CX614
Encyclopedia
CX-614 is an ampakine
drug developed by Cortex Pharmaceuticals. It has been investigated for its effect on AMPA receptor
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 (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
.
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.
Ampakine
Ampakines are a class of compounds known to enhance attention span and alertness, and facilitate learning and memory. The ampakines take their name from the glutamatergic AMPA receptor with which they strongly interact...
drug developed by Cortex Pharmaceuticals. It has been investigated for its effect on AMPA receptor
AMPA receptor
The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor is a non-NMDA-type ionotropic transmembrane receptor for glutamate that mediates fast synaptic transmission in the central nervous system . Its name is derived from its ability to be activated by the artificial glutamate analog AMPA...
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
Synaptic plasticity
In neuroscience, synaptic plasticity is the ability of the connection, or synapse, between two neurons to change in strength in response to either use or disuse of transmission over synaptic pathways. Plastic change also results from the alteration of the number of receptors located on a synapse...
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 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
Synaptic plasticity
In neuroscience, synaptic plasticity is the ability of the connection, or synapse, between two neurons to change in strength in response to either use or disuse of transmission over synaptic pathways. Plastic change also results from the alteration of the number of receptors located on a synapse...
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
MPTP
MPTP is a neurotoxin precursor to MPP+, which causes permanent symptoms of Parkinson's disease by destroying dopaminergic neurons in the substantia nigra of the brain...
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
Parkinson's disease
Parkinson's disease is a degenerative disorder of the central nervous system...
and Alzheimer's Disease
Alzheimer's disease
Alzheimer's disease also known in medical literature as Alzheimer disease is the most common form of dementia. There is no cure for the disease, which worsens as it progresses, and eventually leads to death...
.
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.