P. Ascenzi et al., COMPETITIVE-INHIBITION OF MOUSE-BRAIN NITRIC-OXIDE SYNTHASE BY AMILORIDE - A CASE FOR ENZYME CROSS-INHIBITION, Biochemistry and molecular biology international, 43(3), 1997, pp. 507-511
Amiloride, a diuretic and antihypertensive drug, inhibits Na+ transpor
ting systems, diamine oxidases and the human urinary plasminogen activ
ator. Present results indicate that amiloride is a competitive inhibit
or of mouse brain nitric oxide synthase (NOS; K-i = 4.5x10(-4) M, at p
H 7.5 and 37.0 degrees C), but not a nitric oxide (NO) precursor, repr
esenting a case for enzyme cross-inhibition. The decreased levels of N
O, as a consequence of NOS inhibition, might induce some clinically-ad
verse amiloride reactions, such as an unexpected reduced antihypertens
ive effect.