Cilastatin (MK 0791) is a potent and specific inhibitor of the renal leukotriene D4-dipeptidase.
The metabolism of leukotriene D4 to leukotriene E4 by a dipeptidase of kidney tissue is strongly inhibited by cilastatin (MK 0791) a known renal dehydropeptidase-I inhibitor. The comparison with similar enzyme activities from other tissues (liver, lung, serum, polymorphonuclear granulocytes) revealed a high specificity of cilastatin for the kidney enzyme which was found to be associated with the microsomal fraction. The lowest detectable inhibitory concentration of cilastatin within renal tissue was 8 X 10(-8)M.
D000818:Animals; D015377:Cilastatin; D003521:Cyclopropanes / Q000494:pharmacology*; D004150:Dipeptidases / Q000037:antagonists & inhibitors* / Q000097:blood; D006801:Humans; D007668:Kidney / Q000201:enzymology*; D008099:Liver / Q000201:enzymology; D008168:Lung / Q000201:enzymology; D008861:Microsomes / Q000201:enzymology; D009504:Neutrophils / Q000201:enzymology; D011817:Rabbits; D013189:SRS-A / Q000378:metabolism
D003521:Cyclopropanes; D013189:SRS-A; D015377:Cilastatin; D004150:Dipeptidases; C036942:leukotriene D4 dipeptidase