PNU-282,987
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Chemical compound
Pharmaceutical compound
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| Formula | C14H17ClN2O |
| Molar mass | 264.75 g·mol−1 |
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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] PNU-282987 has been shown to initiate signaling that leads to adult neurogeneis in mammals.[6]
References
[edit ]- ^ Hajós M, Hurst RS, Hoffmann WE, Krause M, Wall TM, Higdon NR, Groppi VE (March 2005). "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. doi:10.1124/jpet.104.076968. PMID 15523001. S2CID 36149268.
- ^ Bodnar AL, Cortes-Burgos LA, Cook KK, Dinh DM, Groppi VE, Hajos M, et al. (February 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.
- ^ Hansen HH, Timmermann DB, Peters D, Walters C, Damaj MI, Mikkelsen JD (June 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. S2CID 37590479.
- ^ Redrobe JP, Nielsen EØ, Christensen JK, Peters D, Timmermann DB, Olsen GM (January 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年09月03日5. PMID 18848931.
- ^ Walker DP, Wishka DG, Piotrowski DW, Jia S, Reitz SC, Yates KM, et al. (December 2006). "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. doi:10.1016/j.bmc.2006年09月01日9. PMID 17011782.
- ^ Webster MK, Cooley-Themm CA, Barnett JD, Bach HB, Vainner JM, Webster SE, Linn CL (March 2017). "Evidence of BrdU-positive retinal neurons after application of an Alpha7 nicotinic acetylcholine receptor agonist". Neuroscience. 346: 437–446. doi:10.1016/j.neuroscience.2017年01月02日9. PMC 5341387 . PMID 28147247.
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