Chromogen-substrate assay--as a tool for monitoring a new thrombin inhibitor.

作者: L. Vereczkey , K. Rasky , M. Patfalusi

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摘要: The N-methyl-D-phenylalanyl-L-prolyl-arginine-aldehyde sulfate tripeptide-aldehyde (GYKI-14766) is an anticoagulant with specific thrombin inhibitor action. molecule proved to be effective in rabbits, rats and dogs upon i.v. administration. Chromogen-substrate assay was developed for monitoring of biologically active tripeptide-inhibitor GYKI-14766 plasma. based on the inhibition center enzyme, so it suitable also all those metabolites which inhibit by a mechanism similar parent compound. chromogen substrate performed range 0.625-10 micrograms/ml dog employed pharmacokinetic study after data obtained chromogen-substrate were analyzed according one-compartment model. major parameters plasma level studies were: D/V = 8.6 microEqv/ml t1/2 30.8 min AUC 380 microEqv/ml.

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