Of all the nootropic drugs, the ampakine class is perhaps the most powerful. Ampakines are positive allosteric modulators of the Glutamate receptors. The stimulation of the AMPA (and NDMA) glutamate receptors by ampakine drugs has extreme benefits for cognitive functioning. Several groups of ampakine drugs like the CX and LY classes are going through clinical trials by two pharmaceutical giants and may be available by prescription in the future.
The racetams are ampakine drugs themselves however it is not known the exact strength they exert on the Glutamate receptors. It is known that racetams act as ampakines by stimulating the Glutmatic systems. Some racetams seem to have a higher affinity to activation of the AMPA and NDMA receptors however it is not sure how effective each racetam is as they also act of the Acetycholine system. This makes it hard to determine which nootropic method of action is more prevalent as Acetylcholine receptor stimulation also contributes to improved cognition.
The CX class is a group of powerful ampakine drugs being investigated by Cortex Pharmaceuticals in Irvine California. The CX class share the benzoylpiperidine and benzoylpyrrolidine structure. Cortex Pharmaceuticals have been experimenting with many AMPA positive allosteric modulators over the last decade and seem to be specifically targeting the area of Alzheimer’s and ADHD treatment. Animal and human trials have been conducted on several of the CX drugs.
One of the first CX drugs to be investigated was CX-516, also known as Ampalex. The trials targeted CX-516 as a treatment of Alzheimer’s and ADHD. Animal trials showed great promise however human trials showed poor results due to low potency and short half-life.
CX-717 is much stronger than the previous CX compounds. It was being investigated by Cortex Pharmaceuticals for both Alzheimer’s and ADHD. According to their studies, CX-717 has great benefits in treating both however the FDA has put their application on hold due to tissue toxicology in animal models. Cortex has stated CX-717 as safe and well tolerated in humans however more evidence needs to be submitted to the FDA before it is brought to market as an ampakine or nootropic drug.
Very little information has been released about CX-1739 by Cortex Pharmaceutical, however it has been proposed to be 5x more potent than CX-717. We are likely to see more of the CX-1739 ampakine nootropic in the future.
Eli Lilly Pharmaceuticals was the first company to bring Penicillin and human insulin to market and they have been focusing specifically on the LY Class of ampakine drugs. The LY class are biarylpropylsulfonamide derivatives and have been shown to be potent nootropics in animal models. Another interesting fact about this LY ampakine class is their apparent stimulation of BDNF protein which is huge in the formation of new neurons and synapses as well as long term memory. This could have some huge benefits for repairing damages to the brain.
This ampakine is being investigated by Eli Lilly and has shown great promise in improving cognitive functioning in animal models. LY-404187 also has possible promise is treating Schizophrenia, Parkinson’s disease and ADHD. Not all of these possible applications relate to the primary AMPA potentiation method of action. It is unsure if Eli Lilly will move ahead with LY-404187 as they have a large group of biarylpropylsulfonamide derivatives to work with and may decide to proceed further with any of them.
This ampakine has been the most researched by Eli Lilly. Like LY-404187, it also seems to have a stimulation of BDNF in the hippocampus. LY-503430 is a potent ampakine nootropic with neuroprotective effects. It is being investigated for use in Alzheimer’s, Parkinson’s, Schizophrenia and depression.
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