PNU-282,987

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	11243536
ChEMBL	CHEMBL177611
Hemijski podaci
Formula	C14H17ClN2O
Mol. masa	264,750
SMILES	eMolekuli & PubHem
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) ; Key: WECKJONDRAUFDD-UHFFFAOYSA-N
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

↑ 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
↑ 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.
↑ 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
↑ 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.
↑ Bodnar, A.; Cortes-Burgos, L.; Cook, K.; Dinh, D.; Groppi, V.; Hajos, M.; Higdon, N.; Hoffmann, W. i dr.. (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, 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.
↑ 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
↑ 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 uredi

	Portal Medicina
	Portal Hemija

[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. i dr.. (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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