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ABT-418
Systematic (IUPAC) name
3-methyl-5-[(2S)-1-methylpyrrolidin-2-yl]-1,2-oxazole
Identifiers
CAS number 147402-53-7
ATC code  ?
PubChem 119380
Chemical data
Formula C9H14N2O 
Mol. mass 166.22
SMILES eMolecules & PubChem
Therapeutic considerations
Pregnancy cat.  ?
Legal status

ABT-418 is a drug developed by Abbott, which acts as an agonist at neural nicotinic acetylcholine receptors. It binds with high affinity to the α4β2, α2β2 and α7 subtypes, but not to the α3β4 subtype.[1][2] It has nootropic, neuroprotective and anxiolytic effects,[3][4][5][6] and has been researched for treatment of both Alzheimer's disease[7] and more recently ADHD.[8][9][10] ABT-418 was reasonably effective for both applications and fairly well tolerated, but produced some side effects, principally nausea, and it is unclear whether ABT-418 itself will proceed to clinical development or if another similar drug will be used instead.[11]

References

  1. ^ 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): 429–38. doi:10.1038/sj.bjp.0700930. PMID 9031746. 
  2. ^ Briggs CA, McKenna DG, Piattoni-Kaplan M (June 1995). "Human alpha 7 nicotinic acetylcholine receptor responses to novel ligands". Neuropharmacology 34 (6): 583–90. doi:10.1016/0028-3908(95)00028-5. PMID 7566493. 
  3. ^ 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. http://jpet.aspetjournals.org/cgi/content/abstract/270/1/310. 
  4. ^ 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. http://jpet.aspetjournals.org/cgi/content/abstract/270/1/319. 
  5. ^ 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. http://jpet.aspetjournals.org/cgi/reprint/271/1/353. 
  6. ^ 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): 276–84. doi:10.1007/s002130050240. PMID 9151363. 
  7. ^ 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): 334–42. doi:10.1007/s002130050897. PMID 10229057. 
  8. ^ 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. http://ajp.psychiatryonline.org/cgi/content/abstract/156/12/1931. 
  9. ^ Horrigan JP (April 2001). "Present and future pharmacotherapeutic options for adult attention deficit/hyperactivity disorder". Expert Opin Pharmacother 2 (4): 573–86. doi:10.1517/14656566.2.4.573. PMID 11336608. 
  10. ^ Spencer T, Biederman J (2002). "Non-stimulant treatment for Attention-Deficit/Hyperactivity Disorder". J Atten Disord 6 Suppl 1: S109–19. PMID 12685525. 
  11. ^ Wilens TE, Decker MW (October 2007). "Neuronal nicotinic receptor agonists for the treatment of attention-deficit/hyperactivity disorder: focus on cognition". Biochem. Pharmacol. 74 (8): 1212–23. doi:10.1016/j.bcp.2007.07.002. PMID 17689498. 
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