Compound R 24571 White solid. A cell-permeable calmodulin antagonist. At least 150 times more potent than Trifluoperazine (Cat. No. 642150) as an inhibitor of brain calmodulin-dependent phosphodiesterase (IC50 = 10 nM). An inhibitor of voltage-gated Ca2+ channels. Stimulates the release of nitric oxide in neuroblastoma cells. Also acts as a strong non-competitive inhibitor of skeletal muscle sarcoplasmic reticulum Ca2+-ATPase (Ki = 60 nM). Known to prolong cardiac refractoriness in vivo. Purity: ≥98% by TLC. CAS 57265-65-3. Note: easily adheres to glass in aqueous solution. Ref.: Hu, J., and El-Fakahany, E.E. 1993. NeuroReport. 4, 198. Nakazawa, K., et al. 1993. Br. J. Pharmacol. 109, 137. Yuasa, T., and Muto, S. 1992. Arch. Biochem. Biophys. 296, 175. Ichikawa, M., et al. 1991. J. Membrane Biol. 120, 211. Silver, P.J., et al. 1989. Cardiovasc. Drug Ther. 3, 675. Anderson, K.W., et al. 1984. J. Biol. Chem. 259, 11487. Gietzen, L., et al. 1982. Biochem. J. 207, 541. Van Belle, H. 1981. Cell Calcium 2, 483. Levin, R.N., and Weiss, B. 1979. J. Pharmacol. Exp. Therap. 208, 454. |
