PNU-282,987

Из Википедије, слободне енциклопедије
PNU-282,987
PNU-282,987.svg
IUPAC ime
N-[(3R)-1-azabiciklo[2.2.2]okt-3-il]-4-hlorobenzamid
Identifikatori
CAS broj 123464-89-1 ДаY
ATC kod None
PubChem CID 11243536
ChEMBL CHEMBL177611 ДаY
Hemijski podaci
Formula C14H17ClN2O
Molarna masa 264,750
  (verify)

PNU-282,987 je lek koji deluje kao potentan i selektivan agonist za α7 podtip neuronskih nikotinskih acetilholinskih receptora.[1][2] U životinjskim studijama, on ispoljava nootropne efekte, te njegovi derivati mogu da budu korisni u tretmanu šizofrenije.[3][4] PNU-282,987 nije podesan za kliničku upotrebu zbog jake inhibicije hERG antimete.[5]

Reference[уреди]

  1. 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. 
  2. Bodnar, A.; Cortes-Burgos, L.; Cook, K.; Dinh, D.; Groppi, V.; Hajos, M.; Higdon, N.; Hoffmann, W.; Hurst, R. (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, 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. 
  4. 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
  5. 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. 

Spoljašnje veze[уреди]