Ampakines


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Therapeutic Uses of Ampakines

Ampakines are a class of drugs that act as positive allosteric modulators of AMPA glutamate receptors in the brain. They do not have any clinically approved therapeutic uses yet, but are being explored and studied as possible treatments for a variety of neurological and psychiatric conditions, including:

Cognitive disorders: Ampakines are being studied as potential cognitive enhancers to treat age-related and neurodegenerative cognitive decline, such as Alzheimer's disease, Parkinson's disease dementia, and mild cognitive impairment. By enhancing glutamatergic transmission, ampakines may improve attention, alertness, memory, and executive function.
Depression: Some research shows ampakines may have antidepressant effects by increasing BDNF and promoting neurogenesis. They are being investigated as possible standalone or adjunct treatments for major depressive disorder and treatment-resistant depression.
Schizophrenia: Ampakines are proposed to potentially normalize glutamatergic dysfunction observed in schizophrenia. Some studies show they may ameliorate cognitive deficits in schizophrenia when used with antipsychotic medications.
ADHD: Early research shows ampakines may reduce hyperactivity and attention deficits in animal models of attention-deficit/hyperactivity disorder (ADHD). Further study is needed to determine efficacy in humans.
Recovery after stroke or trauma: By promoting plasticity, ampakines are being studied to facilitate rehabilitation and functional recovery in neurological disorders involving brain injury, such as stroke or trauma.

While promising, most ampakine compounds are still in early research stages. Further clinical trials are needed to fully demonstrate safety, tolerability and efficacy across these potential therapeutic applications in humans.

Ampakines have a broad range of potential therapeutic applications. These include relief of the effects of sleep deprivation, poor memories, stupidity (yes, they could be smart drugs!), Alzheimers, other forms of dementia, autism, schizophrenia, and general cognitive decline. Memory decline in human aging and dementia is linked to dysfunction of the cholinergic system. Also mentioned as potential candidates for ampakine therapy are Parkinson’s disease, Rhett syndrome, and depression.

Ampakines increase excitatory monosynaptic (that is - by one synapse between two neurons) responses, allowing increased communication rates through the neural network. There is hope that ampakines may improve long-term potentiation that assists in memory.

CX-516 (Ampalex) is known to enhance response of neuronal receptors, and it suspected to be a potential therapy for Alzheimer's Disease. Preliminary results suggest that CX516 and other ampakines hold promise for the treatment of schizophrenia. A 2006 study at the University of Alberta found that CX-546 reversed respitory depression in rats. It worked for both opiod and barbituate-induced repitory depression. The University of Alberta has also been researching the use of ampakines to help surgery patients keep breathing even when they have been given opiates as anaesthesia. Meanwhile University of California at Irvine scientists have found ampakines can affect the symptoms of Huntington's Disease in mice. How the drugs stay in the body is the study of pharmacokinetics.

Scientists at the University of California at Irvine found ampakines had a big effect on the brains and the behavior of rats. They examined the brain dendrites of middle-aged rats that got ampakines ad found the dendtire has length and branching patterns similar to those of young rats. When placed into a maze, the rats that had been treated with ampakines figured out their new environment faster than untreated rats did. These results seem to indicated ampakines have cognitive benefits.

A research team at Wake Forest University is verifying and extending preliminary data demonstrating that ampakines are protective against cognitive deficits associated with sleep deprivation. Ampakines already have been proven safe in humans, and are currently in clinical trials for the restoration of mental function in patients with dementia. Autism is of interest, too. There has also been some work on ampakines for treatment of Rett syndrome. It is envisioned that Ampakines may provide an alternative to current stimulant medications used by pilots.

Nootropic Use by Healthy People

The word nootropic is a combination of the Greek words for "mind" and "bending." Nootropics include coffee, nicotine, and other common substances that that can stimulate the mind. Interest in ampakines focues on their nootropic aspects.

Use of nootropics has become widespread among college students, entrepreneurs, and medical professionals. Although nootropics encompass different forms of mind-altering drugs, the large majority of users aim to boost their memory and focus.

Avid nootropic users sometimes employ “stacks” - combinations of supplements or drugs taken at certain intervals. The nootropic community shares these folk practices person to person and on internet message boards. Recently some commercial concerns have started selling stacks. However, this shows the field is driven more by buyers and users than by sellers.

Memory Enhancement for Good and Bad

Piracatem, a well-known favorite of the "smart drug" community, can be considered an ampakine. It helps with memory.

Scientists continue to delve into the neuroanatomical, neurochemical, and molecular basis of wakefulness, which remains largely a mystery. It is known that multiple brain areas (hypothalamus, thalamus, and basal forebrain) must integrate and relay information from the brainstem to the cortex for the brain to be wakeful. Britain's Academy of Medical Sciences projects that cognitive enhancement drugs will eventually become widespread and prompt regulation. The think-tank Furturelab reported to the British government that enhancement drugs may have to be subsidized so wealthy children do not gain an unfair advantage over their poorer classmates.

Do you want a "super-memory"? Maybe not. People with huge memories are often poor at problem-solving and remembering so much seems to degrade the ability to generalize – which is a hallmark of intelligence. It might be that the memory capacity of the healthy young adult or teen is optimal. Ampakines and similar drugs may find the most demand for age-related memory decline, and certainly for mental illnesses like Alzheimer's and Huntington's. Some worry that long-term use of ampakines will have a negative effect on neural plasticity, especially in the brains of children. But there is very little data.

People worry about potential for excitotoxicity ampakines may cause.

During sleep the brain does synaptic pruning maintenance on itself. Less active synapses are removed. This is an important part of keeping the brain healthy and the person sane. Impaired pruning is associated with autism. Ampakines increase the plasticity of the brain, which can help the person be better and learning and possibly at remembering, but some worry that increase plasticity may decrease pruning activity. Also, some worry that while ampakines may increase the person’s cognitive ability, they may decrease spatial memory and motor functioning abilities.


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