New synthetic inhibitor to the alternative complement pathway

Immunology. 1983 Aug;49(4):685-91.

Abstract

The inhibitory effects of 6-amidino-2-naphthyl 4-guanidinobenzoate (FUT-175) on the activities of factor B, factor D and cobra venom factor (CVF) X Bb were examined. FUT-175 bound specifically to the Bb fragment of factor B or CVF X Bb. FUT-175 was a non-competitive inhibitor of the esterolysis of L-leucyl-L-alanyl-L-arginine naphthylester by factor B and CVF X Bb. FUT-175 also inhibited the haemolytic activity of factor B, the C3 convertase activity of CVF X Bb and the factor B-cleaving activity of factor D. The concentration of FUT-175 causing 50% inhibition of these activities was 10(-5) - 10(-4)M.

MeSH terms

  • Animals
  • Benzamidines
  • Complement Activation / drug effects*
  • Complement Factor B / antagonists & inhibitors
  • Complement Factor D / antagonists & inhibitors
  • Complement Inactivator Proteins / pharmacology*
  • Complement Pathway, Alternative / drug effects*
  • Dose-Response Relationship, Drug
  • Elapid Venoms / antagonists & inhibitors
  • Electrophoresis, Polyacrylamide Gel
  • Guanidines / pharmacology*
  • Hemolysis / drug effects
  • Humans
  • In Vitro Techniques
  • Rabbits

Substances

  • Benzamidines
  • Complement Inactivator Proteins
  • Elapid Venoms
  • Guanidines
  • cobra venom factor
  • CFD protein, human
  • Complement Factor D
  • Complement Factor B
  • nafamostat