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ABT-418

August 25, 2023

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]

ABT-418
Identifiers
  • 3-Methyl-5-[(2S)-1-methylpyrrolidin-2-yl]-1,2-oxazole
CAS Number
  • 147402-53-7 N
PubChem CID
  • 119380
ChemSpider
  • 106627 Y
UNII
  • B9I6MZL7BW
ChEMBL
  • ChEMBL274525 Y
CompTox Dashboard (EPA)
  • DTXSID10163711
Chemical and physical data
FormulaC9H14N2O
Molar mass166.22 g·mol−1
3D model (JSmol)
  • Interactive image
  • CC1=NOC(=C1)[C@@H]2CCCN2C
  • InChI=1S/C9H14N2O/c1-7-6-9(12-10-7)8-4-3-5-11(8)2/h6,8H,3-5H2,1-2H3/t8-/m0/s1 Y
  • Key:ILLGYRJAYAAAEW-QMMMGPOBSA-N Y
 NY (what is this?)  (verify)

See also Edit

References Edit

  1. ^ 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.
  2. ^ 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.
  3. ^ 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.
  4. ^ 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.
  5. ^ 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.
  6. ^ 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.
  7. ^ 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.
  8. ^ 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.
  9. ^ 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.
  10. ^ 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.
  11. ^ 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.
  12. ^ 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.
  13. ^ 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.
 

This article about an anxiolytic is a stub. You can help Wikipedia by expanding it.

August 25, 2023
drug, developed, abbott, that, nootropic, neuroprotective, anxiolytic, effects, been, researched, treatment, both, alzheimer, disease, adhd, acts, agonist, neural, nicotinic, acetylcholine, receptors, subtype, selective, binding, with, high, affinity, α4β2, α2. 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 a4b2 a7 5 HT3 and a2b2 nicotinic acetylcholine receptors but not a3b4 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 ABT 418IdentifiersIUPAC name 3 Methyl 5 2S 1 methylpyrrolidin 2 yl 1 2 oxazoleCAS Number147402 53 7 NPubChem CID119380ChemSpider106627 YUNIIB9I6MZL7BWChEMBLChEMBL274525 YCompTox Dashboard EPA DTXSID10163711Chemical and physical dataFormulaC 9H 14N 2OMolar mass166 22 g mol 13D model JSmol Interactive imageSMILES CC1 NOC C1 C H 2CCCN2CInChI InChI 1S C9H14N2O c1 7 6 9 12 10 7 8 4 3 5 11 8 2 h6 8H 3 5H2 1 2H3 t8 m0 s1 YKey ILLGYRJAYAAAEW QMMMGPOBSA N Y N Y what is this verify See also EditEpiboxidine AnabaseineReferences 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 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 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 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 D2 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 D2 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 This article about an anxiolytic is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title ABT 418 amp oldid 1158937743, wikipedia, wiki, book, books, library,

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