PNU-282,987

Izvor: Wikipedia
PNU-282,987
(IUPAC) ime
N-[(3R)-1-azabiciklo[2.2.2]okt-3-il]-4-hlorobenzamid
Klinički podaci
Identifikatori
CAS broj 123464-89-1
ATC kod nije dodeljen
PubChem[1][2] 11243536
ChEMBL[3] CHEMBL177611 YesY
Hemijski podaci
Formula C14H17ClN2O 
Mol. masa 264,750
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

PNU-282,987 je lek koji deluje kao potentan i selektivan agonist za α7 podtip neuronskih nikotinskih acetilholinskih receptora.[4][5] U životinjskim studijama, on ispoljava nootropne efekte, te njegovi derivati mogu da budu korisni u tretmanu šizofrenije.[6][7] PNU-282,987 nije podesan za kliničku upotrebu zbog jake inhibicije hERG antimete.[8]

Reference[uredi - уреди]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. doi:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. doi:10.1093/nar/gkr777. PMID 21948594.  edit
  4. 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. 
  5. Bodnar, A.; Cortes-Burgos, L.; Cook, K.; Dinh, D.; Groppi, V.; Hajos, M.; Higdon, N.; Hoffmann, W. et al. (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. 
  6. 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. 
  7. 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
  8. 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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