RGPU-95 (p-Cl-Phenylpiracetam), ≥98%
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RGPU-95 (p-Cl-Phenylpiracetam) is an 5x-10x more potent derivative of the nootropic compound Phenylpiracetam.
Chemical Name | 2-(2-oxo-4-(4-chlorophenyl)-pyrrolidin-1-yl)acetamide |
CAS Number | 213178-69-9 |
Purity | ≥98% |
Form | White or off-white powder |
Molecular Weight | 252.7 g/mol |
Melting Point | Unknown |
Molecular Formula | C12H13ClN2O2C12H13ClN2O2 |
Synonyms | 1-Pyrrolidineacetamide, 4-(4-chlorophenyl)-2-oxo; RGPU-95 |
Precaution and Disclaimer:
This Material is Sold For Research Use Only. Terms of Sale Apply.
Not for Human Consumption, nor Medical, Veterinary, or Household Uses.
RGPU-95 (p-Cl-Phenylpiracetam) 1.0 Grams, ≥98%
Chemical Information:
CAS Number: | 213178-69-9 |
Purity: | ≥98% |
Molecular Weight: | 252.7 g/mol |
Melting Point: | Unknown |
Molecular Formula: | C12H13ClN2O2 |
Synonyms: | 1-Pyrrolidineacetamide, 4-(4-chlorophenyl)-2-oxo; 2-(2-oxo-4-(4-chlorophenyl)-pyrrolidin-1-yl)acetamide; RGPU-95 |
PubChem CID: | NA |
SMILES: | C1(C(CN2CC(N)=O)CC2=O)=CC=C(C=C1)Cl |
Technical Information:
Application: | RGPU-95 (p-Cl-Phenylpiracetam) is an 5x-10x more potent derivative of the nootropic compound Phenylpiracetam. |
Appearance: | White or off-white powder |
Physical State: | Solid |
Solubility: | Soluble to 5 mM in Ethanol, Sparingly Soluble in Water. |
Storage: | Store at room temperature or cooler, in a sealed airtight container, protected from heat, light and humidity. |
Stability: | Stable for at least two years when stored as above. |
Background:
RGPU-95, or p-Cl-Phenylpiracetam, is a derivative of Phenylpiracetam, experimentally shown to be around 5x – 10x more potent. RGPU-95 is an experimental compound and was designed to be more effective than Phenylpiracetam in reducing anxiety and depressive behavior (greater anxiolytic and antidepressant potential) in patients with neurological disorders.
Regarding Phenylpiracetam – it is a Nootropic derivative of Piracetam with an added phenyl-group that gives it increased efficacy in clinical studies. Phenylpiracetam has been studied for anti-amnesiac, antidepressant, anticonvulsant, antipsychotic, anxiolytic, and memory enhancing effects. [1]
In some countries, Phenypiracetam has been approved for pharmaceutical use and is prescribed for a variety of clinical uses including to boost cognitive performance and memory, to improve resistance to cold, as an anticonvulsant and antiepileptic, and to improve immune response. [2]
Manufacturers of Phenylpiracetam cite its rapid absorption (thought to be a product of enhanced lipophilicty when compared to Piracetam).[3]
Pharmacokinetics:
RGPU-95 is a very new compound and more research is warranted into its physical, chemical and pharmacological properties. In terms of its pharmacokinetics, it is thought to be similar to Phenylpiracetam.
Animal studies show a half-life of 2.5-3hours for Phenylpiracetam dosage of 100mg/kg and RGPU-95 is thought to exhibit a similar, or slightly longer, timeframe of action.[4]
After a 25mg/kg injection of Phenylpiracetam, some animal studies have shown detectable concentrations of around 67-73µg/g in the brain, while others estimate around a 1% efficacy in terms of the concentration of Phenylpiracetam that reaches the brain.[5] Preliminary research points to a slight to moderate increase in absorption efficacy and ability to cross the blood-brain barrier for RGPU-95 compared to Phenylpiracetam.
It is important to note that there is currently a real lack of data on the pharmacological effects of RGPU-95, both in humans and in animal models. Furthermore, animal models are comprised solely of rodent studies, which often have a low relevance to primate and human models. Even anecdotal evidence and unpublished studies are hard to come by, and it is especially important to emphasize this lack of data to less experienced researchers.
Modes of action:
RGPU-95, being a derivative of Phenylpiracetam, shares much of its physical and chemical attributes. For example, Phenylpiracetam is a weak DRI and sigma receptor agonist, and has been found to upregulate dopamine D2 and D3 receptors. Furthermore, Phenylpiracetam modulates glutamatergic receptors and nACh recepors. Likewise, RGPU-95 is believed to share these attributes, but to a more potent degree. RGPU-95 exhibits more pronounced anxiolytic, antidepressant, cognitive-enhancing effects. The increased anxiolytic and antidepressant effects are most evident, reflecting possible GABAergic activity - indirectly downstream through nACh recepor binding, or perhaps directly through affinity for GABA receptors. This latter possibility is suggested when comparing RGPU-95 to similar compounds around the 4-(4-chlorophenyl)-pyrrolidone pharmacophore.
Further Scientific research:
Please note that this is may not be a complete account of the scientific research on RGPU-95 to date. RGPU-95 is a new experimental research chemical and scientific data is not yet available for much of the information that we would like to provide. We have made an effort to compile a worthy account of the information currently available about this experimental compound here.
Should you or your organization have knowledge of any information that we may have missed – preferably from unbiased and well-organized studies that you have personally conducted using this product – please feel free to send us an email at newmind@newmind.com.
At this point, RGPU-95 needs to be treated as an experimental chemical with a potentially high toxicological risk. It is only suitable for preclinical R&D purposes, for further characterization of its physical and chemical properties, or for biochemical pathways research using cell cultures.
Should you wish to purchase RGPU-95 for either institutional or independent research, it is important to clearly indicate the type of research you will be conducting, the level of expertise held by your research team, and the type of laboratory equipment at your disposal.
Clinical Reviews:
There are not enough data for any meta-analyses or reviews to have been published at this time.
Human studies:
There are currently no published studies on the effects of RGPU-95 on human participants.
Since RGPU-95 (p-Cl-Phenylpiracetam) was developed as a more potent form of Phenylpiracetam, and due to the lack of data on the effects of this compound, we have included a selection of studies pertaining to Phenylpiracetam’s effects below.
A recent study, published in 2015, pointed to Phenylpiracetam’s strong anxiolytic effects. The study was conducted using a group of 70 human participants – patients with mild neurosis or major depressive disorder (MDD), in comorbidity with cardiovascular disease. The findings also found that these effects begin to become reduced after 4-8 weeks of chronic administration. [6]
Another study showed Phenylpiracetam’s strong potential to act as an anticonvulsant and antiepileptic. This clinical study was again conducted using human participants – 75 patients with epileptic disorders. Results showed a significant reduction in the number and severity of seizures as well as improvements in cognitive performance and quality of life parameters. [7]
In 2014, a large Russian-based clinical study was conducted on over 1100 human participants to elucidate the efficacy of Phenylpiracetam on patients suffering from brain ischemia and asthenic syndrome (characterized by irritability and fatigue). The results indicated a 2-fold decrease in negative symptoms after 3 months of daily Phenylpiracetam treatment. [8]
Another Russian study, published in 2010 and conducted on 400 patients with ischemic stroke, found that those treated with Phenylpiracetam showed improved scores on Barthel, Lindmark, Scandinavian scales and Merton and Sutton scales – indicating a significant improvement in neurological performance and in daily living activities (well-being). [9]
In 1999, researchers published results showing that Phenylpiracetam could be detected in human urine. The authors also found that Phenylpiracetam was effective in increasing physical endurance and promoting resistance to cold. [10]
Animal studies:
In animal models of cognitive disorders, RGPU-95 at dosages of between 0.05 – 0.2mg/kg produces slight to moderate cognitive performance increases, memory enhancement, antidepressant, anxiolytic, antipsychotic, and analeptic effects. At this dosage range, RGPU-95 appears to have mild mood-lifting and wakefulness-promoting (eugeroic) effects – similar to a dosage range of 0.5 – 2mg/kg Phenylpiracetam.
One study looked into gender differences in the effects of RGPU-95 and Phenylpiracetam on rats. The authors found that RGPU-95 tended to have stronger anxiolytic and antidepressant effects on male rodents and had stronger anxiolytic effects than Phenylpiracetam but lower than diazepam. [11]
No doses greater than 0.4mg/kg were administered in large animal models due to profound and noticeable effects that were difficult to categorize but did not necessarily reflect the type of research data that was being sought. We would not recommend using dosages equal to or greater than 0.4mg/kg in animal models.
Precaution and Disclaimer:
This Material is Sold For Research Use Only. Terms of Sale Apply.
Not for Human Consumption, nor Medical, Veterinary, or Household Uses.
References:
[1] Phenylpiracetam. (2018). Examine.com: Unbiased Supplements Information [online]. Available from: https://examine.com/supplements/phenylpiracetam/.
[2] Classification Status of Racetams,. (2016). MedSafe New Zealand [online]. Available from: http://www.medsafe.govt.nz/profs/class/Agendas/agen53Racetams.pdf [Accessed 18 July, 2018]
[3] Malykh AG, Sadaie MR. (2010). Piracetam and piracetam-like drugs: from basic science to novel clinical applications to CNS disorders. Drugs, 70(3):287-312.
[4] Spektor SS, Berlyand S. (1996). Experimental pharmacokinetics of carphedon. Pharmaceutical Chemistry Journal, 30(8): 489–490
[5] Zvejniece L, Svalbe B, Veinberg G, Grinberga S, Vorona M, Kalvinsh I, Dambrova M. (2011). Investigation into stereoselective pharmacological activity of phenotropil. Basic Clin Pharmacol Toxicol, 109(5):407-12.
[6] Medvedev VE, Frolova VI, Epifanov AV. (2014). [New possibilities of pharmacotherapy in cardiovascular patients with mental disorders] (Article in Russian) Zh Nevrol Psikhiatr Im S S Korsakova, 114(9):30-7
[7] Savenkov AA, Badalian OL, Avakian GN. (2013). [Nootropics and antioxidants in the complex therapy of symptomatic posttraumatic epilepsy] (Article in Russian), Zh Nevrol Psikhiatr Im S S Korsakova, 113(6):26-34
[8] Fedin A, Solov'eva E, Mironova OP, Fedotova AV. (2014) [Treatment of asthenic syndrome in patients with chronic brain ischemia: results of the non-interventional observational program TRIUMPH]. Zh Nevrol Psikhiatr Im S S Korsakova, 114(12):104-111.
[9] Koval'chuk VV et al. (2010). [Efficacy of phenotropil in the rehabilitation of stroke patients] (Article in Russian). Zh Nevrol Psikhiatr Im S S Korsakova, 110(12 Pt 2):38-40