CX717

CX717 is a ‘nootropic’ meaning that it is a drug that can help boost brain power. In other words it is a drug that is intended to act like ‘steroids for the brain’ and help you to improve your cognitive performance – things like attention, reflexes, memory and creativity. There are many of these already on the market, but none of them has quite managed to deliver results like those seen in the film ‘Limitless’. Thus when new nootropics enter the testing phases this is something that often garners a lot of attention and interest.

One such drug currently undergoing testing is CX717, which is interesting not only because it sounds like something from a science fiction movie, but also because of the very science fiction way in which it has been tested by the military for its effect on soldiers to see if it can help to improve their alertness and their ability to concentrate for long periods of time. It’s the perfect set up for a science fiction story, helped perfectly by the fact that it was created by a company called ‘Cortex Pharmaceuticals’. But the question is – does it work?

What Is CX717?

CX717 is a particular type of nootropic known as an ‘ampakine’. Ampakines are a class of compound that are known to help enhance attention, alertness, learning and memory. They get their name from the glutamatergic AMPA receptor which has an important role in their function. Glutamate is an amino acid and is the most abundant neurotransmitter in the brain and is stored in the vesicles at chemical synapses between neurons. Glutamate is also involved in ‘synaptic plasticity’ meaning that it plays a role in helping create new neural pathways – in other words in helping us to learn new abilities. Likewise glutamate is a precursor for GABA. GABA inhibits the uptake of serotonin, meaning that you have more of the ‘happiness’ hormone in your brain, meaning that ampakines could be a good form of antidepressant.

CX717 is different from other stimulant nootropics in that it doesn’t cause the same side effects which include the jitters and sleeplessness. It doesn’t create any increase in heart rate, blood pressure of other cardiovascular effects.

Testing

So as this drug shows so much promise – where is it? Well actually CX717 is currently still in testing phases. Too much glutamate however is not a good thing, and in some brain injuries and disease an excess amount of glutamate causes a build up outside the cells which allows calcium to enter via the NMDA receptor channels which can cause damage and death to the cells. Like any pharmaceutical there are many phases it needs to go through before it is permitted for release.

While it was developed in 1996 it wasn’t accepted by the FDA for pilot phase 2 clinical trials until 2005. During this same year however the US department of defense found that when used by rhesus monkeys, the drug was able to counteract the effects of sleep deprivation and meanwhile improve results on cognitive tests. However in 2006 a study funded by DARPA failed to produce these same effects in humans.

In 2006 Cortex Pharmaceuticals announced that they had managed to demonstrate positive effects in treating ADHD patients with CX717, but unfortunately the FDA placed the substance on clinical hold following some animal toxicology studies that demonstrated toxic amounts of compounds in the postmortem bodies of animal test subjects following use of CX717. Further research supplied by Cortex demonstrated this to be a ‘postmortem fixation artifact’ that doesn’t affect living tissue, but the company was unable to continue with trials at the necessary doses.

Further, the low brain barrier penetration along with poor oral-bioavailability meant that it is difficult to deliver the substance to the brain in oral form. Thus the 800mg formulation of CX717 was abandoned for use in treating ADHD.

Other Uses

CX717 has also been proposed as a treatment for ADHD, Alzheimer’s disease, depression and respiratory depression. While the research into CX717 and ADHD is on hold, research continues and particularly in the area of respiratory depression. An unexpected discovery that CX717 could provide respiratory stimulant effects resulted in the development of an intravenous formulation for these conditions.

Meanwhile a variation on CX717 – CX1739 – is being trialed as an oral treatment for sleep apnea. CX1739 is three to five times as potent as CX717 and could also have use as a nootropic in theory if it is able to be used by the brain.

Other Ampakines

Ampakines are currently a hot topic in the field of nootropics, and CX717 was not the first of its kind to be developed by Cortex. Previous attempts include CX546 and CX614. Both of these showed promise as treatments for Alzheimer’s and ADHD, but ultimately they were let down once again by poor bioavailability which resulted in very high doses of around 1000mg. CX717 and CX1739 are newer substances and it is presumed they work with similar mechanisms, though interestingly the exact formulation has yet to be released – likely due to issues surrounding intellectual property and the DARPA funding. The science fiction tale continues…