4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 3, Pages 319-321

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0960-894X(00)00670-3

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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. (C) 2001 Elsevier Science Ltd. All rights reserved.

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