PNU-282,987

PNU-282,987 is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors.[1][2] In animal studies, it shows nootropic effects, and derivatives may be useful in the treatment of schizophrenia,[3][4] although PNU-282,987 is not suitable for use in humans because of excessive inhibition of the hERG antitarget.[5]
PNU-282,987
PNU-282,987
PNU-282,987.svg
Identifiers
CAS Number 123464-89-1
PubChem (CID) 9795278
ChemSpider 7971045
ChEMBL CHEMBL177611 YesY
Chemical and physical data
Formula C14H17ClN2O
Molar mass 264.750
3D model (Jmol) Interactive image
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PNU-282,987 is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors.[1][2] In animal studies, it shows nootropic effects, and derivatives may be useful in the treatment of schizophrenia,[3][4] although PNU-282,987 is not suitable for use in humans because of excessive inhibition of the hERG antitarget.[5]

References

  1. ^ Hajós, M.; Hurst, R.; Hoffmann, W.; Krause, M.; Wall, T.; Higdon, N.; Groppi, V. (2005). "The selective alpha7 nicotinic acetylcholine receptor agonist PNU-282987 N-(3R)-1-Azabicyclo2.2.2oct-3-yl-4-chlorobenzamide hydrochloride enhances GABAergic synaptic activity in brain slices and restores auditory gating deficits in anesthetized rats". The Journal of Pharmacology and Experimental Therapeutics. 312 (3): 1213–1222. doi:10.1124/jpet.104.076968. PMID 15523001. 
  2. ^ Bodnar, A.; Cortes-Burgos, L.; Cook, K.; Dinh, D.; Groppi, V.; Hajos, M.; Higdon, N.; Hoffmann, W.; Hurst, R.; Myers, J. K.; Rogers, B. N.; Wall, T. M.; Wolfe, M. L.; Wong, E. (2005). "Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors". Journal of Medicinal Chemistry. 48 (4): 905–908. doi:10.1021/jm049363q. PMID 15715459. 
  3. ^ Hansen, H.; Timmermann, D.; Peters, D.; Walters, C.; Damaj, M.; Mikkelsen, J. (2007). "Alpha-7 nicotinic acetylcholine receptor agonists selectively activate limbic regions of the rat forebrain: an effect similar to antipsychotics". Journal of neuroscience research. 85 (8): 1810–1818. doi:10.1002/jnr.21293. PMID 17455307. 
  4. ^ Redrobe, J (2009). "Alpha7 nicotinic acetylcholine receptor activation ameliorates scopolamine-induced behavioural changes in a modified continuous Y-maze task in mice". European Journal of Pharmacology. 602 (1): 58–65. doi:10.1016/j.ejphar.2008.09.035. PMID 18848931. 
  5. ^ Walker DP, Wishka DG, Piotrowski DW, et al. (2006). "Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as alpha7 nicotinic acetylcholine receptor agonists". Bioorg. Med. Chem. 14 (24): 8219–48. doi:10.1016/j.bmc.2006.09.019. PMID 17011782. 


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