Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM. Zaldaride maleate (CGS-9343B) prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na, Ca and K currents in PC12 cells and inhibits nAChR.
体内研究
Zaldaride maleate (KW 5617, P.O., 3 mg/kg) ameliorates the diarrhea in the 16, 16-dimethyl prostaglandin E2 model.
Animal Model:
Male Sprague-dawley rats neighing 193-265 g.
Dosage:
3-100 mg/kg.
Administration:
P.O..
Result:
KW-5617 at 3 to100 mg/kg 60 min before DMPGE2 challenge, significantly ameliorated the DMPGE-induced diarrhea, when this drug at 100 mg/kg (p.o. significantly reduced fecaevacuation.
Pretreatment with KW-5617 at 3 to 10 mg/kg (p.o.) significantly delayed the onset of diarrhea, and this drug at 30 and 100 mg/kg (p.o. ) reduced or abolished the incidence of diarrhea.
分子式
C26H28N4O2.C4H4O4
分子量
544.60
CAS号
109826-27-9
运输条件
Room temperature in continental US; may vary elsewhere.