The 5-HT 3 antagonist tropisetron (ICS 205-930) is a potent and selective α7 nicotinic receptor partial agonist

Bioorganic & Medicinal Chemistry Letters
2001.0

Abstract

The 5-HT3 receptor antagonist tropisetron (ICS 205-930) was found to be a potent and selective partial agonist at alpha7 nicotinic receptors. Two other 5-HT3 receptor antagonists, ondansetron and LY-278,584, were found to lack high affinity at the alpha7 nicotinic receptor. Quinuclidine analogues (1 and 2) of tropisetron were also found to be potent and selective partial agonists at alpha7 nicotinic receptors.

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