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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 receptor (AMPAR), a type of ionotropic glutamate receptor with which the ampakines interact and act as positive allosteric modulators (PAMs) of. Although all ampakines are AMPAR PAMs, not all AMPAR PAMs are ampakines. They are currently being investigated as potential treatment for a range of conditions involving mental disability and disturbances such as Alzheimer's disease, Parkinson's disease, schizophrenia, treatment-resistant depression (TRD) or neurological disorders such as attention deficit hyperactivity disorder (ADHD), among others. More recently developed ampakine compounds are much more potent and selective for the AMPA receptor target, and while none of the newer selective ampakine compounds have yet come onto the market, various a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CX-1739
CX717 is an ampakine compound created by Christopher Marrs and Gary Rogers in 1996 at Cortex Pharmaceuticals. It affects the neurotransmitter glutamate, with trials showing the drug improves cognitive functioning and memory. Approval process In 2005 the U.S. Food and Drug Administration (FDA) accepted Cortex Pharmaceuticals' Investigational New Drug (IND) application to initiate pilot Phase II clinical trials in the United States. Also, in 2005, the United States Department of Defense funded a study to look into CX717 and the physiological effects of sleepiness. The study found that rhesus monkeys performed faster and better after receiving the drug, and it counteracted the effects of sleep deprivation. However, a 2006 study funded by DARPA found that CX717 did not improve cognitive performance in humans subjected to simulated night shift work. In early March 2006 Cortex reported that, in a small pilot Phase II study, CX717 had demonstrated positive clinical and statistical re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CX-717
CX717 is an ampakine compound created by Christopher Marrs and Gary Rogers in 1996 at Cortex Pharmaceuticals. It affects the neurotransmitter glutamate, with trials showing the drug improves cognitive functioning and memory. Approval process In 2005 the U.S. Food and Drug Administration (FDA) accepted Cortex Pharmaceuticals' Investigational New Drug (IND) application to initiate pilot Phase II clinical trials in the United States. Also, in 2005, the United States Department of Defense funded a study to look into CX717 and the physiological effects of sleepiness. The study found that rhesus monkeys performed faster and better after receiving the drug, and it counteracted the effects of sleep deprivation. However, a 2006 study funded by DARPA found that CX717 did not improve cognitive performance in humans subjected to simulated night shift work. In early March 2006 Cortex reported that, in a small pilot Phase II study, CX717 had demonstrated positive clinical and statistical re ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CX-614
CX-614 is an ampakine drug developed by Cortex Pharmaceuticals. It has been investigated for its effect on AMPA receptors. 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 a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
AMPA Receptor Positive Allosteric Modulator
AMPA receptor positive allosteric modulators are positive allosteric modulators (PAMs) of the receptor (AMPR), a type of ionotropic glutamate receptor which mediates most fast synaptic neurotransmission in the central nervous system. Medical applications AMPAR PAMs have cognition- and memory-enhancing and antidepressant-like effects in preclinical models, and have potential medical applications in the treatment of cognitive impairment (e.g., cognitive symptoms in schizophrenia, mild cognitive impairment), dementia (e.g., Alzheimer's disease), depression, and for other indications. They can broadly be divided into low-impact and high-impact potentiators, with high-impact potentiators able to produce comparatively more robust increases in AMPAR activation. However, high-impact AMPAR PAMs can cause motor coordination disruptions, convulsions, and neurotoxicity at sufficiently high doses, similarly to orthosteric AMPAR activators (i.e., active/glutamate site agonists). The A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CX-516
CX-516 is an ampakine and nootropic that acts as an AMPA receptor positive allosteric modulator and had been undergoing development by a collaboration between Cortex, Shire, and Servier. It was studied as a potential treatment for Alzheimer's disease under the brand name Ampalex, and was also being examined as a treatment for ADHD. CX-516 was the first ampakine compound developed by Cortex and while it showed good ''in vitro'' activity and positive results in animal tests, the human trials proved disappointing due mainly to low potency and short half-life. However, CX-516 is still widely used in animal research into the ampakine drugs and is the standard reference compound that newer, more potent drugs of this class such as farampator and CX-717 are compared to. See also * AMPA receptor positive allosteric modulator AMPA receptor positive allosteric modulators are positive allosteric modulators (PAMs) of the receptor (AMPR), a type of ionotropic glutamate receptor which m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ORG-26576
ORG-26576 is an ampakine originally developed by Cortex Pharmaceuticals and then licensed to Organon International for development. In animal studies it has been shown to effectively potentiate AMPA receptor function, leading to increased BDNF release and enhanced neuronal differentiation and survival, as well as producing nootropic effects in standardised assays. Development as an antidepressant has been halted due to a failed Phase II trial for major depressive disorder Major depressive disorder (MDD), also known as clinical depression, is a mental disorder characterized by at least two weeks of pervasive low mood, low self-esteem, and loss of interest or pleasure in normally enjoyable activities. Intro .... See also * AMPA receptor positive allosteric modulator References Ampakines AMPA receptor positive allosteric modulators Experimental drugs {{nervous-system-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CX-546
CX-546 is an ampakine drug developed by Cortex Pharmaceuticals. It has been proposed as a treatment for schizophrenia. CX-546 was the second drug of note to come out of the Cortex research program, after CX-516, but while it was an improvement over its predecessor in some respects, it still has problems with limited oral bioavailability. However, CX-546 still represented a significant advance that led on to the development of newer compounds such as CX-614 and CX-717 with superior properties over the earlier drugs. CX-546 itself has been investigated for other applications, and most notably has been found to show significant efficacy in reversing the respiratory depression produced by sedative drugs such as opioids and barbiturates. No effective respiratory stimulants are currently marketed for this application, with CX-546 being only the third drug discovered (after BIMU-8 and BW373U86) that effectively relieves the respiratory depression induced by fentanyl without reducing th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CX-691
Farampator (developmental code names CX-691, ORG-24448, SCH-900460) is an ampakine drug. It was developed by Cortex Pharmaceuticals, and licensed to Organon BioSciences for commercial development. Following the purchase of Organon by Schering-Plough in 2007, the development license to farampator was transferred. The development of farampator was eventually terminated, reportedly due to concerns about cardiac toxicity. Farampator has been investigated for its effect on AMPA receptors and researched for potential use in the treatment of schizophrenia and Alzheimer's disease. It was found to improve short-term memory, but impaired episodic memory. It produced side effects such as headache, somnolence and nausea. Subjects reporting side effects had significantly higher plasma levels of farampator than subjects without. Additional analyses revealed that in the farampator condition the group without side effects showed a significantly superior memory performance relative to the group w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Farampator
Farampator (developmental code names CX-691, ORG-24448, SCH-900460) is an ampakine drug. It was developed by Cortex Pharmaceuticals, and licensed to Organon BioSciences for commercial development. Following the purchase of Organon by Schering-Plough in 2007, the development license to farampator was transferred. The development of farampator was eventually terminated, reportedly due to concerns about cardiac toxicity. Farampator has been investigated for its effect on AMPA receptors and researched for potential use in the treatment of schizophrenia 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 .... It was found to improve short-term memory, but impaired episodic memory. It produced side effects such as headache, somnolence and nausea. Subjects reporting s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ADHD
Attention deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder characterised by excessive amounts of inattention, hyperactivity, and impulsivity that are pervasive, impairing in multiple contexts, and otherwise age-inappropriate. ADHD symptoms arise from executive dysfunction, and emotional dysregulation is often considered a core symptom. In children, problems paying attention may result in poor school performance. ADHD is associated with other neurodevelopmental and mental disorders as well as some non-psychiatric disorders, which can cause additional impairment, especially in modern society. Although people with ADHD struggle to focus on tasks they are not particularly interested in completing, they are often able to maintain an unusually prolonged and intense level of attention for tasks they do find interesting or rewarding; this is known as hyperfocus. The precise causes of ADHD are unknown in the majority of cases. Genetic factors play an import ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Spinal-cord Injury
A spinal cord injury (SCI) is damage to the spinal cord that causes temporary or permanent changes in its function. Symptoms may include loss of muscle function, sensation, or autonomic function in the parts of the body served by the spinal cord below the level of the injury. Injury can occur at any level of the spinal cord and can be ''complete'', with a total loss of sensation and muscle function at lower sacral segments, or ''incomplete'', meaning some nervous signals are able to travel past the injured area of the cord up to the Sacral S4-5 spinal cord segments. Depending on the location and severity of damage, the symptoms vary, from numbness to paralysis, including bowel or bladder incontinence. Long term outcomes also range widely, from full recovery to permanent tetraplegia (also called quadriplegia) or paraplegia. Complications can include muscle atrophy, loss of voluntary motor control, spasticity, pressure sores, infections, and breathing problems. In the majority of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
