What are Ampakines?
Ampakines are drugs that target specific nerve receptors in the brain known as AMPA receptors. By binding onto these receptors, the drugs promote activity and signal transduction. In order to understand what makes them so useful, below is a short analogy.
The human body is basically one gigantic electrical circuit. Think of the nerves as electrical wires responsible for signal transmission and the body’s neurotransmitters as the transformers responsible for modulating the signal transmission process itself and nerve receptors s the wire ports that connect the wires through the transformer.
Understanding of these processes has proven handy when it comes to medical intervention in a variety of diseases and conditions especially those involving the brain. This is where compounds such as Ampakines come in. They are useful when there is deficiency in the glutamate neurotransmitter. The drugs are available in a variety of formulations and combinations but the effects are more or less the same.
Ampakines Mechanism Of Action
The term Ampakines generally refers to compounds that target AMPA receptors in the brain and facilitate activity. However, different Ampakines have different mechanisms of action. Below are the four main mechanisms.
1.) Direct action on AMPA receptors
Some of the Ampakines act by directly binding to the AMPA receptors and facilitating faster and more efficient signal transmission. This is made possible by the fact that some Ampakines are structural and functional analogues of endogenous neurotransmitters. This ensures that there is both affinity (binding) and efficacy (activity) making these drugs true agonists on the receptors.
2.) Direct action on NMDA receptors
This is mechanism of action is also made possible on account of Ampakines’ similarity with the neurotransmitter glutamate. They bind onto the receptors and mediate a variety of functions of which pain relief is one of the most important.
3.) Conversion neurotransmitters
The second common mechanism of action by Ampakines is by metabolism and conversion into active metabolites with activity on the appropriate receptors. Most are converted into glutamate which makes it possible for them to act on the glutamatergic AMPA receptors. This mechanism is just as effective as the first but the need for metabolism makes the drugs much slower.
4.) They lower the pain threshold on pain receptors
Like opioids, they reduce pain by increasing the receptor threshold. These means that only high frequency stimulation signals will be recognized as pain. This activity is experienced on peripheral nerves.
Ampakines are available under different names based on composition and formulation. Below are some of the most popular ones in the market today.
1. Sunifiram-This is a piperazine derivative and is the most widely used Ampakine in the market. Its popularity is on account of the high potency and efficiency that users get to enjoy. It is best known for the memory boosting and concentration improving activity as well as other nootropic effects.
2. Benzoyl Piperidines– These are popular for their brain stimulant effects as well as antipsychotic effect in Alzheimer’s.
3. Benzothiazines– These have a variety of effects on different systems but when used as Ampakines, their inhibitory action on the brain comes in handy for management of ADHD kids.
4. Benzyl Piperazines– These have potent analgesic effects that come in handy when the Ampakines are used in analgesia.
5. Propyl sulfonamides– This group consists of drugs with general nootropic effects including mood regulation, improved memory, creativity and motivation.
Common Uses And Benefits Of Ampakines
With so much diversity in terms of modes of action, Ampakines have a lot to offer users. Below are some of its uses, both common and rare:
· Memory improvement ~ The improved brain function promotes memory consolidation and recall.
· Management of Alzheimer’s ~ This is due to the correlation between glutamate deficiency and progress of the disease.
· Management of Attention Deficit Hyperactive Disorder in children ~ Glutamate has an inhibitory effect on brain cells in children. This is what makes the drugs so effective.
· Improve alertness and concentration ~ This benefit has been applied in the military and is also used by pilots on long flights,
· It is used in minor surgeries as adjuvants to anesthetics for their analgesic effects.
Possible Side Effects Of Ampakines
Side effects are rare and are usually not determined by the dose taken. They are also unpredictable and affect some users while sparing others. They include:
· Nausea and vomiting
· Dysphoria and general loss of motivation
The fact that Ampakines are a group of drugs and not a single drug means that the recommended doses vary greatly. This usually depends on the particular drug. For instance, Sunifiram is the prototype drug in this group and is available in tablet for at a recommended dose of 4-8 mg per day.