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- W2024349013 abstract "Zabicipril (Z), a new angiotensin-converting-enzyme inhibitor under development, is a prodrug that has to be deesterified in vivo to the active metabolite, zabiciprilat (ZT), to reach its antihypertensive pharmacological properties. Two radioimmunoassays have been developed for the measurement of both Z and ZT in human plasma. Anti-Z and anti-ZT antibodies were raised in rabbits against their respective lysine analogues conjugated to bovine serum albumin. [3H]Z and [3H]ZT were used as radioligands for the prodrug (Z) and the drug (ZT), respectively. Studies on anti-Z antiserum specificity showed no significant cross-reactivity (< 0.1%) with the active metabolite (ZT); similarly, Z is poorly recognized (0.5%) by the anti-ZT antiserum. Both antisera showed little cross-reaction (2%) with glucuronide metabolites. The sensitivities of the assays were 1 and 0.2 ng/mL for Z and ZT, respectively. Interassay coefficients of variation ranged from 9 to 12% for Z at 2–50 ng/mL and from 8 to 13% for ZT at 0.5–5 ng/mL. These assays were used to investigate the pharmacokinetic profile of both Z and its pharmacologically active metabolite ZT after intravenous infusion of Z in human volunteers." @default.
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- W2024349013 date "1992-11-01" @default.
- W2024349013 modified "2023-09-27" @default.
- W2024349013 title "Radioimmunoassays for a New Angiotensin-Converting Enzyme Inhibitor, Zabicipril, and its Active Metabolite, Zabiciprilat, in Human Plasma" @default.
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- W2024349013 doi "https://doi.org/10.1002/jps.2600811104" @default.
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