RGPU-95
From €34.41
RGPU-95 is a novel nootropic compound with potential neuroprotective and cognitive-enhancing effects. It may improve memory, focus, and learning abilities, while also providing protection against oxidative stress and neuroinflammation.
For a more detailed description and lab analysis, please see the sections below.

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Description
RGPU-95 (p-Cl-Phenylpiracetam) – Powder
At a Glance: High-Potency Synthetic Racetam & AMPA Receptor PAM
RGPU-95 — also known as p-Cl-Phenylpiracetam or 4-chlorophenylpiracetam. A synthetic racetam bearing a chlorine substituent at the para position of the phenyl ring; the (R)-enantiomer of 4-chlorophenylpiracetam.
Positive allosteric modulator (PAM) of AMPA-type glutamate receptors; reported to also interact with nicotinic acetylcholine receptors (nAChR). Demonstrates higher binding affinity than Phenylpiracetam.
Glutamatergic modulation studies, AMPA receptor PAM pharmacology, structure-activity relationship (SAR) research within the racetam class, cognitive and neuroplasticity models.
Not FDA-approved. Not authorized for human or veterinary use. Phenylpiracetam is prohibited by WADA; RGPU-95 is expected to carry the same classification. For laboratory research only.
Research Context and Compound Background
Phenylpiracetam (Phenotropil) was developed in Russia in the 1980s as a structurally enhanced analog of the founding racetam, Piracetam. The addition of a phenyl ring to the pyrrolidone core conferred increased CNS penetration and greater apparent potency. RGPU-95 represents a further rational modification: replacing a hydrogen atom on the phenyl ring with a chlorine substituent at the 4′ (para) position.
This halogenation step was investigated by researchers at the Russian State Pedagogical University (RGPU) in St. Petersburg, from which the compound derives its name. The para-chloro substitution increases electron-withdrawing character of the phenyl ring, which is reported to improve binding affinity at target receptors and shift the effective concentration range downward relative to Phenylpiracetam.
Phenylpiracetam appears on the World Anti-Doping Agency (WADA) Prohibited List as a stimulant analog. As a close structural derivative, RGPU-95 is expected to fall within the same or an analogous prohibited category. This compound is not approved by any regulatory authority for human use and is supplied exclusively for qualified laboratory research.
Within the broader racetam SAR landscape, RGPU-95 occupies the niche of a higher-potency, lower-dose-range tool compound — useful for probing AMPA receptor pharmacology at concentrations where the parent compound shows minimal activity, and for comparative studies examining how halogenation of the phenyl ring influences receptor selectivity, cognitive assay outcomes, and off-target interaction profiles.
Mechanistic Overview
RGPU-95 is understood to act through at least two primary receptor systems, with a potential secondary interaction involving monoaminergic pathways. The mechanistic profile is consistent with other members of the phenylpiracetam class, but the chloro substitution appears to increase receptor binding affinity across these targets.
- Binds to allosteric site on AMPA-type ionotropic glutamate receptors
- Slows receptor desensitization and deactivation kinetics
- Enhances EPSP amplitude and duration at active synapses
- Facilitates long-term potentiation (LTP) induction thresholds
- Improves signal-to-noise ratio of fast excitatory transmission
- Proposed weak allosteric interaction with nAChR subtypes
- May modulate cholinergic tone in attention-related circuits
- Potential synergistic interaction between glutamatergic and cholinergic pathways
- Consistent with the pro-attentional effects observed in Phenylpiracetam preclinical models
- Phenylpiracetam exhibits indirect dopaminergic-adjacent effects; RGPU-95 is expected to follow similarly
- Does not appear to directly bind monoamine transporters at standard research concentrations
- Mild locomotor activation observed in rodent models — basis for WADA-class stimulant classification
- Dopaminergic affinity of the R-isomer specifically remains incompletely characterized in public literature
Comparative Profile: RGPU-95 vs. Phenylpiracetam
| Property | Phenylpiracetam | RGPU-95 (R-isomer) |
|---|---|---|
| Core scaffold | 2-oxopyrrolidine + phenyl ring | 2-oxopyrrolidine + 4-chlorophenyl ring |
| Halogenation | None | Cl at para position |
| Reported relative potency | Standard reference (1×) | 2×–5× higher (preclinical reports) |
| AMPAR binding affinity | Moderate | Increased |
| Effective in vivo dose (rodent) | 50–100 mg/kg | 25–50 mg/kg |
| Onset in rodent models | 60–90 min (oral) | Likely comparable; potentially faster IP onset |
| Stimulant-like effect | Mild | Mild; comparable |
| Tolerance onset | Rapid (2–3 days repeated dosing) | Expected similar; limited repeat-dose data |
| Public literature availability | Established | Limited; primarily patent literature |
Reported Preclinical Research Findings
Scope: The following findings are drawn from peer-reviewed publications, patent filings originating from RGPU, and data from collaborating Russian research institutions. The majority of available evidence is preclinical (rodent models). No peer-reviewed human clinical trial data exist.
Spatial & Declarative Learning
- Facilitated acquisition in T-maze and Morris water maze paradigms
- Enhanced performance in step-through passive avoidance tasks
- Improved active avoidance learning at 25–50 mg/kg doses
- Accelerated novel behavioral task acquisition
Locomotor & Physical Performance
- Brief, dose-dependent increase in voluntary locomotion in open-field assays
- Elevated voluntary wheel running in rodent models
- No direct peripheral sympathomimetic cardiovascular activation reported
- CNS-mediated stimulant profile consistent with WADA classification
Affective & Anti-immobility Effects
- Reduced behavioral immobility in forced-swim test models
- Anti-immobility profile consistent with antidepressant-like activity
- Elevated exploratory behavior in anxiolytic-adjacent paradigms
Tolerance & Repeat Dosing
- Parent compound (Phenylpiracetam) shows behavioral tolerance within 2–3 days of continuous dosing
- Repeat-dose behavioral data for RGPU-95 specifically are extremely limited
- Cycling protocols (3 weeks on / 1 week off) recommended based on class-level evidence
- Tolerance characterization should be included in any chronic dosing study design
Co-administration Considerations in Experimental Models
- Choline Precursors (Alpha-GPC, Citicoline): Support cholinergic substrate availability; relevant given RGPU-95’s proposed nAChR interactions. Useful in paradigms examining combined glutamatergic-cholinergic modulation.
- Other AMPA PAMs (Aniracetam, Noopept): Potential additive effects at the AMPA receptor. Use dose-response matrices to distinguish additive from supra-additive interactions; risk of over-excitation at high combined concentrations.
- ⚠️ Serotonergic Agents (SSRIs, 5-HTP): Interaction profile unknown; potential for additive effects on affective behavioral measures. Include appropriate washout periods and separate experimental groups.
- ⚠️ Dopaminergic Precursors (L-Tyrosine, L-DOPA): Given RGPU-95’s monoaminergic-adjacent profile, combination with direct dopamine precursors may confound interpretation of behavioral endpoints. Characterize individually first.
- 🚫 GABAergic Agents / Seizure Medications: Functionally oppose the glutamatergic enhancement mechanism; combination may produce paradoxical or difficult-to-interpret results. Do not co-administer without explicit study design justification.
- 🚫 Pro-convulsant Compounds: AMPA PAMs lower the threshold for excitotoxic events at high concentrations. Avoid co-administration with compounds that independently reduce seizure threshold.
- 🚫 NMDA Antagonists (Concurrent): Simultaneous AMPA enhancement and NMDA blockade produces complex, unpredictable plasticity effects. Separate mechanistic studies before designing co-administration paradigms.
Safety, Toxicological Profile, and Handling
Available Toxicological Data: Formal GLP toxicology data specific to RGPU-95 are not available in the public domain. The following is extrapolated from Phenylpiracetam preclinical data and general racetam class characterization.
| Parameter | Available Information | Source / Confidence |
|---|---|---|
| Acute rodent LD₅₀ | Estimated >150 mg/kg based on class data; specific RGPU-95 LD₅₀ not formally established | Extrapolated |
| Hepatotoxicity | No hepatotoxicity reported at research concentrations in racetam class | Class-level |
| Cardiotoxicity | No direct sympathomimetic cardiovascular effects reported; peripheral activation appears minimal | Class-level |
| Lipophilicity / Tissue accumulation | Moderate lipophilicity; potential for adipose tissue accumulation with repeated dosing — factor cessation kinetics into chronic study design | Predicted |
| Excitotoxicity risk | Theoretical risk at supratherapeutic AMPA PAM concentrations; dose-response verification essential | Theoretical |
In Vivo Behavioral Observations (Transient)
- Mild agitation / increased locomotion: Observed in the first 2–3 hours post-administration; consistent with the compound’s stimulant-adjacent mechanism. Typically self-resolving.
- Elevated motor activity: Dose-dependent increase in exploratory behavior in open-field assays; should be distinguished from cognitive effects using appropriate behavioral controls.
- Reduced food intake: Mild anorexigenic effect reported in some rodent models; monitor body weight in chronic paradigms and adjust caloric access protocols accordingly.
- Diuresis: Mild diuretic effect noted in some animal models; ensure animals have ad libitum water access during treatment periods.
- 🚫 Not for use in pregnant or lactating models.
- 🚫 Not for juvenile models without specific developmental neuroscience justification; baseline neuroplasticity is maximal in developing animals and may confound interpretation.
- ⚠️ Caution in seizure-prone models. AMPA positive modulation lowers excitotoxic threshold; use with appropriate seizure monitoring in susceptible strains.
- ⚠️ Caution in anticoagulation studies. Flavonoid-adjacent scaffold may interact with clotting pathway assays; verify in your specific model.
Frequently Asked Research Questions
How does RGPU-95 differ structurally and pharmacologically from Phenylpiracetam?
Structurally, RGPU-95 differs by a single modification: a chlorine atom at the para position (C-4′) of the phenyl ring. The pyrrolidone core and acetamide tail of the racetam scaffold are conserved. Pharmacologically, RGPU-95 (as the R-enantiomer) is reported to produce comparable qualitative effects to Phenylpiracetam at approximately 2–5× lower doses in rodent behavioral models.
Why is only the R-enantiomer used? What about the S-isomer?
Consistent with the broader racetam SAR literature, the (R)-enantiomer demonstrates substantially greater binding affinity and behavioral efficacy than the (S)-enantiomer in AMPA receptor assays. The designation “RGPU-95” in published patent literature refers specifically to the (R)-4-(4-chlorophenyl)-2-oxopyrrolidine-1-acetamide.
Can RGPU-95 be combined with other AMPA PAMs in the same experiment?
Co-administration with other AMPA positive allosteric modulators is theoretically additive at the receptor level. In practice, combined AMPA PAM dosing carries an elevated risk of excitotoxic overstimulation at the synapse. Establish dose-response curves individually first and monitor behavioral toxicity markers.
How should tolerance be managed in chronic dosing paradigms?
The parent compound Phenylpiracetam is well-documented to show behavioral tolerance within 2–3 days of continuous daily administration. Recommended protocol: Administer for no longer than 3 consecutive weeks, followed by a minimum 7-day washout.
Why does RGPU-95 cost more per gram than Phenylpiracetam?
The synthesis of RGPU-95 requires an additional halogenation step and enantioselective purification to yield the (R)-isomer at high optical purity. However, since the effective research concentration is 2–5× lower than Phenylpiracetam, the cost-per-effective-dose is often comparable.
Research Value and Conclusion
RGPU-95 represents a strategically designed modification of the phenylpiracetam scaffold: a single halogenation that predictably increases AMPA receptor binding affinity, shifts the effective concentration range downward, and provides a pharmacologically cleaner tool for interrogating glutamatergic contributions to learning, memory, and cognitive flexibility.
RGPU-95’s value lies in precision, not volume. Its enhanced potency at the AMPA receptor, combined with its position as a structurally defined single-enantiomer compound, makes it a high-quality reference tool for research groups investigating glutamatergic modulation of cognition.
This compound is manufactured and supplied exclusively for laboratory research and analytical purposes. RGPU-95 has not been evaluated by the FDA, EMA, or any comparable regulatory authority for safety or efficacy. It is not a dietary supplement, pharmaceutical drug, or food ingredient.
The parent compound, Phenylpiracetam, is prohibited by WADA; this compound is expected to carry an analogous prohibited status in competitive sport contexts. The purchaser assumes full responsibility for compliance with all applicable local, national, and international laws and regulations governing the acquisition, possession, use, and disposal of research chemicals.
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Previous batches :
2310EURO.923C_RGPU-95 LOT= 230913 (HNMR)
Chemical Informations
| Technical Information | |
|---|---|
| CAS Number | 213178-69-9 |
| Purity | ≥98% |
| Molecular Weight | 252.7 g/mol |
| 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 | 10824736 |
| SMILES Notation | C1(C(CN2CC(N)=O)CC2=O)=CC=C(C=C1)Cl |
| Appearance | White or off-white powder |
| Physical State | Solid |
| Solubility | – Soluble to 5 mM in Ethanol – Sparingly Soluble in Water |
| Storage Conditions | Store at room temperature or cooler, in a sealed airtight container, protected from heat, light, and humidity. |

