CX614

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CX614
CX614.png
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
Clinical data
Legal status
  • Investigational New Medicine
Identifiers
CAS Number 191744-13-5 YesY
PubChem CID: 6451148
IUPHAR/BPS 7842
UNII 87V631480W YesY
Synonyms CX-614
Chemical data
Formula C13H13NO4
Molecular mass 247.24662 g/mol
  • C1CC2N(C1)C(=O)C3=CC4=C(C=C3O2)OCCO4
  (verify)

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

Chronic CX-614 treatments produce rapid increases in the synthesis of the brain-derived neurotrophic factor BDNF which has very important effects on synaptic plasticity [2] and may have applications in the treatment of neurodegenerative diseases such as Alzheimer's disease.

Acute CX-614 treatments activate local mRNA translation (new protein synthesis) within dendrites [3] and this is mediated by a fast upregulation of BDNF release. CX-614-dependent release of BDNF rapidly increases translation of proteins that are important for synaptic plasticity such as ARC/Arg3.1 and CaMKIIalpha.[3]

CX-614 has also been proposed as a treatment for conditions such as depression and schizophrenia,[4][5] but produces receptor downregulation following chronic administration, which might limit the potential for extended use.[6][7]

However, downregulation of AMPA receptors with prolonged CX-614 administration can be avoided by designing and using short and intermittent treatment protocols, which could still upregulate BDNF protein levels without reducing the levels of AMPA receptors.[8]

Importantly, such short and intermittent treatment protocols are neuroprotective against neurotoxicity induced with MPTP and MPP+ in cultured midbrain (mesencephalic) and hippocampal organotypic slices.[9]

These results uncovered the neuroprotective effects of CX-614 and indicated that opened the way for further experimentation with CX-614 as an important new treatment for Parkinson's Disease and Alzheimer's Disease.

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.[10]

References

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