Aromatic diamidines are reversible inhibitors of porcine kidney diamine oxidase.
The inhibitory ability of aromatic diamidines has been studied on porcine kidney diamine oxidase. The reversibility of drug-protein interactions has been tested by means of exhaustive dialysis experiments, showing in all cases a reversible binding pattern. Ki values obtained by means of Lineweaver-Burk plots were: stilbamidine 12 microM, 2-OH-stilbamide 8.5 microM, phenamidine 4 microM, propamidine 8 microM, dibromopropamidine 4.9 microM and amicarbalide 12 microM.
Cubría
J C
JC
Departamento de Fisiología, Farmacología y Toxicología, Facultad de Veterinaria, Universidad de León, Spain.
Balaña Fouce
R
R
Alvarez-Bujidos
M L
ML
Negro
A
A
Ortiz
A I
AI
Ordóñez
D
D
D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy; D006631:Amine Oxidase (Copper-Containing) / Q000037:antagonists & inhibitors*; D000818:Animals; D001550:Benzamidines / Q000494:pharmacology; D001665:Binding Sites; D004133:Diminazene / Q000031:analogs & derivatives* / Q000494:pharmacology; D007668:Kidney / Q000187:drug effects* / Q000201:enzymology; D007700:Kinetics; D010419:Pentamidine / Q000494:pharmacology*; D013266:Stilbamidines / Q000494:pharmacology; D013552:Swine
D001550:Benzamidines; D013266:Stilbamidines; C001787:phenamidine; D010419:Pentamidine; D006631:Amine Oxidase (Copper-Containing); C005555:propamidine; C003915:diminazene aceturate; C042560:stilbamidine; D004133:Diminazene