The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.

Article Details

Citation

Macor JE, Gurley D, Lanthorn T, Loch J, Mack RA, Mullen G, Tran O, Wright N, Gordon JC

The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.

Bioorg Med Chem Lett. 2001 Feb 12;11(3):319-21.

PubMed ID
11212100 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
NicotineNeuronal acetylcholine receptor subunit alpha-3Ki (nM)220N/AN/ADetails
NicotineNeuronal acetylcholine receptor subunit beta-2Ki (nM)2.3N/AN/ADetails
Ondansetron5-hydroxytryptamine receptor 3AKi (nM)12N/AN/ADetails