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Acta Pharmacol Sin. 2000 Mar;21(3):281-5.

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

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Department of Physiology, Beijing Medical College of PLA, Beijing 100071, China.



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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