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 ?M), 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 ?M). Also acts as
a Hh pathway antagonist. Shown to inhibit apoptosis in cerebellar granule cells and to induce apoptosis in resting human B lymphocytes.
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Form
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White to off-white crystalline solid
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Molar mass
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410.5
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Purity
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