PNU-282,987 explained

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-282987 has been shown to initiate signaling that leads to adult neurogeneis in mammals.[6]

Notes and References

  1. Hajós M, Hurst RS, Hoffmann WE, Krause M, Wall TM, Higdon NR, Groppi VE . The selective alpha7 nicotinic acetylcholine receptor agonist PNU-282987 [N-[(3R)-1-Azabicyclo[2.2.2]oct-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 . March 2005 . 15523001 . 10.1124/jpet.104.076968 . 36149268 .
  2. Bodnar AL, Cortes-Burgos LA, Cook KK, Dinh DM, Groppi VE, Hajos M, Higdon NR, Hoffmann WE, Hurst RS, Myers JK, Rogers BN, Wall TM, Wolfe ML, Wong E . 6 . Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors . Journal of Medicinal Chemistry . 48 . 4 . 905–908 . February 2005 . 15715459 . 10.1021/jm049363q .
  3. Hansen HH, Timmermann DB, Peters D, Walters C, Damaj MI, Mikkelsen JD . 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 . June 2007 . 17455307 . 10.1002/jnr.21293 . 37590479 .
  4. Redrobe JP, Nielsen EØ, Christensen JK, Peters D, Timmermann DB, Olsen GM . 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 . January 2009 . 18848931 . 10.1016/j.ejphar.2008.09.035 .
  5. Walker DP, Wishka DG, Piotrowski DW, Jia S, Reitz SC, Yates KM, Myers JK, Vetman TN, Margolis BJ, Jacobsen EJ, Acker BA, Groppi VE, Wolfe ML, Thornburgh BA, Tinholt PM, Cortes-Burgos LA, Walters RR, Hester MR, Seest EP, Dolak LA, Han F, Olson BA, Fitzgerald L, Staton BA, Raub TJ, Hajos M, Hoffmann WE, Li KS, Higdon NR, Wall TM, Hurst RS, Wong EH, Rogers BN . 6 . Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as alpha7 nicotinic acetylcholine receptor agonists . Bioorganic & Medicinal Chemistry . 14 . 24 . 8219–8248 . December 2006 . 17011782 . 10.1016/j.bmc.2006.09.019 .
  6. Webster MK, Cooley-Themm CA, Barnett JD, Bach HB, Vainner JM, Webster SE, Linn CL . Evidence of BrdU-positive retinal neurons after application of an Alpha7 nicotinic acetylcholine receptor agonist . Neuroscience . 346 . 437–446 . March 2017 . 28147247 . 5341387 . 10.1016/j.neuroscience.2017.01.029 .

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