Phenylpiracetam
| Chemical Information: | |
|---|---|
| Chemical Name: | (RS)-2-(2-oxo-4-phenylpyrrolidin-1-yl)acetamide |
| CAS Number: | 77472-70-9 |
| Molecular Formula: | C₁₂H₁₄N₂O₂ |
| Molecular Weight: | 218.25 g/mol |
| Purity: | ≥99% (as confirmed by Liquid Chromatography-Mass Spectrometry, LC-MS) |
Phenylpiracetam: An In-Depth Guide for Research Applications
Phenylpiracetam, a nootropic compound derived from the original racetam class of drugs, was developed to enhance cognitive performance and physical endurance. Its addition of a phenyl group to the parent molecule, piracetam, makes it significantly more potent, with increased bioavailability and improved blood-brain barrier permeability.
First synthesized in the Soviet Union in 1983, phenylpiracetam was initially developed to support cosmonauts during long-term space missions. It remains a subject of research interest for its potential applications in enhancing memory, focus, and resilience under stress. This guide explores its development, mechanisms, and utility in research contexts.
Development and Purpose
Phenylpiracetam was developed during the Soviet era as a strategic solution to enhance human performance in high-stress and extreme conditions, particularly for astronauts and military personnel. Its development was rooted in the necessity to create a compound that could simultaneously bolster mental acuity, physical resilience, and neural protection, making it indispensable for demanding environments.
Cognitive Enhancement
- Phenylpiracetam’s design specifically targeted improvements in cognitive functions, such as memory retention, learning capacity, and information processing speed, crucial for tasks requiring precision under pressure.
- It was formulated to aid in the recovery from neurological impairments, such as stroke, traumatic brain injuries, and age-related neurodegenerative conditions like Alzheimer’s disease.
- By interacting with neurotransmitter systems, it supports synaptic plasticity, enabling faster adaptation to new information and scenarios, particularly valuable in space exploration where quick decision-making is vital.
Physical Endurance
- The compound was engineered to enhance physical stamina and resilience during prolonged periods of physical and mental stress.
- Its ability to combat fatigue made it suitable for astronauts enduring long missions, as well as for athletes and military personnel operating in physically demanding conditions.
- Phenylpiracetam’s impact on thermoregulation pathways was particularly relevant in cold environments, enabling individuals to maintain optimal function in sub-zero temperatures by reducing the perception of cold and improving energy efficiency.
Neuroprotection
- Recognizing the risks of oxidative stress and ischemia in extreme environments, phenylpiracetam was designed with neuroprotective properties to safeguard brain cells against damage.
- Its ability to stabilize neuronal membranes and enhance cerebral blood flow not only prevents damage but also facilitates faster recovery from injuries and conditions such as hypoxia.
- The compound was further intended to support long-term neural health by reducing inflammation and promoting cellular repair mechanisms, offering potential applications in both acute trauma and chronic neurodegenerative diseases.
The dual focus on cognitive optimization and physical resilience, combined with its robust neuroprotective properties, underscores phenylpiracetam’s role as a multifaceted tool for high-performance scenarios. This strategic development reflects its origin as a solution for some of the most challenging environments encountered by humanity.
Mechanisms of Action
Phenylpiracetam’s mechanisms of action reflect its comprehensive influence on neurotransmitter systems, neuronal integrity, and energy utilization, extending its potential applications across cognitive and physical domains:
Neurotransmitter Modulation
- Phenylpiracetam enhances dopamine and norepinephrine activity, fostering improved mood, heightened alertness, and increased motivation.
- It interacts with acetylcholine receptors, particularly those involved in memory formation and learning processes, further supporting its cognitive-enhancing properties.
- The compound also acts as an AMPA receptor potentiator, contributing to its neuroprotective and excitatory effects on the central nervous system.
Neuroprotection
- By stabilizing neuronal membranes, phenylpiracetam reduces oxidative stress and mitigates excitotoxic damage, which can result from overstimulation of nerve cells.
- Enhanced cerebral blood flow under its influence minimizes the impact of ischemic events, providing protection against conditions that compromise oxygen delivery to the brain.
- Its ability to influence synaptic plasticity supports long-term cognitive resilience and recovery from neurological insults.
Energy Metabolism
- Phenylpiracetam increases ATP production within neurons, optimizing cellular energy availability to sustain prolonged mental and physical activity.
- This energy-boosting effect underpins its role in reducing mental fatigue and enhancing overall stamina during demanding tasks.
Cold Resistance
- Research suggests phenylpiracetam may interact with thermoregulation pathways, reducing the perception of cold and improving tolerance to low-temperature environments.
- Its adaptogenic effects are thought to enhance the body’s resilience to environmental stressors, including extreme cold, making it particularly useful in conditions requiring physical endurance.
- These pathways emphasize phenylpiracetam’s unique combination of cognitive enhancement, neuroprotection, and physical performance benefits, marking its distinct role in both research and application settings.
Applications in Research
Phenylpiracetam is being studied for its broad range of effects on cognition, neuroprotection, and physical endurance. Key research applications include:
1. Cognitive Enhancement
Phenylpiracetam is frequently studied for its ability to improve learning and memory in animal models. Studies suggest that it enhances synaptic plasticity and long-term potentiation, which are critical for memory formation.
2. Neuroprotection
Preclinical models of stroke and traumatic brain injury have shown that phenylpiracetam reduces neuronal damage and improves functional recovery. These findings make it a candidate for exploring treatments for neurodegenerative diseases like Alzheimer’s and Parkinson’s.
3. Physical Performance
Phenylpiracetam’s stimulant-like properties make it a focus of research into fatigue resistance and endurance. Animal studies have demonstrated increased physical activity and resilience under stress.
4. Psychiatric Applications
Research is ongoing into phenylpiracetam’s potential to alleviate symptoms of depression and anxiety by modulating dopamine and norepinephrine systems.
Dosage and Administration in Research
Phenylpiracetam is typically administered orally in research studies. Common dosages in animal models include:
- Low Dose: 10 mg/kg, often used for exploratory cognitive enhancement studies.
- Moderate Dose: 50 mg/kg, commonly applied in neuroprotection and physical endurance research.
- High Dose: 100 mg/kg, reserved for studies involving stress resistance or severe neurodegenerative conditions.
Research durations vary, with studies often lasting from 1 to 12 weeks.
Safety Profile in Research
Phenylpiracetam has a favorable safety profile in animal studies, but some side effects have been observed:
CNS Stimulation:
Increased alertness and wakefulness, which may lead to insomnia in high doses.
Tolerance Development:
Repeated dosing can result in reduced efficacy, suggesting the need for intermittent use in long-term studies.
Mild Behavioral Changes:
Increased locomotor activity and reduced anxiety levels, which may confound certain behavioral studies.
Clinical Development and Status
Phenylpiracetam has been used clinically in Eastern Europe for conditions such as stroke recovery, neurodegenerative diseases, and chronic fatigue syndrome. However, it has not been approved by major regulatory agencies like the FDA or EMA for widespread therapeutic use. Its primary utilization remains in research and specialized clinical contexts.
Recent Research and Findings
Cognitive Recovery in Stroke Models:
Phenylpiracetam improved motor and cognitive functions in rodent models of ischemic stroke, suggesting its potential for aiding recovery after cerebral ischemia.
Memory Enhancement:
Studies demonstrated improved working memory and spatial learning in rats treated with phenylpiracetam, linked to enhanced synaptic plasticity.
Cold Resistance:
In a controlled study, phenylpiracetam-treated mice displayed improved survival rates and reduced stress markers under extreme cold conditions.
Fatigue Resistance:
Phenylpiracetam increased physical endurance in forced swim tests, supporting its application in studying fatigue mechanisms.
Legal and Ethical Considerations
Phenylpiracetam is classified as a research compound and is not approved for therapeutic use in many regions. It is banned by the World Anti-Doping Agency (WADA) due to its performance-enhancing effects. Researchers must ensure compliance with ethical guidelines and restrict its use to controlled laboratory studies.
Conclusion
Phenylpiracetam offers a unique combination of cognitive enhancement, neuroprotection, and physical endurance, making it a valuable tool for researchers exploring nootropic and neurotherapeutic compounds. Its broad range of mechanisms and applications highlights its potential in preclinical and translational research.
As research progresses, phenylpiracetam remains an important compound for understanding the interplay between cognition, neuroprotection, and physical resilience, contributing to advancements in neuroscience and pharmacology.
References
- Zvejniece L, Svalbe B, Vavers E, Makrecka-Kuka M, Makarova E, Liepins V, Kalvinsh I, Liepinsh E, Dambrova M. S-phenylpiracetam, a selective DAT inhibitor, reduces body weight gain without influencing locomotor activity. Pharmacol Biochem Behav. 2017 Sep;160:21-29. doi: 10.1016/j.pbb.2017.07.009. Epub 2017 Jul 22. PMID: 28743458.
- Zhilyuk VI, Levykh AE, Mamchur VI. A study of the mechanisms for antiaggregant activity of pyrrolidone derivatives in rats with chronic hyperglycemia. Bull Exp Biol Med. 2014 Apr;156(6):799-802. doi: 10.1007/s10517-014-2454-8. Epub 2014 May 3. PMID: 24824701.
