CV-159

CV-159 is a unique dihydropyridine Ca²⁺ antagonist with an anti-calmodulin (CaM) action, and has antiinflammatory activities. In Vitro: CV-159 (0.1-10 μM) significantly inhibits TNF-α (10 ng/ml, 24 h)-induced VCAM-1 in SMCs in a concentrationdependent manner. CV-159 (10 μM, 30 min) significantly inhibits the TNF-induced ROS production^[1]. CV-159 (10 μM) inhibits TNF (24 h)-induced expression of e-selectin but not vascular cell adhesion molecule-1 and intercellular adhesion molecule-1. CV-159 inhibits TNF (20 min)-induced phosphorylation of JNK, p38, and NF-κB p65 (Ser536)^[2]. In Vivo: CV-159 (5 and 10 mg/kg, p.o.) gives significant protection against delayed neuronal death in the hippocampal CA1 region of the rats after 15-min transient forebrain ischemia. CV-159 also diminishes the size of the brain infarct after permanent middle cerebral artery (MCA) occlusion. CV-159 significantly reduces the increase in the water content of the infarcted cortex induced by MCA occlusion^[3].