Chemistry:PNU-282,987
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Short description: Chemical compound
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| Formula | C14H17ClN2O |
| Molar mass | 264.750 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
- ↑ "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. doi:10.1124/jpet.104.076968. PMID 15523001.
- ↑ "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. doi:10.1021/jm049363q. PMID 15715459.
- ↑ "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. doi:10.1002/jnr.21293. PMID 17455307.
- ↑ "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. doi:10.1016/j.ejphar.2008.09.035. PMID 18848931.
- ↑ "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. doi:10.1016/j.bmc.2006.09.019. PMID 17011782.
- ↑ "Evidence of BrdU-positive retinal neurons after application of an Alpha7 nicotinic acetylcholine receptor agonist". Neuroscience 346: 437–446. March 2017. doi:10.1016/j.neuroscience.2017.01.029. PMID 28147247.
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