H.D. symptoms in dynamic ECG observations. 相似文献
97.
98.
99.
Matthew D Robson Peter D Gatehouse Graeme M Bydder Stefan Neubauer 《Magnetic resonance in medicine》2004,51(5):888-892
Phosphorus was imaged in vivo in human cortical and trabecular bone and the T(1) and T(2) (*) were measured. An ultrashort TE (UTE) pulse sequence (TE = 70 microm) was used with half pulse excitation and radial mapping of k-space from the center out. T(2) (*) was measured using multiple echo times and T(1) was measured both by saturation recovery and by a method using different RF pulse amplitudes. Seven normal subjects (32-85 years) were examined. Phosphorus was imaged, with a true in-plane resolution of 2.9 x 2.9 mm and a signal-to-noise ratio (SNR) of 19:1, in both cortical and trabecular bone. The mean T(2) (*) value was 207 +/- 12 micros, and the mean T(1) value was 8.6 +/- 3.0 sec. Images and measurements were obtained in realistic times on a clinical MR system. This may provide a new approach to characterizing disease of bone. 相似文献
100.