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CX614
Systematic (IUPAC) name
2H,3H,6aH-pyrrolidino(2,1-3',2')1,3-oxazino(6',5'-5,4)benzo(e)1,4-dioxan-10-one
Identifiers
CAS number 191744-13-5
ATC code  ?
PubChem 6451148
Chemical data
Formula C13H13NO4 
Mol. mass 247.24662 g/mol
SMILES eMolecules & PubChem
Synonyms CX-614
Therapeutic considerations
Pregnancy cat.  ?
Legal status Investigational New Medicine

CX-614 is an ampakine drug developed by Cortex Pharmaceuticals. It has been investigated for its effect on AMPA receptors.[1]

CX-614 produces rapid increases in release of the neurotrophic factor BDNF[2] and may have applications in the treatment of neurodegenerative diseases such as Alzheimer's disease. It has also been proposed as a treatment for conditions such as depression and schizophrenia,[3][4] but produces receptor downregulation following chronic administration, which might limit the potential for extended use.[5][6] CX-614 has also been shown to reduce the behavioural effects of methamphetamine in mice, and may have application in the treatment of stimulant abuse.[7]

References

  1. ^ Arai AC, Kessler M, Rogers G, Lynch G (2000). "Effects of the potent ampakine CX614 on hippocampal and recombinant AMPA receptors: interactions with cyclothiazide and GYKI 52466". Mol. Pharmacol. 58 (4): 802–13. PMID 10999951. 
  2. ^ Lauterborn JC, Truong GS, Baudry M, Bi X, Lynch G, Gall CM (Oct 2003). "Chronic elevation of brain-derived neurotrophic factor by ampakines". J Pharmacol Exp Ther. 307 (1): 297–305. doi:10.1124/jpet.103.053694. PMID 12893840. 
  3. ^ Jin R, Clark S, Weeks AM, Dudman JT, Gouaux E, Partin KM (Sep 2005). "Mechanism of positive allosteric modulators acting on AMPA receptors". J Neurosci. 25 (39): 9027–36. doi:10.1523/JNEUROSCI.2567-05.2005. PMID 16192394. 
  4. ^ Lynch G (Feb 2006). "Glutamate-based therapeutic approaches: ampakines". Curr Opin Pharmacol 6 (1): 82–8. doi:10.1016/j.coph.2005.09.005. PMID 16361116. 
  5. ^ Jourdi H, Lu X, Yanagihara T, et al. (Jul 2005). "Prolonged positive modulation of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors induces calpain-mediated PSD-95/Dlg/ZO-1 protein degradation and AMPA receptor down-regulation in cultured hippocampal slices". J Pharmacol Exp Ther. 314 (1): 16–26. doi:10.1124/jpet.105.083873. PMID 15784649. 
  6. ^ Mitchell NA, Fleck MW (Apr 2007). "Targeting AMPA receptor gating processes with allosteric modulators and mutations". Biophys J. 92 (7): 2392–402. doi:10.1529/biophysj.106.095091. PMID 17208968. 
  7. ^ Hess US, Whalen SP, Sandoval LM, Lynch G, Gall CM (2003). "Ampakines reduce methamphetamine-driven rotation and activate neocortex in a regionally selective fashion". Neuroscience 121 (2): 509–21. doi:10.1016/S0306-4522(03)00423-8. PMID 14522010. http://linkinghub.elsevier.com/retrieve/pii/S0306452203004238. 
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