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Acta pharmacologica Sinica

Effect of forskolin on acetylcholine-induced current in rat pheochromocytoma cells.


PMID 11324432

Abstract

To study the effect of forskolin on the nicotinic receptor (NicR) of PC12 cells. The acetylcholine (ACh)-induced current (IACh) was measured on PC12 cells by whole-cell clamp technique. The IACh could be blocked by d-tubocurarine chloride and atropine had no effect on IACh. Infusion of forskolin (1-50 mumol.L-1) caused an inhibition on IACh, which was reversible, concentration-dependent, and voltage-independent. Preincubation with 8-bromo-adenosine-3', 5'-adenosine monophosphate (8-Br-cAMP), a cell-permeable cAMP analog which preferentially activated cyclic AMP-dependent protein kinase (CADPK), for 20 min, did not affect the IACh and the inhibitory effect of forskolin. Infusion of 1,9-dideoxyforskolin, an analog of forskolin which did not activate adenyl cyclase, also caused an inhibition on IACh. The inhibitory effect of forskolin on IACh in PC12 cells is not mediated by activating the adenyl cyclase. Probably, the lipophilic forskolin acts via perturbing the plasma membrane lipid structure and altering the function of the NicR.

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D3658
1,9-Dideoxyforskolin from Coleus forskohlii, ≥97%, solid
C22H34O5