CX-614 is an

ampakine Ampakines, also stylized as AMPAkines, are a subgroup of AMPA receptor positive allosteric modulators with a benzamide or closely related chemical structure. They are also known as "CX compounds". Ampakines take their name from the AMPA recepto ...

drug developed by Cortex Pharmaceuticals. It has been investigated for its effect on

AMPA receptor The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, AMPAR, or quisqualate receptor) is an ionotropic receptor, ionotropic transmembrane receptor for glutamate (iGluR) that mediates fast synapse, synap ...

s. 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 and may have applications in the treatment of neurodegenerative diseases such as Alzheimer's disease. Acute CX-614 treatments activate

local mRNA translation In molecular biology and genetics, translation is the process in which ribosomes in the cytoplasm or endoplasmic reticulum synthesize proteins after the process of transcription of DNA to RNA in the cell's nucleus. The entire process is ...

(new protein synthesis) within dendrites 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. CX-614 has also been proposed as a treatment for conditions such as depression and schizophrenia, but produces receptor downregulation following chronic administration, which might limit the potential for extended use. 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. Importantly, such short and intermittent treatment protocols are neuroprotective against neurotoxicity induced with MPTP and MPP⁺ in cultured midbrain (mesencephalic) and hippocampal organotypic slices. 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 Alzheimer's disease (AD) is a neurodegeneration, neurodegenerative disease that usually starts slowly and progressively worsens. It is the cause of 60–70% of cases of dementia. The most common early symptom is difficulty in short-term me ...

. 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.

References

{{Ionotropic glutamate receptor modulators Pyrrolidines Ampakines Lactams Benzodioxoles AMPA receptor positive allosteric modulators Experimental drugs

See also

References