Radioimmunoassay for Clebopride, a New Benzamide Drug with Antidopaminergic Activity

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A radioimmunoassay method has been developed for the measurement of low concentrations of clebopride in human serum and urine samples. Antisera (clebopride-binding antibodies) were obtained from albino rabbits eight weeks after the first injection of clebopride-bovine serum albumin (BSA) conjugates. The antisera, ³H-antigen and human serum (or urine) samples or standard clebopride solutions were used in the incubation mixtures for the assay. The method has been found to be very specific, because although clebopride is extensively metabolized in man, only clebopride and its glucuronide conjugate were found to be susceptible to the antisera. The unchanged drug could be separated from the conjugate by ether-extraction prior to assay. The limit of sensitivity of this method is 0.1 ng of clebopride per ml of sample and is sufficient to measure clebopride concentrations in serum and urine of human subjects after oral administration of the therapeutic dose of 0.5 mg per man. Serum concentration profiles and some of the pharmacokinetic properties of clebopride in man have been elucidated for the first time.