High affinity ligands for the alpha7 nicotinic receptor that show no cross-reactivity with the 5-HT3 receptor |
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Authors: | Baker S Richard Boot John Brunavs Michael Dobson David Green Rachel Hayhurst Lorna Keenan Martine Wallace Louise |
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Affiliation: | Eli Lilly and Company Ltd., Lilly Research Centre, Erl Wood Manor, Windlesham, Surrey, GU20 6PH, UK. |
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Abstract: | Potent and selective ligands of the alpha7 nicotinic acetylcholine receptor are required to understand the pharmacological effect of alpha7 activation. A common cross-reactivity occurs with serotonergic 5-HT3 receptors with which alpha7 receptors have a high sequence homology. We demonstrate that certain quinuclidine 3-biaryl carboxamides are high affinity alpha7 ligands with an excellent binding selectivity over 5-HT3 receptors. |
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