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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SKU: RGPU95-XG-PW Categories: Glutamatergics, Ampakines, Nootropic Powders

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Description
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Chemical Informations

Description

🔬 Research Chemical · For Laboratory Use Only

RGPU-95 (p-Cl-Phenylpiracetam) – Powder

At a Glance

Compound

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.

Mechanism of Interest

Positive allosteric modulator (PAM) of AMPA-type glutamate receptors; reported to also interact with nicotinic acetylcholine receptors (nAChR). Demonstrates higher binding affinity than the parent compound, Phenylpiracetam, in preclinical models.

Primary Research Applications

Glutamatergic modulation studies, AMPA receptor PAM pharmacology, structure-activity relationship (SAR) research within the racetam class, cognitive and neuroplasticity models, comparative potency benchmarking.

Regulatory Status

Not FDA-approved. Not authorized for human or veterinary use. Phenylpiracetam (parent compound) 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.

⚠️ Regulatory Note: 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.

AMPA Receptor Positive Allosteric Modulation

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

Nicotinic Acetylcholine Receptor Interaction

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

Monoaminergic / Stimulant-Adjacent Properties

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. All findings should be considered within that evidential context.

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

Compounds with Complementary Mechanisms

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.

Co-administration Requiring Caution or Avoidance

⚠️ 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. This information pertains strictly to laboratory animal model observations
and in vitro assessments.

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.

Research Use Restrictions

🚫
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.
This halogenation increases the electron-withdrawing character of the phenyl ring, which is
associated with improved binding affinity at AMPA receptor allosteric sites.

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.
This translates to a lower effective concentration range in both in vivo and in vitro assays —
making it a more potent tool compound for receptor occupancy studies where precise dose-effect
relationships are critical.

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 (S)-isomer is not inactive, but its potency is markedly lower and its
receptor selectivity profile less clean.

The designation “RGPU-95” in published patent literature refers specifically to the
(R)-4-(4-chlorophenyl)-2-oxopyrrolidine-1-acetamide — the biologically active
isomer. Researchers should confirm stereochemical purity of their source material using
chiral HPLC or optical rotation measurements if enantiomeric ratio is critical to their study design.

Can RGPU-95 be combined with other AMPA PAMs in the same experiment?

Co-administration with other AMPA positive allosteric modulators (e.g., aniracetam, noopept,
CX-series AMPAkines) is theoretically additive at the receptor level. In practice, combined
AMPA PAM dosing carries an elevated risk of excitotoxic overstimulation at the synapse —
particularly in models involving NMDA receptor co-activation or elevated baseline glutamate
release.

If combination studies are required, establish the dose-response curve for RGPU-95 alone
before introducing a second agent. Use behavioral toxicity markers (stereotypy, seizure
activity, elevated corticosterone) as safety endpoints, and reduce individual doses
proportionally when combining agents at the same receptor class.

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 — one of the most rapid tolerance
profiles in the racetam class. Although RGPU-95-specific repeat-dose data are limited,
the structural similarity strongly predicts a comparable pattern.

Recommended protocol: Administer for no longer than 3 consecutive weeks,
followed by a minimum 7-day washout. Assess primary behavioral endpoints at days 1, 7,
and 14 to document tolerance trajectory. Include a drug-naive control group throughout
the washout period to distinguish residual drug effects from genuine recovery of baseline
performance.

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. Both steps reduce batch
yield and require specialized reagents and quality control verification (chiral HPLC,
optical rotation).

However, since the effective research concentration is 2–5× lower than Phenylpiracetam,
the cost-per-effective-dose is often comparable. For experiments requiring
precise receptor occupancy control at low concentrations — where Phenylpiracetam’s effective
dose range produces confounding locomotor effects — RGPU-95’s higher potency represents
genuine scientific value rather than simply a premium price point.

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.

Key Research Principle: 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 — particularly in the context
of racetam SAR studies where dose-effect precision is paramount.

⚠️ Important Legal & Regulatory Disclaimer

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.

By acquiring this compound, you confirm that you are an authorized researcher
operating within an approved institutional or commercial research setting, and that this
material will be used solely for legitimate scientific investigation.

Lab Analysis

View full report

COA_RGPU-95_2024-08-08

Previous batches :

CoA_RGPU-95_2024-02-21

2310EURO.923C_RGPU-95 LOT= 230913 (HNMR)

23-EMA-1_P01_CoA_m0_RGPU-95 LOT : 230913

2209EURO.764G_RGPU-95 CAS=213178-69-9 LOT=120722 (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.

RGPU-95

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