Ispronicline

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Ispronicline
Ispronicline.png
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC14H22N2O
Molar mass234.336 g·mol−1
3D model (JSmol)
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Ispronicline (TC-1734, AZD-3480) is an experimental drug which acts as a partial agonist at neural nicotinic acetylcholine receptors. It progressed to phase II clinical trials for the treatment of dementia and Alzheimer's disease, but is no longer under development.[1]

Ispronicline is subtype-selective, binding primarily to the α4β2 subtype. It has antidepressant, nootropic and neuroprotective effects.[medical citation needed]

Early stage clinical trials showed that ispronicline was well tolerated, with the main side effects being dizziness and headache.[2][3][4][5][6] However, mid stage clinical trials failed to show sufficient efficacy to continue development as a pharmaceutical drug.[1]

References[edit]

  1. ^ a b Targacept Drops Development of Alzheimer's Drug
  2. ^ Gatto GJ, Bohme GA, Caldwell WS, Letchworth SR, Traina VM, Obinu MC, et al. "TC-1734: an orally active neuronal nicotinic acetylcholine receptor modulator with antidepressant, neuroprotective and long-lasting cognitive effects". CNS Drug Reviews. 10 (2): 147–66. PMID 15179444.
  3. ^ Dunbar G, Demazières A, Monreal A, Cisterni C, Metzger D, Kuchibhatla R, Luthringer R (July 2006). "Pharmacokinetics and safety profile of ispronicline (TC-1734), a new brain nicotinic receptor partial agonist, in young healthy male volunteers". Journal of Clinical Pharmacology. 46 (7): 715–26. doi:10.1177/0091270006288730. PMID 16809797.
  4. ^ 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. 30 (1–2): 19–20. doi:10.1385/JMN:30:1:19. PMID 17192610.
  5. ^ Dunbar G, Boeijinga PH, Demazières A, Cisterni C, Kuchibhatla R, Wesnes K, Luthringer R (May 2007). "Effects of TC-1734 (AZD3480), a selective neuronal nicotinic receptor agonist, on cognitive performance and the EEG of young healthy male volunteers". Psychopharmacology. 191 (4): 919–29. doi:10.1007/s00213-006-0675-x. PMID 17225162.
  6. ^ Dunbar GC, Inglis F, Kuchibhatla R, Sharma T, Tomlinson M, Wamsley J (March 2007). "Effect of ispronicline, a neuronal nicotinic acetylcholine receptor partial agonist, in subjects with age associated memory impairment (AAMI)". Journal of Psychopharmacology. 21 (2): 171–8. doi:10.1177/0269881107066855. PMID 17329297.