Accession Number : ADA307633

Title :   Preclinical Pharmacodynamic and Pharmacokinetic Studies of Investigational New Drugs.

Descriptive Note : Annual rept. 2 Nov 94-1 Nov 95,

Corporate Author : SOUTHERN RESEARCH INST BIRMINGHAM AL

Personal Author(s) : Noker, Patricia E.

PDF Url : ADA307633

Report Date : NOV 1995

Pagination or Media Count : 74

Abstract : During the past year of this contract, efforts were focused on isolating and identifying the urinary and fecal metabolites eliminated following administration of either 14Chi-6, 14Cpahp or 14Cwr242511 to dogs and to rats (PAHP only). Identification of the metabolites was based on mass spectral, UV absorbance and chromatographic data. Metabolites eliminated by dogs following administration of 14Chi-6 have been tentatively identified and include 2-pyridine aldoxime, a pyridone derivative of H-6 and picolinic acid. In dogs administered 14Cpahp, evidence was obtained for the elimination 6-4'-HYDROXYAMINOBENZOYLhexanol and 6-4'-HYDROXYAMINOBENZOYLhexanoate, as well as other radiolabeled metabolites, in urine. In rats administered 14Cpahp, one urinary metabolite was tentatively identified as hydroxyaminobenzoylhexanol. Preliminary data indicate that following administration of 14Cwr242511 to dogs, at least one metabolite eliminated in urine is a dealkylated derivative of the compound. Further efforts to isolate and identify the other urinary metabolites of these compounds, and the fecal metabolites of PAHP, are in progress.

Descriptors :   *PHARMACOKINETICS, *DRUGS, *PHARMACOLOGY, RATS, MASS, CLINICAL MEDICINE, IDENTIFICATION, FECES, DOGS, METABOLITES, URINE, LABELED SUBSTANCES, RADIOACTIVE ISOTOPES, CHROMATOGRAPHS.

Subject Categories : Pharmacology
      Biochemistry

Distribution Statement : APPROVED FOR PUBLIC RELEASE