Enantioselective pharmacokinetics of ketoprofen in piglets: the significance of neonatal age     

Fosse TK  Horsberg TE  Haga HA  Hormazabal V  Ranheim B 《Journal of veterinary pharmacology and therapeutics》2011,34(2):153-159

Following intravenous dose of 6mg/kg racemic ketoprofen, the chiral pharmacokinetics of ketoprofen was investigated in eight piglets aged 6 and 21days old. S-ketoprofen predominated over R-ketoprofen in plasma of the piglets in both age groups. The volumes of distribution of S-ketoprofen for the 6- and 21-day-old piglets were 241.7 (211.3-276.5) mL/kg and 155.0 (138.7-173.1) mL/kg, respectively, while the corresponding parameters for R-ketoprofen were 289.2 (250.3-334.2) mL/kg and 193.0 (168.7-220.8) mL/kg. The clearances of R-ketoprofen [948.4 (768.0-1171.2) mL/h/kg and 425 (319.1-566.0) mL/h/kg for the 6- and 21-day-old piglets, respectively] were significantly higher compared to the clearances of S-ketoprofen [57.3 (46.6-70.4) mL/h/kg and 33.8 (27.0-42.2) mL/h/kg for 6- and 21-day-old piglets, respectively]. The elimination half-life of S-ketoprofen was 3.4h for both age groups, while the elimination half-life of R-ketoprofen was 0.2h for the 6-day-old and 0.4h for the 21-day-old piglets. The clearances of both R- and S-ketoprofen were significantly higher in the 6-day-old piglets compared to when they were 21 days old. Furthermore, the volumes of distribution were larger in the youngest age group.  相似文献   

Ketoprofen in piglets: enantioselective pharmacokinetics, pharmacodynamics and PK/PD modelling     

Fosse TK  Toutain PL  Spadavecchia C  Haga HA  Horsberg TE  Ranheim B 《Journal of veterinary pharmacology and therapeutics》2011,34(4):338-349

The chiral pharmacokinetics and pharmacodynamics of ketoprofen were investigated in a placebo-controlled study in piglets after intramuscular administration of 6 mg/kg racemic ketoprofen. The absorption half-lives of both enantiomers were short, and S-ketoprofen predominated over R-ketoprofen in plasma. A kaolin-induced inflammation model was used to evaluate the anti-inflammatory, antipyretic and analgesic effects of ketoprofen. Skin temperatures increased after the kaolin injection, but the effect of ketoprofen was small. No significant antipyretic effects could be detected, but body temperatures tended to be lower in the ketoprofen-treated piglets. Mechanical nociceptive threshold testing was used to evaluate the analgesic effects. The piglets in the ketoprofen-treated group had significantly higher mechanical nociceptive thresholds compared to the piglets in the placebo group for 12-24 h following the treatment. Pharmacokinetic/pharmacodynamic modelling of the results from the mechanical nociceptive threshold testing gave a median IC(50) for S-ketoprofen of 26.7 μg/mL and an IC(50) for R-ketoprofen of 1.6 μg/mL. This indicates that R-ketoprofen is a more potent analgesic than S-ketoprofen in piglets. Estimated ED(50) for racemic ketoprofen was 2.5 mg/kg.  相似文献   

Polymers with Very Low Polydispersities from Atom Transfer Radical Polymerization     

TE Patten  J Xia  T Abernathy  K Matyjaszewski 《Science (New York, N.Y.)》1996,272(5263):866-868

A radical polymerization process that yields well-defined polymers normally obtained only through anionic polymerizations is reported. Atom transfer radical polymerizations of styrene were conducted with several solubilizing ligands for the copper(I) halides: 4,4'-di-tert-butyl, 4,4'-di-n-heptyl, and 4,4'-di-(5-nonyl)-2,2'-dipyridyl. The resulting polymerizations have all of the characteristics of a living polymerization and displayed linear semilogarithmic kinetic plots, a linear correlation between the number-average molecular weight and the monomer conversion, and low polydispersities (ratio of the weight-average to number-average molecular weights of 1.04 to 1.05). Similar results were obtained for the polymerization of acrylates.  相似文献   

Nearly singular magnetic fluctuations in the normal state of a high-Tc cuprate superconductor     

G Aeppli  TE Mason  SM Hayden  HA Mook  J Kulda 《Science (New York, N.Y.)》1997,278(5342):1432-1435

Polarized and unpolarized neutron scattering was used to measure the wave vector- and frequency-dependent magnetic fluctuations in the normal state (from the superconducting transition temperature, Tc = 35 kelvin, up to 350 kelvin) of single crystals of La1.86Sr0.14CuO4. The peaks that dominate the fluctuations have amplitudes that decrease as T-2 and widths that increase in proportion to the thermal energy, kBT (where kB is Boltzmann's constant), and energy transfer added in quadrature. The nearly singular fluctuations are consistent with a nearby quantum critical point.  相似文献   

Influence of different materials on the concentration of delousing agents in sea water during bioassays     

K O Helgesen  T E Horsberg 《Journal of fish diseases》2013,36(5):529-532

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Phosphorus supplements and fluorosis in cattle—a northern Australian experience     

TF JUBB  TE ANNAND  DC MAIN  GM MURPHY 《Australian veterinary journal》1993,70(10):379-383

SUMMARY Chronic fluoride toxicosis caused lameness, dental lesions and illthrift in an extensive beef cattle herd in northern Australia. Up to 15% of the herd was lame and the disease forced the culling of large numbers of cows. The source of fluoride was fertiliser-grade monoammonium and diammonlum phosphate fed as part of a mineral supplement. Large quantities of mineral supplement were provided to the cattle because lameness was attributed to phosphorus deficiency, which is endemic in the area. Most lameness developed in the late dry season in the post-lactation phase. Severe lameness was caused by fractured pedal bones.  相似文献   

KINETICS OF DICHLOBENIL DEGRADATION IN SOIL   总被引：2，自引：0，他引：2  

M. MONTGOMERY  TE C. YU  V. H. FREED 《Weed Research》1972,12(1):31-36

Summary. The rates of degradation of dichlobenil (2,6-dichlorobenzonitrile) in soil were determined at 67 and 267°C. The degradation followed first-order kinetics but at 67°C this occurred after an initial lag period of 10 weeks. The half-lives were 28 weeks (+ 10 weeks lag) at 6.7°C and 19 weeks at 26.7°C. The activation energy for the decomposition was the relatively low value of 3.57 kcal/mole, indicating that the degradation of dichlobenil is not as markedly affected by temperature as that of many other herbicides. The only detectable metabolite was 2,6-dichlorobenzamide, a compound that should have a substantially lower vapour pressure and a higher affinity for surfaces than the parent compound. Cinétique de la dégradation du dichlobénil dans le sol Résumé. Les taux de dégradation du dichlobénil (2,6-dichlorobenzonitrile) dans le sol ont été détermines à 6,7 et 26,7°C. La déSgradation suivit une loi cinétique du premier ordre, mais à 6,7°C ceci se produisit aprés une période initiate de latence de 10 semaines. Les demi-vies furent de 28 semaines (plus 10 semaines de latence) a 6,7°C et 19 semaines à. 26,7°C. L'énergie d'activation pour la décomposition s'établit à la valeur relativement faible de 3,57 kcal/mole; ceci indique que la dégradation du dichlobénil n'est pas aussi profondément affcctée par la température quc celle de beaucoup d'autres herbicides. Le seul métabolite detectable fut le 2,6-dichlorobenzamide, composé qui devrait avoir une pression de vapeur notablement plus faible et une affinité plus grande pour les surfaces que le composé apparenté. Kinetik des Dichlohenil-Abbaus im Boden Zusammenfassung. Es wurde die Abbaugeschwindigkeit von Dichlobenil (2,6-Dichlorbenzonitril) im Boden bei 6,7°C und 26,7°C bestinimt. Der Abbau entsprach einer Reaktion erster Ordnung. Bei 6,7°G setzte der Abbau nach einer lag-Phase von 10 Wochen ein. Die Halbwertzeiten betrugen 28 Wochen (+10 Wochen lag-Phase) bei 6,7°C und 19 Wochen bei 26,7°C. Die Aktivierungsenergie war verhältnisniässig niedrig und betrug 3,57 Kcal/Mol und zeigt, dass der Abbau von Dichlobenil durch Temperatur nicht so stark beeinflusst wird wie bei vielen anderen Herbiziden. Der einzige nachweisbare Metabolit war 2,6-Dichlorbenzamid, der einen wcsentlich nieddgeren Dampfdruck und eine grössere Affinität gegenüber Oberfiächen haben dürfte als die ursprüngliche Verbindung.  相似文献   

Excretion of flumequine in free-swimming Atlantic salmon (Salmo salar), determined by cannulation of the dorsal aorta, gall bladder and urethra     

Sohlberg S  Martinsen B  Horsberg TE  Søli NE 《Journal of veterinary pharmacology and therapeutics》1999,22(1):72-75

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Medetomidine and atipamezole in sheep: disposition and clinical effects     

Ranheim B  Arnemo JM  Stuen S  Horsberg TE 《Journal of veterinary pharmacology and therapeutics》2000,23(6):401-404

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Isolation,Culture and Identification of Testis Sertoli Cells in Mongolian Horses in vitro     

SONG Lianjie  CUI Yingying  ZHAO Yiping  BAI Dongyi  REN Xiujuan  TE Rigele  DUGARJAVIIN Manglai  LI Bei 《中国畜牧兽医》2007,47(9):2751-2758

To study a simple and rapid separation of testis Sertoli cells in Mongolian horses and ensure their activity,the testis tissue of two-year-old Mongolian horses was mechanically isolated under a low temperature environment in this experiment,and 1-3 g of testis tissue was chopped,the free red blood cells and interstitial cells were removed by gravity precipitation method.0.1% collagenase Ⅳ and 0.25% trypsin-EDTA were used for tissue digestion, and cells were cultured in medium containing 10% fetal bovine serum.After inoculation,the purified Sertoli cells were isolated and purified by differential sticking method,and the impurity cells were removed by Tris-HCl infiltration method,and were identified by alkaline phosphatase (AKP) staining,HE staining and Real-time quantitative PCR.The results showed that most of the cells began to adhere to the wall after culture 24 h,and the shape of the cells was oval.After culture 48 h,the cytoplasm increased and the refraction became stronger.After culture 3-4 d,the cytoplasm of the cells expanded into tight junction.At this time,the cells were triangular with obvious nucleoli.After culture 6-7 d,the cells entered the stable phase.Real-time quantitative PCR results showed that the expression of GATA4 and GDNF genes were extremely significantly expressed in cultured cells (P<0.01).AKP staining supported the negative expression in Sertoli cells,indicating that the isolated cultured cells were indeed Sertoli cells.In this experiment,tissue was treated by mechanical separation and two-step enzyme digestion,and testicular support cells were obtained quickly and efficiently,the method of culturing Sertoli cells in Mongolian horses testis in vitro was successfully constructed.  相似文献