• Corpus ID: 24017523

Biotransformation of nitrendipine in rat, dog, and mouse.

  title={Biotransformation of nitrendipine in rat, dog, and mouse.},
  author={Dietrich Scherling and Wolfgang Karl and Hans Juergen Ahr and Armin Kern and H. M. Siefert},
  volume={41 10},
14C-Labelled Nitrendipine (Bay e 5009; Baypress, Bayotensin; CAS 39562-70-4) was administered by the oral and intraduodenal route to rats, dogs, and mice (oral dosing only) to elucidate the biotransformation pathways in these three species. The drug was extensively metabolized: 20 biotransformation products were identified by comparison with synthetic reference compounds using two-dimensional TLC, HPLC, GC/radio-GC, combined GC/MS (EI-, CI-mode), FAB-MS, and 1H-NMR-spectroscopy. The metabolites… 
Metabolic fate of a new dihydropyridine calcium antagonist, CD-349, in rat and dog.
The low ratio of unchanged drug to total radioactivity in plasma suggested that 14C-CD-349 underwent rapid metabolism in both species, and principal routes of biotransformation of CD-349 were similar in bothspecies, although quantitative interspecies differences were observed.
Metabolism of the dihydropyridine calcium channel blockers mebudipine and dibudipine by isolated rat hepatocytes
These newer 1,4‐DHPs address the problem of the short half‐life of nifedipine and have potential for further development in view of their comparable potency to nifingipine.
Importance of metabolic stability and hepatic distribution to the pharmacokinetic profile of amlodipine.
In an isolated perfused rat liver (IPRL) model, the extensive hepatic uptake and subsequent slow redistribution of amlodipine into the perfusate have been demonstrated and the discrepancy between relative clearance rates for the two preparations may be explained by consideration of the hepatic volume of the two compounds.
In vitro to in vivo extrapolation and physiologically based modeling of cytochrome P450 mediated metabolism in beagle dog gut wall and liver.
This study demonstrates an approach for prediction of the gut wall extraction of CYP substrates in the beagle dog, thus enhancing the value of dog studies as a component in a strategy for the prediction of human pharmacokinetics.
Systematic toxicological analysis procedures for acidic drugs and/or metabolites relevant to clinical and forensic toxicology and/or doping control.
  • H. Maurer
  • Chemistry, Medicine
    Journal of chromatography. B, Biomedical sciences and applications
  • 1999
STA procedures for acidic drugs and/or metabolites relevant to clinical and forensic toxicology or doping control using gas Chromatography, gas chromatography-mass spectrometry, liquid chromatography, thin-layer chromatography and capillary electrophoresis are reviewed.
Pharmacokinetics and bioavailability of a newly synthesized dihydropyridine compound with multidrug resistance reversal activity
The terminal half‐life of (±)‐DHP‐014 increased and the systemic clearance significantly decreased at higher doses, indicating nonlinear elimination, and the dose‐dependent clearance is likely due to saturation of metabolism.
Evaluating the clinical importance of bacterial degradation of therapeutic agents in the lower intestine of adults using adult fecal material
Optimal fecal material composition was based on recently reported degradation profiles of metronidazole and olsalazine in the lower intestine of healthy adults which are clinically important, and data in SCoB only are useful for evaluating whether bacterial degradation in P‐COL and in D‐SI is likely to be clinically important for orally administered, highly permeable drugs or prodrugs which act locally after bacterial degradation.