ABT-418

Из Википедије, слободне енциклопедије
ABT-418
(IUPAC) ime
3-metil-5-[(2S)-1-metilpirolidin-2-il]-1,2-oksazol
Klinički podaci
Identifikatori
CAS broj 147402-53-7
ATC kod nije dodeljen
PubChem[1][2] 119380
ChemSpider[3] 106627
ChEMBL[4] CHEMBL274525 YesY
Hemijski podaci
Formula C9H14N2O 
Mol. masa 166.22
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

ABT-418 je lek koji je razvilo preduzeće Abbott. On deluje kao agonist na neuronskim nikotinskim acetilholinskim receptorima. Ovaj ligand se vezuje sa visokim afinitetom za α4β2, α2β2 i α7 receptore, a ne vezuje se za α3β4 receptor.[5][6] On ispoljava nootropne, neuroprotektivne i anksiolitičke efekte,[7][8][9][10] i ispitivan je za moguću primenu u lečenju Alchajmerove bolesti[11] i ADHD.[12][13][14]

Reference[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. ^ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining“. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. ^ 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
  5. ^ Papke RL, Thinschmidt JS, Moulton BA, Meyer EM, Poirier A (February 1997). „Activation and inhibition of rat neuronal nicotinic receptors by ABT-418“. Br. J. Pharmacol. 120 (3): 429–438. DOI:10.1038/sj.bjp.0700930. PMC 1564486. PMID 9031746. 
  6. ^ Briggs CA, McKenna DG, Piattoni-Kaplan M (June 1995). „Human alpha 7 nicotinic acetylcholine receptor responses to novel ligands“. Neuropharmacology 34 (6): 583–590. DOI:10.1016/0028-3908(95)00028-5. PMID 7566493. 
  7. ^ Arneric SP, Sullivan JP, Briggs CA, Donnelly-Roberts D, Anderson DJ, Raszkiewicz JL, Hughes ML, Cadman ED, Adams P, Garvey DS' (July 1994). „(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization“. J. Pharmacol. Exp. Ther. 270 (1): 310–8. PMID 7518514. 
  8. ^ Decker MW, Brioni JD, Sullivan JP, Buckley MJ, Radek RJ, Raszkiewicz JL, Kang CH, Kim DJ, Giardina WJ, Wasicak JT (July 1994). „(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: II. In vivo characterization“. J. Pharmacol. Exp. Ther. 270 (1): 319–28. PMID 7913497. 
  9. ^ Brioni JD, O'Neill AB, Kim DJ, Buckley MJ, Decker MW, Arneric SP (October 1994). „Anxiolytic-like effects of the novel cholinergic channel activator ABT-418“. J. Pharmacol. Exp. Ther. 271 (1): 353–61. PMID 7965735. 
  10. ^ Prendergast MA, Terry AV, Jackson WJ et al. (April 1997). „Improvement in accuracy of delayed recall in aged and non-aged, mature monkeys after intramuscular or transdermal administration of the CNS nicotinic receptor agonist ABT-418“. Psychopharmacology (Berl.) 130 (3): 276–284. DOI:10.1007/s002130050240. PMID 9151363. 
  11. ^ Potter A, Corwin J, Lang J, Piasecki M, Lenox R, Newhouse PA (March 1999). „Acute effects of the selective cholinergic channel activator (nicotinic agonist) ABT-418 in Alzheimer's disease“. Psychopharmacology (Berl.) 142 (4): 334–342. DOI:10.1007/s002130050897. PMID 10229057. 
  12. ^ Wilens TE, Biederman J, Spencer TJ, Bostic J, Prince J, Monuteaux MC, Soriano J, Fine C, Abrams A, Rater M, Polisner D (December 1999). „A pilot controlled clinical trial of ABT-418, a cholinergic agonist, in the treatment of adults with attention deficit hyperactivity disorder“. Am J Psychiatry 156 (12): 1931–7. PMID 10588407. 
  13. ^ Horrigan JP (April 2001). „Present and future pharmacotherapeutic options for adult attention deficit/hyperactivity disorder“. Expert Opin Pharmacother 2 (4): 573–586. DOI:10.1517/14656566.2.4.573. PMID 11336608. 
  14. ^ Spencer T, Biederman J (2002). „Non-stimulant treatment for Attention-Deficit/Hyperactivity Disorder“. J Atten Disord 6 Suppl 1: S109–19. PMID 12685525.