CX614
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CX614
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| 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 | |
| ATC code | ? |
| PubChem | |
| Chemical data | |
| Formula | C13H13NO4 |
| Mol. mass | 247.24662 g/mol |
| SMILES | & |
| Synonyms | CX-614 |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | ? |
| Half life | ? |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
? |
| Legal status |
Investigational New Medicine |
| Routes | ? |
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]
[edit] References
- ^ 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.
- ^ Lauterborn JC, Truong GS, Baudry M, Bi X, Lynch G, Gall CM. Chronic elevation of brain-derived neurotrophic factor by ampakines. Journal of Pharmacology and Experimental Therapeutics. 2003 Oct;307(1):297-305. PMID 12893840
- ^ Jin R, Clark S, Weeks AM, Dudman JT, Gouaux E, Partin KM. Mechanism of positive allosteric modulators acting on AMPA receptors. Journal of Neuroscience. 2005 Sep 28;25(39):9027-36. PMID 16192394
- ^ Lynch G. Glutamate-based therapeutic approaches: ampakines. Current Opinion in Pharmacology. 2006 Feb;6(1):82-8. PMID 16361116
- ^ Jourdi H, Lu X, Yanagihara T, Lauterborn JC, Bi X, Gall CM, Baudry M. 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. Journal of Pharmacology and Experimental Therapeutics. 2005 Jul;314(1):16-26. PMID 15784649
- ^ Mitchell NA, Fleck MW. Targeting AMPA receptor gating processes with allosteric modulators and mutations. Biophysical Journal. 2007 Apr 1;92(7):2392-402. PMID 17208968
- ^ Hess US, Whalen SP, Sandoval LM, Lynch G, Gall CM. Ampakines reduce methamphetamine-driven rotation and activate neocortex in a regionally selective fashion. Neuroscience. 2003;121(2):509-21. PMID 14522010
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