ABT-418

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ABT-418
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Identifiers
CAS Number
PubChem CID
E number{{#property:P628}}
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Chemical and physical data
FormulaC9H14N2O
Molar mass166.22
3D model (JSmol)

ABT-418 is a drug which acts as a partial 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. Activation and inhibition of rat neuronal nicotinic receptors by ABT-418. British Journal of Pharmacology. 1997 Feb;120(3):429-38. PMID 9031746
  2. Briggs CA, McKenna DG, Piattoni-Kaplan M. Human alpha 7 nicotinic acetylcholine receptor responses to novel ligands. Neuropharmacology. 1995 Jun;34(6):583-90. PMID 7566493
  3. Arneric SP, Sullivan JP, Briggs CA, Donnelly-Roberts D, Anderson DJ, Raszkiewicz JL, Hughes ML, Cadman ED, Adams P, Garvey DS, et al. (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. Journal of Pharmacology and Experimental Therapeutics. 1994 Jul;270(1):310-8. PMID 7518514
  4. Decker MW, Brioni JD, Sullivan JP, Buckley MJ, Radek RJ, Raszkiewicz JL, Kang CH, Kim DJ, Giardina WJ, Wasicak JT, et al. (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. Journal of Pharmacology and Experimental Therapeutics. 1994 Jul;270(1):319-28. PMID 7913497
  5. Brioni JD, O'Neill AB, Kim DJ, Buckley MJ, Decker MW, Arneric SP. Anxiolytic-like effects of the novel cholinergic channel activator ABT-418. Journal of Pharmacology and Experimental Therapeutics. 1994 Oct;271(1):353-61. PMID 7965735
  6. Prendergast MA, Terry AV Jr, Jackson WJ, Marsh KC, Decker MW, Arneric SP, Buccafusco JJ. 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 (Berlin). 1997 Apr;130(3):276-84. PMID 9151363
  7. Potter A, Corwin J, Lang J, Piasecki M, Lenox R, Newhouse PA. Acute effects of the selective cholinergic channel activator (nicotinic agonist) ABT-418 in Alzheimer's disease. Psychopharmacology (Berlin). 1999 Mar;142(4):334-42. 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. A pilot controlled clinical trial of ABT-418, a cholinergic agonist, in the treatment of adults with attention deficit hyperactivity disorder. American Journal of Psychiatry. 1999 Dec;156(12):1931-7. PMID 10588407
  9. Horrigan JP. Present and future pharmacotherapeutic options for adult attention deficit/hyperactivity disorder. Expert Opinion on Pharmacotherapy. 2001 Apr;2(4):573-86. PMID 11336608
  10. Spencer T, Biederman J. Non-stimulant treatment for Attention-Deficit/Hyperactivity Disorder. Journal of Attention Disorders. 2002;6 Suppl 1:S109-19. PMID 12685525
  11. Wilens TE, Decker MW. Neuronal nicotinic receptor agonists for the treatment of attention-deficit/hyperactivity disorder: focus on cognition. Biochemical Pharmacology. 2007 Oct 15;74(8):1212-23. PMID 17689498



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