Description
REV 5901 is an antagonist of cysteinyl-
leukotriene receptors with a K
i value of 0.7 μM for guinea pig lung membranes. It is also an inhibitor of rat neutrophil 5-
LO with an IC
50 value of 0.12 μM.
Uses
L-655,238 is a potent and selective inhibitor of FLAP (5-LO-activating protein).
Uses
REV 5901 is an antagonist of cysteinyl-leukotriene receptors with a Ki value of 0.7 μM for guinea pig lung membranes. It is also an inhibitor of rat neutrophil 5-LO with an IC50 value of 0.12 μM.
Definition
ChEBI: 1-[3-(2-quinolinylmethoxy)phenyl]-1-hexanol is a member of quinolines.
in vitro
previous in-vitro showed that rev 5901 had a ki value of 0.7 μm vs. [3h]leukotriene d4 ([3h]-ltd4) binding to membranes from guinea pig lung. against ltc4-, ltd4- and lte4-induced contractions of guinea pig parenchymal strips, rev 5901 had kb values of ca 3 μm and was relatively ineffective against contractions that was induced by other spasmogens. moreover, in isolated guinea pig hearts, the peptiodoleukotriene-antagonist activity was also observed against the hemodynamic and vasoconstriction effects of ltd4. in addition, unlike other reported antagonists, rev 5901 was found to be ineffective against the multiple forms of cyclic nucleotide phosphodiesterases [1].
in vivo
animal study found that the oral antagonist activity had been shown with an ltd4-induced bronchoconstriction model and with an ltd4-induced wheal response model in guinea pigs [1].
References
[1] van inwegen, r. g.,khandwala, a.,gordon, r., et al. rev 5901: an orally effective peptidoleukotriene antagonist, detailed biochemical/pharmacological profile. journal of pharmacology and experimental therapeutics 241, 117-124 (1987).
