The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha 7 nicotinic receptor partial agonist

Authors
Macor, JE Gurley, D Lanthorn, T Loch, J Mack, RA Mullen, G Tran, O Wright, N Gordon, JC
Citation
Je. Macor et al., The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha 7 nicotinic receptor partial agonist, BIOORG MED, 11(3), 2001, pp. 319-321
Citations number
12
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
3
Year of publication
2001
Pages
319 - 321
Database
ISI
SICI code
0960-894X(20010212)11:3<319:T5AT(2>2.0.ZU;2-R
Abstract
The 5-HT3 receptor antagonist tropisetron (ICS 205-930) was found to be a p otent and selective partial agonist at alpha7 nicotinic receptors. Two othe r 5-HT3 receptor antagonists, ondansetron and LY-278,584. were found to lac k high affinity at the alpha7 nicotinic receptor. Quinuclidine analogues (1 and 2) of tropisetron were also found to be potent and selective partial a gonists at alpha7 nicotinic receptors. (C) 2001 Elsevier Science Ltd. All r ights reserved.