A Radioimmunoassay for MC-838 (Altiopril Calcium), a Novel Angiotensin-Converting Enzyme Inhibitor

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A radioimmunoassay was developed for a new, potent inhibitor of angiotensin-converting enzyme (ACE, EC 3.4.15.1), calcium (-)-N-[(S)-3-[(N-cyclohexylcarbonyl-D-alanyl) thio]-2-methylpropionyl]-L-prolinate (MC-838,altiopril calcium). The antiserum was obtained by immunizing rabbits with MC-838-bovine serum albumin (BSA) conjugate. MC-838-L-tyrosine labeled with ^<125>I and purified by thin-layer chromatography was used as a tracer. The assay sensitivity was 0.1 ng/ml, the average intra-assay coefficient of variation was 7.9%, and the average inter-assay coefficient of variation was 13.7%. The antiserum was specific for MC-838,showing only slight crossreactivity with degradation products of MC-838. After a single oral dose of MC-838 (2 mg/kg), radioimmunoassay of MC-838 canine serum demonstrated rapid absorption from the gastrointestinal tract with a peak level of 40.6 ng/ml. The decline in serum concentration was a biphasic decay, with a half-life of 80 min during rapid falloff followed by a slower decline.
公益社団法人日本薬学会の論文