High affinity ligands for the α7 nicotinic receptor that show no cross-reactivity with the 5-HT3 receptor

Potent and selective ligands of the α7 nicotinic acetylcholine receptor are required to understand the pharmacological effect of α7 activation. A common cross-reactivity occurs with serotonergic 5-HT3 receptors with which α7 receptors have a high sequence homology. We demonstrate that certain quinuclidine 3-biaryl carboxamides are high affinity α7 ligands with an excellent binding selectivity over 5-HT3 receptors.

Certain quinuclidine 3-biarylcarboxamides are high affinity nicotinic α7 ligands with an excellent binding selectivity over the 5-HT3 receptor.Figure optionsDownload as PowerPoint slide