PHA 568487 is an agonist of AChR α7 (Ki values are 44 and 2800 for α7 and 5-HT3, respectively, IC50 values are > 100 µM for α3β4 and α1β1δγ, respectively, and % inhibition is < 1 and 5 % for α4β2 and hERG, respectively). It is orally active and a brain penetrant.
Walker et al (2006) Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as a7 nicotinic acetylcholine receptor agonists. Bioorg.Med.Chem. 14 8219.
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