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PNU-282,987

Identifiers
IUPAC name N-oct-3'-yl]-4-chlorobenzamide
CAS Number	123464-89-1
PubChem CID	9795278
ChemSpider	7971045
UNII	810P1694K2
ChEMBL	ChEMBL177611
CompTox Dashboard (EPA)	DTXSID801017103
Chemical and physical data
Formula	C14H17ClN2O
Molar mass	264.75 g·mol
3D model (JSmol)	Interactive image
SMILES C1CN2CCC1(C2)NC(=O)C3=CC=C(C=C3)Cl
InChI InChI=1S/C14H17ClN2O/c15-12-3-1-11(2-4-12)14(18)16-13-9-17-7-5-10(13)6-8-17/h1-4,10,13H,5-9H2,(H,16,18)/t13-/m0/s1 Key:WECKJONDRAUFDD-ZDUSSCGKSA-N
(verify)

PNU-282,987 is a drug that acts as a potent and selective agonist for the α7 subtype of neural nicotinic acetylcholine receptors. In animal studies, it shows nootropic effects, and derivatives may be useful in the treatment of schizophrenia, although PNU-282,987 is not suitable for use in humans because of excessive inhibition of the hERG antitarget. PNU-282987 has been shown to initiate signaling that leads to adult neurogeneis in mammals.

References

1. 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 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.
2. 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.
3. 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.
4. 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.2008.09.035. PMID 18848931.
5. 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.2006.09.019. PMID 17011782.
6. 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.2017.01.029. PMC 5341387. PMID 28147247.

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