Forskolin (da Coleus forskohlii)
Forskolin is the major diterpene isolated from the Indian plant Coleus forskohlii. At low doses, forskolin is a positive inotropic agent in dogs, cats, spontaneously hypertensive and normal rats and in an isolated guinea pig heart (Langendorf) preparation. At higher doses, forskolin is a hypotensive and vasodilatory agent because of its function as a smooth muscle relaxant. No major side effects are observed at effective doses.
Forskolin's pharmacological activities are due to its activation of adenylate cyclase, resulting in increased intracellular cyclic AMP in most tissues and cells. The exact mechanism of forskolin's positive inotropic effect is unknown but may be related to a cyclic AMP-dependent increase in Na+ permeability that results in an indirect augmentation of calcium release. Forskolin, 7-o-Hemisuccinyl-7-deacetyl is a biologically active and useful derivative of forskolin. It has been attached to Sepharose as an affinity support for the purification of adenylate cyclase.
Forkolin is reported to demonstrate positive inotropic and heart rate-increasing activity at low doses in animals. Also functions as an antihypertensive and vasodilator at higher doses. Activates adenylcyclase in rat liver membranes.
Cell-permeable diterpenoid that possesses anti-hypertensive, positive inotropic, and adenylyl cyclase activating properties. Many of its biological effects are due to its activation of adenylyl cyclase and the resulting increase in intracellular cAMP concentration. Forskolin effects calcium currents and inhibits MAP kinase.
Soluble at 6 mg per ml in 95% ethanol and at 2,5 mg per 5 µl in anhydrous dimethylsulphoxide (DMSO).