drugbox
IUPAC_name = 2H,3H,6aH-pyrrolidino(2",1"-3',2')1,3-oxazino(6',5'-5,4)benzo(e)1,4-dioxan-10-one
width = 180
CAS_number = 191744-13-5
synonyms = CX-614
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PubChem = 6451148
DrugBank =
C = 13 | H = 13 | N = 1 | O = 4
molecular_weight = 247.24662 g/mol
smiles = C1CC2N(C1)C(=O)C3=CC4=C(C=C3O2)OCCO4
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legal_status = Investigational New Medicine
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CX-614 is an ampakine drug developed by Cortex Pharmaceuticals. It has been investigated for its effect on AMPA receptors.[cite journal |author=Arai AC, Kessler M, Rogers G, Lynch G |title=Effects of the potent ampakine CX614 on hippocampal and recombinant AMPA receptors: interactions with cyclothiazide and GYKI 52466 |journal=Mol. Pharmacol. |volume=58 |issue=4 |pages=802–13 |year=2000 |pmid=10999951 |doi=] ]CX-614 produces rapid increases in release of the neurotrophic factor BDNF [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. [http://www.ncbi.nlm.nih.gov/pubmed/12893840 PMID 12893840] ] 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, [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. [http://www.ncbi.nlm.nih.gov/pubmed/16192394 PMID 16192394] ] [Lynch G. Glutamate-based therapeutic approaches: ampakines. "Current Opinion in Pharmacology". 2006 Feb;6(1):82-8. [http://www.ncbi.nlm.nih.gov/pubmed/16361116 PMID 16361116] ] but produces receptor downregulation following chronic administration, which might limit the potential for extended use. [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. [http://www.ncbi.nlm.nih.gov/pubmed/15784649 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. [http://www.ncbi.nlm.nih.gov/pubmed/17208968 PMID 17208968] ] 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. [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. [http://www.ncbi.nlm.nih.gov/pubmed/14522010 PMID 14522010] ]
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