ABT-418
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ABT-418
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| Systematic (IUPAC) name | |
| 3-methyl-5-[(2S)-1-methylpyrrolidin-2-yl]-1,2-oxazole | |
| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C9H14N2O |
| Mol. mass | 166.22 |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Legal status | |
| Routes | ? |
ABT-418 is a drug developed by Abbott, 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]
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[edit] References
- ^ 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:. PMID 9031746.
- ^ 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:. PMID 7566493.
- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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:. PMID 9151363.
- ^ 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:. PMID 10229057.
- ^ 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.
- ^ Horrigan JP (April 2001). "Present and future pharmacotherapeutic options for adult attention deficit/hyperactivity disorder". Expert Opin Pharmacother 2 (4): 573–86. doi:. PMID 11336608.
- ^ Spencer T, Biederman J (2002). "Non-stimulant treatment for Attention-Deficit/Hyperactivity Disorder". J Atten Disord 6 Suppl 1: S109–19. PMID 12685525.
- ^ 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:. PMID 17689498.
