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CGS 9343B is a calmodulin inhibitor.1,2,3 It inhibits calmodulin-induced phosphodiesterase (PDE) activity (IC50 = 3.3 µM) but does not inhibit basal PKC activity at 100 µM.2 CGS 9343B (120 µM) inhibits calcium release induced by inositol 1,4,5-trisphosphate (IP3) in 261B rat liver epithelial cells.2 It reduces the incidence of diarrhea without affecting gastrointestinal transit time in a mouse model of secretory diarrhea induced by castor oil when administered at a dose of 3 mg/kg.3
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1. CGS 9343B, a novel, potent, and selective inhibitor of calmodulin activity. Mol. Pharmacol. 31(5), 535-540 (1987).
2. Inhibition of inositol trisphosphate-
3. Novel calmodulin antagonist CGS 9343B inhibits secretory diarrhea. J. Pharmacol. Exp. Ther. 251(1), 247-252 (1989).