Inhibition of C1s-induced vascular leakage in guinea pigs by substituted benzamidine and pyridinium compounds.
A variety of benzamidine and pyridinium compounds were examined for their ability to inhibit irreversibly C1s-induced vascular leakage in guinea pig skin. Vascular leakage was compared with esterolysis of N-Z-L-Tyr-Np and catalysis of EAC42 formation by C1s. Vascular leakage correlated significantly better with esterolytic activity than with EAC42 formation. The presence of a sulfonyl fluoride moiety in the compounds is important in the inhibition of C1s-induced vascular leakage.
D000578:Amidines / Q000494:pharmacology*; D000818:Animals; D001550:Benzamidines / Q000494:pharmacology*; D002199:Capillary Permeability / Q000187:drug effects*; D003172:Complement C1 / Q000378:metabolism*; D003165:Complement System Proteins / Q000378:metabolism*; D004952:Esters; D005260:Female; D005459:Fluorides / Q000378:metabolism; D006168:Guinea Pigs; D006801:Humans; D007158:Immunologic Techniques; D007536:Isomerism; D009578:Nitrobenzenes / Q000378:metabolism; D011726:Pyridinium Compounds / Q000494:pharmacology*; D012867:Skin / Q000098:blood supply* / Q000648:ultrastructure; D014443:Tyrosine / Q000378:metabolism
D000578:Amidines; D001550:Benzamidines; D003172:Complement C1; D004952:Esters; D009578:Nitrobenzenes; D011726:Pyridinium Compounds; D014443:Tyrosine; D003165:Complement System Proteins; D005459:Fluorides