SDZ-MKS 492 (MKS 492) is a selective inhibitor of cyclic GMP-inhibited phosphodiesterase (type III PDE). SDZ-MKS 492 inhibits antigen- or platelet activating factor (PAF)-induced bronchoconstriction and allergic reactions in guinea pigs and rats.
IC50&Target
type III phosphodiesterase
体外研究
MKS 492 relaxes airway smooth muscle in vitro.
体内研究
MKS-492 (3-10 mg/kg; i.v.) inhibits antigen-induced bronchoconstriction in guinea pigs.
MKS-492 (1-3 mg/kg; i.v.) inhibits PAF-induced bronchoconstriction and the increase in airway responsiveness to histamine in guinea pigs.
MKS-492 (30-100 mg/kg; i.p.) inhibits leukotriene B4 (LTB4)-induced airway eosinophilia in guinea pigs.
MKS-492 (10-100 mg/kg; i.p.) inhibits passive cutaneous anaphylaxis and mediator-induced skin reactions in rats.
Animal Model:
Female Hartley guinea pigs (250-300 g) were passively sensitized with anti-BPO BGG guinea pig serum
Dosage:
3, 10 mg/kg
Administration:
I.v. 5 min before antigen challenge
Result:
Inhibited antigen-induced bron choconstriction in a dose-related manner.
分子式
C20H27N5O6
分子量
433.46
CAS号
114606-56-3
运输条件
Room temperature in continental US; may vary elsewhere.