Pinealon: Benefits, side effects, dosage details, and how it works

Many adults fear aging because of potential health concerns such as neurodegeneration and cognitive decline.1 Although one can take preventive measures to lower their risk for unfortunate age-related changes, such disorders and dysfunctions are unpredictable in their onset.2

There’s a drug therapy, however, that may help smooth over the bumps in the aging process. It’s called Pinealon, a synthetic peptide with clinical uses for neuroprotection, cognitive enhancement, longevity, and other issues related to growing older. In this guide, we examine not only how Pinealon works to achieve outcomes in these areas but also its safety profile, protocol, and other factors to steer you toward the right health decision.

Over the past two decades, Innerbody Research has helped tens of millions of readers make more informed decisions about staying healthy and living healthier lifestyles.

To date, our team has spent more than 1,000 cumulative hours researching and writing about therapeutic peptides. In that time, we’ve studied hundreds of scientific sources, consulted with licensed peptide prescribers, spoken with peptide users, and even tried peptides ourselves. So this guide to Pinealon rests on an enormous foundation of theoretical and practical knowledge, allowing us to give you the most illuminating spotlight on the subject that’s currently possible.

Additionally, like all health-related content on this website, this guide was thoroughly vetted by one or more members of our Medical Review Board for accuracy and will continue to be monitored for updates by our editorial team.

Pinealon is a synthetic tripeptide consisting of the amino acid sequence glutamic acid, aspartic acid, and arginine. It’s also known as EDR peptide.

Pinealon belongs to a class of drugs called peptide bioregulators, or biochemical compounds that come from naturally occurring organisms. In Pinealon’s case, the compound comes from a nootropic and neuroprotective polypeptide complex called Cortexin, whose neuropeptide fractions are derived from the brains of cows and pigs.3 Pinealon’s simpler, ultra-short structure may imbue it with higher stability, better tissue penetration, and a lower risk of hazardous immune responses than its more intricate polypeptide predecessor.4

Research suggests that Pinealon’s mechanism of action involves activating the gene expression and the synthesis of proteins associated with neuronal activity, as well as decreasing the intensity of neuronal cell death.5 More specifically, Pinealon is believed to enter cells and interact with DNA sequences, thereby influencing the activities of several key factors related to cellular and bodily processes. These include:5

• MAPK/ERK signaling pathway: The MAPK/EKR signaling pathway is important for cell proliferation, cell differentiation, and the elimination of damaged cells, among other things.6
• Proapoptotic proteins: Proapoptotic proteins help trigger apoptosis, or programmed cell death, which is critical for removing damaged or unwanted cells (e.g., cancer cells). Examples of proapoptotic proteins activated by Pinealon are caspase-3 (which is also crucial to brain development)7 and p53 (which has a tumor-suppressing action as well).8
• Antioxidant proteins: Antioxidant proteins play a critical defensive role against free radicals and reactive oxygen species, the proliferation of which can lead to dysregulated apoptosis, which in turn is associated with pathologies such as autoimmune diseases, cancer, and neurodegeneration.9 10 11

In addition to the above, Pinealon appears to extend cellular lifespans via telomere lengthening. As we discussed in our epitalon guide, telomeres are protective “caps” of DNA sequences at the ends of chromosomes. They shorten every time a cell divides and eventually reach the point at which proper cell division is no longer possible, resulting in cellular senescence.12 Senescent cells, in turn, can lead to various age-related diseases, including but not limited to cancer, atherosclerosis, osteoarthritis, and cognitive decline.13 14

Pinealon can prevent cellular senescence by regulating the production of a hormone called irisin,15 high levels of which are associated with longer telomere lengths and, therefore, longer cellular lifespans.16

Pinealon’s relationship to DNA sequences and irisin is the basis for its main therapeutic applications: improved cognitive function, neuroprotection, and antiaging.

Below, we summarize the research in support of its use in these areas:

Smaller bodies of research suggest that Pinealon may have other uses as well. For example, a 2012 study in old rats found that Pinealon injection could improve behavioral sleep,30 and a 2014 in vitro study in brain cortex cells demonstrated that the peptide may stimulate the expression of serotonin,31 a neurotransmitter that regulates mood.32

There are few to no dedicated safety studies on Pinealon — not in the English language, at least — but the existing relevant research points to a generally small side effect profile for peptide bioregulators in general.5 By way of a more specific example, we can look to studies on Cortexin (the complex from which Pinealon is derived), which is described in a 2014 study as having “high efficacy and safety.”33

That’s not to say that adverse events aren’t possible. Some people may experience allergic reactions to Pinealon, or really any peptide,34 and by virtue of its being an injectable peptide, it may cause milder but fairly common side effects such as injection site reactions, muscle aches, gastrointestinal discomfort, headache, fatigue, lightheadness, flushing, and possibly fever.

Research-grade vs. pharmaceutical-grade Pinealon

Pinealon is not an FDA-approved medication, so you may find its clinical availability to be quite limited and then be tempted to seek it out from an online retailer. That’s a potentially treacherous path to tread, as many online retailers not only lack verified reputations but also deal in research-grade peptides.

The difference between research-grade and pharmaceutical-grade peptides comes down to purity and fitness for human consumption. Because research-grade peptides aren’t held to the same quality standards as their pharmaceutical-grade counterparts, they’re often of a dangerously low purity that increases the risk of adverse events.35 Hence, they are for laboratory use only and are not suitable for human consumption. If you want to have your peptide and benefit from it too, you should either stick to a prescription from a licensed physician or carefully read the fine print on the product page to ensure you’re getting pharmaceutical-grade material.

Admittedly, getting a Pinealon prescription may be difficult, but it isn’t impossible. If your physician determines that it’s necessary to treat an indicated health condition, and no other treatment is viable for you, then you could be exempted from rules that prohibit the use of non-FDA-approved medications.36

Expectations and user experiences aren’t normally among the available information about a therapeutic peptide. Fortunately, the medical providers we’ve consulted, who are licensed prescribers of peptides, have given us invaluable insight into these otherwise esoteric factors. Thus, we’re able to summarize the key points about Pinealon’s dosing, administration, storage, and timeline of benefits below.

Dosing, administration, and storage of Pinealon

A standard Pinealon dose is 1mg, though your exact dosage may depend on individual factors such as age and weight. Your prescribing physician will likely instruct you to take five doses per week, with administration in the morning or early afternoon to optimize use of the peptide’s cognitive-enhancing effects.

Pinealon is normally administered via subcutaneous injection into the belly, thigh, or arm. Like other injectable peptides, it will likely come packaged as a powder in a vial along with needle syringes and a vial of bacteriostatic water. Before you can dose the peptide, you must reconstitute the powder into an injectable solution, which entails combining a specific measure of the water with the powder. Take your time here so that all of the powder gets dissolved. Be gentle and don’t shake the mixture, as agitation can cause degradation.

Once reconstituted, the supply of Pinealon should last four weeks. Between doses, you should store the peptide at around 4°C, or 39°F.37 A refrigerator, then, would be the ideal storage container.

Timeline of benefits from Pinealon

Within 1-2 weeks of beginning your Pinealon treatment, you should see an increase in your focus and mental clarity — less brain fog and more cognitive vigor — as well as improvements in mood and stress resilience.

In 4-6 weeks, the cognition- and mood-enhancing effects become more pronounced, with significantly improved memory recall and emotional balance. During this time, you may notice attendant decreases in chronic fatigue. These benefits improve further at up to 8-12 weeks.

Thereafter, Pinealon begins to yield its less outwardly noticeable (but no less important) health effects, namely the ability to reduce the risk and effects of age-related cognitive decline.

Pinealon’s various therapeutic properties make it a suitable peptide therapy for the following populations:

• Older adults: Pinealon’s neuroprotective action may help stave off forms of age-related cognitive decline, including those related to a neurodegenerative disease. Additionally, its antioxidant and telomere-preserving potential can slow aspects of the aging process and improve one’s quality of life as they do age.
• Other people with cognitive needs: Anyone whose occupation requires long periods of focus could benefit from Pinealon’s nootropic effects. That’s a broad potential user base that includes students, creatives, office employees, and trade workers.
• People with mood disorders: With its ability to regulate neurotransmitters, Pinealon may help people with generalized anxiety, depressive symptoms, or other symptoms of a mood disorder.
• People with sleep disorders: The same regulatory action on neurotransmitters means that Pinealon could potentially help normalize a person’s sleep-wake cycle and thereby improve their sleep quality.

Who is not a candidate for Pinealon?

As for people who should not take Pinealon, the list includes:

• Pregnant or breastfeeding mothers: Like many other drug treatments, Pinealon lacks sufficient scientific evidence to support its safety for the developing fetus or child.
• People with active cancer or a history of cancer: Pinealon’s action on proapoptotic cells is, paradoxically, both anti- and procarcinogenic. It can lead to cancer when the apoptotic process doesn’t work correctly.38 Indeed, in a 2019 study published in the International Journal of Cancer, the researchers noted that the proapoptotic caspase-3 can potentially promote tumor formation while preventing cancer cell development.39

Because Pinealon is not an FDA-approved substance, its availability in the United States is relatively scarce. As we suggested earlier, some licensed physicians are willing to prescribe it, but you may first need to demonstrate that Pinealon meets a health need that other, approved medications do not.36

No doubt that you can also find Pinealon online, but you’ll come across many research-grade products that (again) are not suitable for human use. Perhaps there are some online retailers that sell pharmaceutical-grade products, but you have to read the fine print carefully to make sure you’re getting legitimate medication.

That said, pharmaceutical peptides belong to an ever-shifting medical landscape, and the regulations concerning Pinealon may eventually become more permissible. We’ll closely monitor the peptide space in the meantime and update this guide accordingly.