The effects of hexasulfobutylated (FC4S), the fullerene derivative on the contraction of smooth muscle were tested pharmacologically on the circular muscle of stomach of guinea pigs. The effects of monomalonic acid C60 (MMA C60) on the same preparations were compared. The effects of those compounds on the taenia coli, portal vein and vas deferens of guinea pigs were also tested. The FC4S did, while MMA C60 did not elicit contracture of the circular muscle of stomach and taenia coli. Both FC4S and MMA C60 did not elicit contraction on the portal vein and on the vas deferens of the guinea pig. Prazosin (0.5 μM) or propranolol (0.5 μM) did not alter the FC4S elicit contracture of the circular muscle of stomach. However, atropine (0.01, 0.1 and 1 μM), tetrodotoxin (0.1 μM) or low calcium medium decreased reversibly the FC4S elicited contracture of the circular muscle of stomach. The effect of FC4S on the contracture of the gastric muscles was also tested using various muscarinic receptor subtype antagonists. 4-DAMP (1 μM), muscarinic M3 receptor antagonist, and tropicamide (1 μM), muscarinic M4 receptor antagonist, did not alter the contracture elicited by FC4S. Pirenzepine (0.1 μM), muscarinic M1 receptor antagonist, and methoctramine (0.25 μM), muscarinic M2 receptor antagonist, significantly decreased the FC4S elicited contracture of the circular muscle. Atropine (1 μM) or tetrodotoxin (0.1 μM) completely blocked the FC4S elicited contracture of the circular muscle of stomach. It is concluded that FC4S elicited contracture of the circular muscle of stomach. The effect may be due to FC4S acts on the cholinergic cells existed in the gastric muscle and indirectly activating the tetrodotoxin dependent releasing of the transmitters from the cells, then, activating the muscarinice M1, M2 receptors in the muscle eliciting the contractures.
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