• Publications
  • Influence
Influence of different calcic antagonists on the Caco-2 cell monolayer integrity or “TEER, a measurement of toxicity ?”
The TEER measurement appeared as a quite simple approach of comparative toxicity of anticalcic agents as an evaluation of toxicity, in function of time and level of drug in the experimental medium, for different anticalCic agents.
Multiple binding of bepridil in human blood.
The binding parameters were used to simulate the distribution of bepridil between serum proteins, blood cells and platelets over the therapeutic range and showed that serum albumin, alpha 1-acid glycoprotein and RBC were the major binding components.
Zipeprol metabolism in man and in the animal.
Zipeprol is partially eliminated untransformed from the body, is mainly metabolised by N-dealkylation, oxidation, hydroxylation and methylation.
Biotransformation study of para-substituted phenylpiperazines in beagle dogs by gas chromatography-mass spectrometry.
Beagle dogs were treated orally with para-chloro-, para-fluoro- and para-methyl-phenylpiperazine derivatives, and urine was collected for 72 h after treatment and two kinds of hydroxylated metabolites were found.
An in vitro investigation of the relationships between potency, lipophilicity, cytotoxicity and chemical class of representative calcium antagonist drugs.
It is suggested that the higher cytotoxicity of the DPAs is at least partly due to a greater incorporation of the drugs into the hepatocyte plasmalemma compared to compounds in other chemical classes investigated, although further studies are required to elucidate the particular cytotoxic mechanisms involved.
N-dephenylation of CERM 3517 (mociprazine) in beagle dogs. A mass spectrometric determination.
CERM 3517 (mociprazine), a new antiemetic compound, was administered orally at 10 mg/kg twice a day for 4 days to six Beagle dogs in order to identify the major metabolite. Mass spectrometric
Comparative study of the biotransformation of bepridil analogs in isolated liver cells from one rat. Relationships between structure and in vitro liver toxicity
The biotransformation of several analogs of the anti-calcium agent bepridil was studied comparatively in liver cells isolated from one rat, finding thatortho-substituted analogs were more toxic thanpara- ormeta-subStituted ones.