Maria Locher

Learn More
Disposition and metabolism of cetrorelix was studied in intact and bile duct-cannulated rats and dogs after s.c. injection. An s.c. dose of 0.1 mg/kg [(14)C]cetrorelix was rapidly and completely absorbed in rats. T(max) in plasma and most tissues was at 2 h. Radioactivity at the injection site in rats declined to 10% by 24 h. The extent of (14)C absorption(More)
The in vitro activity of posaconazole plus amphotericin B against conidia and hyphae of 30 clinical zygomycetes was investigated. The combination of posaconazole with amphotericin B was found to be significantly more synergistic (40%) against hyphae (P < 0.05) than against conidia (10%). Antagonism was not observed.
A specific plasma level assay for the enantiomers of alpha-lipoic acid is described. It makes use of liquid-liquid extraction, chemical reduction to the dithiol enantiomers, and their precolumn chiral derivatisation with o-phthalaldehyde in the presence of D-phenylalanine. The two diastereomeric derivatives are separated by reversed-phase HPLC with(More)
A HPLC assay with tandem mass spectrometric detection in the positive-ion atmospheric pressure chemical ionisation (APCI) mode for the sensitive determination of retigabine [(I), D-23129] and its acetyl metabolite [(II), ADW 21-360] in plasma was developed, utilising the structural analogue (D-10328), (III), as internal standard. Automated on-line(More)
This study was conducted to investigate the effects of rumen-protected tryptophan (125 g tryptophan per day) in heifers and dairy cows. Blood samples from dairy cows and heifers were collected for 24h in 3-h intervals on the day before tryptophan supplementation, on day 2, 5 and 7 of tryptophan supplementation, and in heifers additionally on d 14 after(More)
An HPLC assay with tandem mass spectrometric detection in the positive-ion Turbo-Ion-Spray (TISP) mode for the fast and sensitive determination of perifosine ((I), D-21266) in human plasma was developed, utilising the structural analogue, miltefosine ((II), D-18506), as internal standard. Automated solid-phase extraction of diluted plasma samples, based on(More)
Lipoic acid (alpha-lipoic acid, thioctic acid) is applied as a therapeutic agent in various diseases accompanied by polyneuropathia such as diabetes mellitus. The stereoselectivity and specificity of lipoic acid for the pyruvate dehydrogenase complex and its component enzymes from different sources has been studied. The dihydrolipoamide dehydrogenase(More)
The metabolism of 14C-naftopidil ((R,S)-1-(2-methoxyphenyl)-1-piperazinyl-3- (1-naphthyl-oxy-2-propanol, CAS 57149-07-2) and the pharmacodynamic action of the metabolites was investigated. The metabolic pathway in rat, dog, mouse and man was qualitatively similar, with preference for the hydroxylation of the phenyl or naphthyl moiety of naftopidil(More)
Cells from liver, jejunum, ileum, colon and kidney of the guinea pig were freshly prepared by standard isolation procedures. Cells were incubated in the presence of several concentrations of 1(14C)-naphthol, and formation of 1-naphthol glucuronide and 1-naphthol sulphate was assessed at various times by thin layer chromatography. Cells from all five tissues(More)
Arachidonic acid metabolism was studied in isolated gastric mucous and parietal cells. During a 90 min incubation, mucous cells incorporated [1-14C]arachidonic acid (4.5 mumol/l) into triacylglycerols (500 pmol/mg protein), phosphatidylcholine (520), phosphatidylethanolamine (290) and phosphatidylinositol (100). 230 pmol/mg protein was recovered as 14CO2(More)