RADIOIMMUNOASSAY OF ANTI-HYPERTENSIVE AGENT DEBRISOQUIN

  • 1 January 1977
    • journal article
    • research article
    • Vol. 16  (1) , 121-129
Abstract
Antisera to debrisoquin, a widely used anti-hypertensive agent, were obtained from rabbits following immunization with a conjugate of 4-[(1,2,3,4-tetrahydroisoquinolin-2-yl)(imino)-methylamino] butanoic acid and bovine serum albumin. Employing tritium labeled debrisoquin as the radioligand for the antisera, a radioimmunoassay (RIA) was developed which allows for the specific determination of the drug directly in plasma. After logit transformation, a linear calibration line was obtained between 0.1-10 ng of unlabeled debrisoquin. The 4, 5, 6, 7 and 8-hydroxy derivatives of debrisoquin, known metabolites in man, showed less than 1.5% cross-reaction with the antisera. The specificity of the RIA was established when good agreement was obtained for the levels of debrisoquin in patients'' plasma using the RIA and a specific GC/MS [gas chromatography-mass spectrometry] method. The simplicity of the RIA makes this method attractive for the routine clinical monitoring of the plasma levels and/or experimental protocols in which high sample throughput is required.

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