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Ispronicline
Systematic (IUPAC) name
(2S,4E)-5-(5-isopropoxypyridin-3-yl)- N-methylpent-4-en-2-amine
Identifiers
CAS number 252870-53-4
ATC code none
PubChem 9824145
Chemical data
Formula C 14H22N2O 
Mol. mass 234.336
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

Ispronicline (TC-1734, AZD-3480) is a drug which acts as a partial agonist at neural nicotinic acetylcholine receptors. It is subtype-selective, binding primarily to the α4β2 subtype. It has antidepressant, nootropic and neuroprotective effects, and is under development for the treatment of dementia and Alzheimer's disease. Clinical trials so far have shown ispronicline to be effective and well tolerated, with the main side effects being dizziness and headache.[1][2][3][4][5]

References

  1. ^ Gatto GJ, Bohme GA, Caldwell WS, Letchworth SR, Traina VM, Obinu MC, Laville M, Reibaud M, Pradier L, Dunbar G, Bencherif M. TC-1734: an orally active neuronal nicotinic acetylcholine receptor modulator with antidepressant, neuroprotective and long-lasting cognitive effects. CNS Drug Reviews. 2004 Summer;10(2):147-66. PMID 15179444
  2. ^ Dunbar G, Demazières A, Monreal A, Cisterni C, Metzger D, Kuchibhatla R, Luthringer R. Pharmacokinetics and safety profile of ispronicline (TC-1734), a new brain nicotinic receptor partial agonist, in young healthy male volunteers. Journal of Clinical Pharmacology. 2006 Jul;46(7):715-26. PMID 16809797
  3. ^ Lippiello P, Letchworth SR, Gatto GJ, Traina VM, Bencherif M. Ispronicline: a novel alpha4beta2 nicotinic acetylcholine receptor-selective agonist with cognition-enhancing and neuroprotective properties. Journal of Molecular Neuroscience. 2006;30(1-2):19-20. PMID 17192610
  4. ^ Dunbar G, Boeijinga PH, Demazières A, Cisterni C, Kuchibhatla R, Wesnes K, Luthringer R. Effects of TC-1734 (AZD3480), a selective neuronal nicotinic receptor agonist, on cognitive performance and the EEG of young healthy male volunteers. Psychopharmacology (Berlin). 2007 May;191(4):919-29. PMID 17225162
  5. ^ Dunbar GC, Inglis F, Kuchibhatla R, Sharma T, Tomlinson M, Wamsley J. Effect of ispronicline, a neuronal nicotinic acetylcholine receptor partial agonist, in subjects with age associated memory impairment (AAMI). Journal of Psychopharmacology. 2007 Mar;21(2):171-8. PMID 17329297
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