emopamil

Emopamil is a small molecule phenylalkylamine calcium channel antagonist and P-glycoprotein (P-gp) inhibitor. It has been studied for its ability to prevent renal injury after warm and cold ischemia and can reduce ischemia-induced neuronal cell damage. Emopamil also reverses multidrug resistance in certain cancer cell lines by inhibiting P-glycoprotein. Mechanistically, it acts as a calcium channel blocker and binds with high affinity to the emopamil binding protein (EBP), which is involved in cholesterol biosynthesis as a Δ8–Δ7 sterol isomerase. The drug has optically active stereoisomers; the racemic mixture and (-)-enantiomer are pharmacologically active while the (+)-enantiomer is not effective. Emopamil reached up to Phase II clinical trials but development appears discontinued[1][2][3][4].

Other names

emopamiloemopamilum2-isopropyl-5-(methyl-(2-phenylethyl)amino)-2-phenylpentanenitrile