Renal dehydropeptidase-I stability of LJC 10,627, a new carbapenem antibiotic.
LJC 10,627 is a new parenteral carbapenem antibiotic. LJC 10,627 stability against human renal dehydropeptidase-I was compared with that of imipenem. Hydrolysis of this compound was not detectable by spectrophotometrical assay. Even after a 2-h incubation of antibiotics with this enzyme at 30 degrees C, the concentration of LJC 10,627 remained at 92.3% of the initial concentration, whereas imipenem completely disappeared. Thus, it was found that this compound was highly stable against human renal dehydropeptidase-I. Furthermore, LJC 10,627 had a low affinity for this enzyme, as indicated by the high Ki value (0.38 mM).
Hikida
M
M
Biological Research Laboratories, Lederle Ltd., Saitama, Japan.
Kawashima
K
K
Nishiki
K
K
Furukawa
Y
Y
Nishizawa
K
K
Saito
I
I
Kuwao
S
S
D000818:Animals; D015780:Carbapenems / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D004150:Dipeptidases / Q000378:metabolism*; D006801:Humans; D006868:Hydrolysis; D015378:Imipenem / Q000378:metabolism; D066298:In Vitro Techniques; D007668:Kidney / Q000201:enzymology*; D007700:Kinetics; D008252:Macaca fascicularis; D013056:Spectrophotometry, Ultraviolet; D013552:Swine; D013845:Thienamycins
D015780:Carbapenems; D013845:Thienamycins; D015378:Imipenem; D004150:Dipeptidases; C038937:dipeptidase; C065257:biapenem