ABT-418
ABT-418 is a drug developed by Abbott, that has nootropic, neuroprotective and anxiolytic effects, and has been researched for treatment of both Alzheimer's disease and ADHD. It acts as an agonist at neural nicotinic acetylcholine receptors, subtype-selective binding with high affinity to the α4β2, α7/5-HT3, and α2β2 nicotinic acetylcholine receptors but not α3β4 receptors 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.
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| Formula | C9H14N2O |
| Molar mass | 166.224 g·mol−1 |
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ABT-418 is a drug developed by Abbott, that has nootropic, neuroprotective and anxiolytic effects,[1][2][3][4][5] and has been researched for treatment of both Alzheimer's disease[6] and ADHD.[7][8][9] It acts as an agonist at neural nicotinic acetylcholine receptors, subtype-selective binding with high affinity to the α4β2, α7/5-HT3, and α2β2 nicotinic acetylcholine receptors but not α3β4 receptors[10][11][12] 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.[13]
See also
[edit]References
[edit]- ^ Arneric SP, Sullivan JP, Briggs CA, Donnelly-Roberts D, Anderson DJ, Raszkiewicz JL, et al. (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". The Journal of Pharmacology and Experimental Therapeutics. 270 (1): 310–318. PMID 7518514. Archived from the original on 2005-05-07. Retrieved 2008-06-08.
- ^ Decker MW, Brioni JD, Sullivan JP, Buckley MJ, Radek RJ, Raszkiewicz JL, et al. (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". The Journal of Pharmacology and Experimental Therapeutics. 270 (1): 319–328. PMID 7913497. Archived from the original on 2005-05-07. Retrieved 2008-06-08.
- ^ 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". The Journal of Pharmacology and Experimental Therapeutics. 271 (1): 353–361. PMID 7965735. Archived from the original on 2009-09-05. Retrieved 2008-06-08.
- ^ Prendergast MA, Terry AV, Jackson WJ, Marsh KC, Decker MW, Arneric SP, Buccafusco JJ (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. 130 (3): 276–284. doi:10.1007/s002130050240. PMID 9151363. S2CID 34377165.
- ^ Dallanoce C, Magrone P, Matera C, Lo Presti L, De Amici M, Riganti L, et al. (December 2010). "Synthesis of novel chiral Δ2-isoxazoline derivatives related to ABT-418 and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes". European Journal of Medicinal Chemistry. 45 (12): 5594–5601. doi:10.1016/j.ejmech.2010.09.009. PMID 20932609.
- ^ 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. 142 (4): 334–342. doi:10.1007/s002130050897. PMID 10229057. S2CID 27337634.
- ^ Wilens TE, Biederman J, Spencer TJ, Bostic J, Prince J, Monuteaux MC, et al. (December 1999). "A pilot controlled clinical trial of ABT-418, a cholinergic agonist, in the treatment of adults with attention deficit hyperactivity disorder". The American Journal of Psychiatry. 156 (12): 1931–1937. doi:10.1176/ajp.156.12.1931. PMID 10588407. S2CID 20375475.
- ^ Horrigan JP (April 2001). "Present and future pharmacotherapeutic options for adult attention deficit/hyperactivity disorder". Expert Opinion on Pharmacotherapy. 2 (4): 573–586. doi:10.1517/14656566.2.4.573. PMID 11336608. S2CID 41914443.
- ^ Spencer T, Biederman J (2002). "Non-stimulant treatment for Attention-Deficit/Hyperactivity Disorder". Journal of Attention Disorders. 6 (Suppl 1): S109–S119. doi:10.1177/070674370200601s13. PMID 12685525. S2CID 26801069.
- ^ Papke RL, Thinschmidt JS, Moulton BA, Meyer EM, Poirier A (February 1997). "Activation and inhibition of rat neuronal nicotinic receptors by ABT-418". British Journal of Pharmacology. 120 (3): 429–438. doi:10.1038/sj.bjp.0700930. PMC 1564486. PMID 9031746.
- ^ Dallanoce C, Magrone P, Matera C, Lo Presti L, De Amici M, Riganti L, et al. (December 2010). "Synthesis of novel chiral Δ2-isoxazoline derivatives related to ABT-418 and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes". European Journal of Medicinal Chemistry. 45 (12): 5594–5601. doi:10.1016/j.ejmech.2010.09.009. PMID 20932609.
- ^ 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. S2CID 54338489.
- ^ Wilens TE, Decker MW (October 2007). "Neuronal nicotinic receptor agonists for the treatment of attention-deficit/hyperactivity disorder: focus on cognition". Biochemical Pharmacology. 74 (8): 1212–1223. doi:10.1016/j.bcp.2007.07.002. PMC 2974320. PMID 17689498.
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