The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective α7 nicotinic receptor partial agonist

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Abstract

The 5-HT3 receptor antagonist tropisetron (ICS 205-930) was found to be a potent and selective partial agonist at α7 nicotinic receptors. Two other 5-HT3 receptor antagonists, ondansetron and LY-278,584, were found to lack high affinity at the α7 nicotinic receptor. Quinuclidine analogues (1 and 2) of tropisetron were also found to be potent and selective partial agonists at α7 nicotinic receptors.

The 5-HT3 receptor antagonist tropisetron (ICS 205-930) was found to be a potent and selective partial agonist at α7 nicotinic receptors. Quinuclidine analogues (1 and 2) are also potent and selective partial agonists at α7 nAChRs.

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Acknowledgements

The mouse nAChR α7 clone was kindly provided by Dr. Avi Orr-Urtreger at the Tel-Aviv Sourasky Medical Center, Tel-Aviv, Israel.

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