Analytical studies and murine pharmacokinetics of quinobene (Meeting abstract). NLM AIDSLINE Important note: Information in this article was accurate in 1993. The state of the art may have changed since the publication date.

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Analytical studies and murine pharmacokinetics of quinobene (Meeting abstract).

Proc Annu Meet Am Assoc Cancer Res; 34:A2368 1993. Unique Identifier : AIDSLINE ICDB/93693320
Bigelow J; Mathews L; McCormack J; Dept. of Pharmacology, Univ. of Vermont, Burlington, VT 05405

Abstract: Quinobene (QB; NSC 638352 ) is a sulfonated stilbene derivative that also contains aromatic azo and hydroxyquinoline substituents. QB has anti-HIV activity in vitro in the micromolar range. We have developed an assay for QB that is suitable for use with biological fluids. Samples are prepared for analysis by treatment with ammonium sulfate and methanol. HPLC analysis is accomplished with a polymeric reversed-phase column and gradient elution (pH 6 citrate buffer/methanol); QB and derived compounds are detected by visible spectroscopy (540 nm). After iv administration of QB (25 mg/kg) to mice, 'peak' plasma concentrations are in the 20-40 uM range and elimination of the drug from plasma appears to be biexponential (half-lives of 5 and 100 min). Estimated values for AUC, Vd and Cl are 3000 umol/L x min, 8 ml, and 0.2 ml/min, respectively. The pharmacokinetic profile for QB in mice is comparatively complex and involves rapid formation of a major metabolite (less well retained than QB on HPLC) and apparently facile association with tissues. Little, if any, QB is absorbed after oral dosing and absorption after ip dosing is inefficient.
Keywords: Animal Antiviral Agents/*PHARMACOKINETICS Biological Availability Half-Life HIV/DRUG EFFECTS Infusions, Intravenous Metabolic Clearance Rate/PHYSIOLOGY Mice Stilbenes/*PHARMACOKINETICS ABSTRACTKWDanimalantiviralagents/KWDpharmacokineticsbiologicalavailabilityhalf-lifehiv/drugeffectsinfusions,intravenousmetabolicclearancerate/physiologymicestilbenes/KWDpharmacokineticsabstract
931030
M93A0773

Copyright © 1993 - National Library of Medicine. Reproduced under license with the National Library of Medicine, Bethesda, MD.

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