Warfarin enantiomer disposition: determination by stereoselective radioimmunoassay. 1979

C E Cook, and N H Ballentine, and T B Seltzman, and C R Tallent

Immunoassay techniques offer promise for the selective analysis of enantiomeric substances without prior separation. In a demonstrationof this selective analysis, radioimmunoassays were developed for R- and S-warfarin. The 4'-carboxyethyl analog of R,S-warfarin was resolved and the enantiomeric acids were coupled to bovine serum albumin. Immunization of rabbits with the conjugates led to formation of antisera which selectively bound the predicted enantiomer. Cross-reactions with various metabolites of warfarin were low (0.1--4%) except for 4'-hydroxywarfarin, as were cross-reactions with the opposite enantiomer (0.3--3%). Assays were developed and used to determine enantiomer half-lives in rats dosed with racemic warfarin. Results were consistent with those found previously by administration of individual enantiomers, thus indicating the utility of the radioimmunoassay method.

UI MeSH Term Description Entries
D008297 Male Males
D008722 Methods A series of steps taken in order to conduct research. Techniques,Methodological Studies,Methodological Study,Procedures,Studies, Methodological,Study, Methodological,Method,Procedure,Technique
D011863 Radioimmunoassay Classic quantitative assay for detection of antigen-antibody reactions using a radioactively labeled substance (radioligand) either directly or indirectly to measure the binding of the unlabeled substance to a specific antibody or other receptor system. Non-immunogenic substances (e.g., haptens) can be measured if coupled to larger carrier proteins (e.g., bovine gamma-globulin or human serum albumin) capable of inducing antibody formation. Radioimmunoassays
D003429 Cross Reactions Serological reactions in which an antiserum against one antigen reacts with a non-identical but closely related antigen. Cross Reaction,Reaction, Cross,Reactions, Cross
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000917 Antibody Formation The production of ANTIBODIES by proliferating and differentiated B-LYMPHOCYTES under stimulation by ANTIGENS. Antibody Production,Antibody Response,Antibody Responses,Formation, Antibody,Production, Antibody,Response, Antibody,Responses, Antibody
D000941 Antigens Substances that are recognized by the immune system and induce an immune reaction. Antigen
D012710 Serum Albumin, Bovine Serum albumin from cows, commonly used in in vitro biological studies. (From Stedman, 25th ed) Fetal Bovine Serum,Fetal Calf Serum,Albumin Bovine,Bovine Albumin,Bovine Serum Albumin,Albumin, Bovine,Albumin, Bovine Serum,Bovine Serum, Fetal,Bovine, Albumin,Calf Serum, Fetal,Serum, Fetal Bovine,Serum, Fetal Calf
D013237 Stereoisomerism The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed) Molecular Stereochemistry,Stereoisomers,Stereochemistry, Molecular,Stereoisomer

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