ANALYTICAL AND PHARMACOKINETIC STUDIES WITH AN ANTIVIRAL LECTIN DERIVATIVE (MEETING ABSTRACT)

Important note: Information in this article was accurate in 1992. The state of the art may have changed since the publication date.

ANALYTICAL AND PHARMACOKINETIC STUDIES WITH AN ANTIVIRAL LECTIN DERIVATIVE (MEETING ABSTRACT)

Proc Annu Meet Am Assoc Cancer Res; 33:A3177 1992. Unique Identifier : AIDSLINE ICDB/92685712
Moore AL; Chrin LR; Mathews LA; McCormack JJ; Dept. of Pharmacology, Univ. of Vermont, Burlington, VT 05405

Abstract: NSC 619858 (SCA) is a succinylated derivative of concanavalin A that has shown provocative activity against HIV in vitro. SCA can be detected using a standard ELISA, as well as a modified ELISA, in representative biological fluids and tissue extracts obtained from mice. Concentrations of SCA as low as 1 ng/ml can be detected in mouse plasma and urine using ELISA; plots of concentration (log) vs absorbance show good linearity, and assay reproducibility is satisfactory (+/- 5% on separate days). SCA is stable in mouse plasma and neutral aqueous solutions for periods of up to 24 hr at 37 degrees as judged by ELISA and other methods (eg, PAGE). Centrifugal ultrafiltration studies indicate extensive binding (greater than 99%) to model proteins such as BSA. Iv administration of SCA (50 mg/kg) to mice resulted in plasma concentrations in the 800-900 ug/ml range 10 min after injection; elimination of SCA from plasma was relatively rapid (half-life of 30 min). In addition to the rapid elimination phase, there appears to be a much slower elimination phase (half-life 8 hr). The estimated Vd was approx 1 ml and the estimated clearance was 1 ml/hr. SCA was detectable in plasma samples taken at 24 and 48 hr, but not at 72 hr after iv administration. Only 1% of the administered SCA is accounted for in urine collected for 24 hr after iv administration. SCA is detected readily in tissues such as liver, kidney and small intestine, but not in brain, within 1 hr after injection.

Keywords: Animal Antiviral Agents/ADMINISTRATION & DOSAGE/ANALYSIS/ *PHARMACOKINETICS Concanavalin A/ADMINISTRATION & DOSAGE/ANALYSIS Enzyme-Linked Immunosorbent Assay Half-Life Injections, Intravenous Metabolic Clearance Rate Mice Organ Specificity Tissue Distribution Ultrafiltration ABSTRACT
920930
M9290907

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