7b-Acetoxy-8,13-epoxy-1a,6b,9a-trihydroxy-labd-14-en-11-one Colforsin White to off-white crystalline solid. The major cell-permeable diterpene isolated from the Indian plant Coleus forskohlii. At low doses, it acts as a positive inotropic agent. At higher doses, it serves as a hypotensive and vasodilatory agent due to its actions as a smooth muscle relaxant. No major side effects are observed at effective doses. Forskolins pharmacological activities are due to its activation of adenylate cyclase (EC50 = 4 µM), resulting in increased cAMP levels. The exact mechanism of forskolins positive inotropic effect is unknown but may be related to a cAMP-dependent increase in Na+ permeability that results in indirect augmentation of Ca2+ release. Inhibits MAP kinase in rat renal mesangial cells (IC50 = 25 µM). Also acts as a Hh pathway antagonist. Shown to inhibit apoptosis in cerebellar granule cells and to induce apoptosis in resting human B lymphocytes. Purity: ≥99% by HPLC. RTECS QL6150000, CAS 66575-29-9. Merck Index: 14, 2476 Ref.: D'Orazio, J.A., et al. 2006. Nature 443, 340. Noveen, A., et al. 1996. Biochem. Biophys. Res. Commun. 219, 180. Galli, C., et al. 1995. J. Neurosci. 15, 1172. Li, X., et al. 1995. Am. J. Physiol. 269, C986. Lomo, J., et al. 1995. J. Immunol. 154, 1634. Uneyama, H., et al. 1993. J. Biol. Chem. 268, 168. Laurenza, A., et al. 1989. Trends Pharmacol. Sci. 10, 442. Adashi, E.Y., and Resnick, C.E. 1986. J. Cell. Biochem. 31, 217. Seamon, K.B., and Daly, J.W. 1986. Adv. Cyclic Nucleotide Protein Phosphorylation Res. 20, 1. Huang, R., et al. 1982. Cyclic Nucleotide Res. 8, 385. Metzger, H., and Lindner, E. 1981. IRCS Med. Sci. Biochem. Cardiovasc. System Pharmacol. 9, 99. R: 21; S: 36 |