| Abstract
| - A library of benzamides was tested for α7 nicotinicacetylcholine receptor (nAChR) agonist activity using a chimeric receptor in a functional, cell-based, high-throughputassay. From this library, quinuclidine benzamides were foundto have α7 nAChR agonist activity. The SAR diverged fromthe activity of this compound class verses the 5-HT3 receptor,a structural homologue of the α7 nAChR. PNU-282987, themost potent compound from this series, was also shown to opennative α7 nAChRs in cultured rat neurons and to reverse anamphetamine-induced gating deficit in rats.
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