| abstract |
Fluorogenic substrates for proteolytic enzymes having the formula: (FORMULA) or their acid salts or: R1 is hydrogen-L, hydrogen-D, benzoyl, benzene-sulfonyl, glutaryl, pyroglutamyl, carbobenzoxy, D-serine, or carbobenzoxyserine; R2 is hydrogen, phenyl, branched or cyclic linear alkyl having 1 to 4 carbon atoms, or propionic acid; R3 is hydrogen, linear or branched or cyclic alkyl having 1 to 4 carbon atoms, 4-aminobutane, or 3-guanidylpropane; R4 is methyl, 4-aminobutane, or 3-guanidylpropane; R5 is a fluorogenic fraction, separable from said compound by a proteolytic enzyme and having a different fluorescent property when it is separated from said compound than when it is part of it. The enzymes when they react with the substrate, remove the fluorogenic group R5 producing an increase in its fluorescence. The increase in fluorescence is an indication of the activity of the enzyme present. Specific enzymes thus detectable include plasmin, thrombin, factors Xa, XIa, & XIIa, callicrein, trypsin, elastase, uroquinase, and cathepsin B1. |