Talk:RGPU-95
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Summary sheet: RGPU-95 |
RGPU-95 | |||||||||||||||||||||||||||
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Chemical Nomenclature | |||||||||||||||||||||||||||
Common names | RGPU-95, p-Cl-Phenylpiracetam | ||||||||||||||||||||||||||
Substitutive name | p-Cl-Phenylpiracetam | ||||||||||||||||||||||||||
Systematic name | (R,S)-2-(2-oxo-4-(4-chlorophenyl)-pyrrolidin-1-yl)acetamide | ||||||||||||||||||||||||||
Class Membership | |||||||||||||||||||||||||||
Psychoactive class | Nootropic / Stimulant | ||||||||||||||||||||||||||
Chemical class | Racetam | ||||||||||||||||||||||||||
Routes of Administration | |||||||||||||||||||||||||||
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RGPU-95 (also known as p-Cl-Phenylpiracetam) is a central nervous system stimulant and nootropic agent belonging to the racetam family of drugs. It is a derivative of phenylpiracetam and by extension piracetam, research into its properties and efficacy in humans is limited.
RGPU-95 is available and sold through online vendors as a research chemical in the United States. Dosages are commonly reported to be around a tenth of those pertaining to phenylpiracetam, making it more potent while offering comparable benefit.
Chemistry
RGPU-95 is based on the phenylpiracetam molecular skeleton with an additional chlorine attached to the phenyl group. Due to the chiral center at the fourth position of the pyrrolidinone ring, it can exist in an S or R-isomer; the clinically used form is the racemic mixture.[1]
RGPU-95 technically conforms to the structural framework of a substituted phenethylamine, albeit two of the substituents are part of the pyrrolidone ring. It does have monoamine-associated effects.
Pharmacology
This pharmacology section is incomplete. You can help by adding to it. |
RGPU-95 is shown to be around five to ten times more potent than phenylpiracetam. Information pertaining to its parent compound can be applied to RGPU-95 for the most part due to its similarity. In terms of its pharmacokinetics, it is thought to be similar to phenylpiracetam.
Animal studies show a half-life of 2.5-3 hours for phenylpiracetam doses of 100mg/kg and RGPU-95 is thought to exhibit a similar, or slightly longer timeframe of action.
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.
In animals models of cognitive disorders, administering RGPU-95 at doses ranging from 0.05 to 0.2 mg/kg resulted in slight to moderate improvements in cognitive performance, memory enhancement, antidepressant, anxiolytic, antipsychotic, and analeptic effects. Within this dosage range, RGPU-95 exhibits mild mood-elevating properties and promotes wakefulness, similar to the effects observed with phenylpiracetam at doses ranging from 0.5 to 2 mg/kg.
As RGPU-95 (p-Cl-Phenylpiracetam) was developed to be a stronger derivative of phenylpiracetam, and considering the limited available data on the effects of RGPU-95, information focusing on the effects of Phenylpiracetam is provided below.
As with other racetams, phenylpiracetam is thought to increase acetylcholine release within hippocampal cells.[2] Similarly, RGPU-95 is thought to share these attributes, but with greater potency. As acetycholine is involved in the function of memory, this could potentially account for its reported nootropic effects.
Phenylpiracetam has protected against scopolamine-induced amnesia both in rat populations, suggesting it can aid recovery from deliriant intoxication and other typically cognitively impaired states by preserving adequate levels of acetylcholine as a primary mechanism.[3]
Many people report that phenylpiracetam effects (especially stimulation) are more pronounced than other racetams. That may be due to the fact that phenylpiracetam is an NDRI. Specifically, both enantiomers of phenylpiracetam are dopamine reuptake inhibitors.[4][5] The R enantiomer is also a weak noradrenaline reuptake inhibitor (thus, an NDRI) with 11-fold lower affinity to NET than to DAT, while the S enantiomer has no such effect. Accordingly, the R enantiomer causes locomotor stimulation while the S does not.[5] A confounding factor in this reasoning is that both phenylpiracetam and piracetam are reported to increase dopamine and noradrenaline concentrations.[3]
Phenylpiracetam appears to have a series of trials conducted on it[6][2] showing improvement in cognition in persons with cognitive decline from organic causes, with one study noting a minor improvement in cognition in those with youth epilepsy.[7]
Subjective effects
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
In comparison to the effects of other nootropics such as noopept, this compound can be described as focusing primarily on cognitive focus over that of cognitive stimulation. RGPU-95 demonstrates more prominent anxiolytic, antidepressant, and cognitive-enhancing effects compared to its parent compound phenylpiracetam.
Physical effects
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- Stimulation - The stimulation which RGPU-95 presents in common doses can be considered more prominent that that of phenylpiracetam, in heavy doses it can be uncomfortably overstimulating.
- Increased heart rate - This may be a result of the dopamine and noradrenaline reuptake inhibition.
- Stamina enhancement - This effect is relatively mild compared to other stimulants such as amphetamine.
- Headaches - This is more prominent at higher doses. It can be promoted by redosing multiple times. This is likely attributed to a depletion of choline.
- Appetite suppression[citation needed]
Sensory effects
- Although these effects are not universal, certain people may experience sensory enhancements under the influence of this compound.
Cognitive effects
-
In terms of its cognitive effects, this compound can be described as stimulating, more so than phenylpiracetam.
- Analysis enhancement
- Wakefulness
- Mindfulness
- Anxiety suppression
- Thought connectivity
- Focus enhancement
- Motivation enhancement
- Memory enhancement
- Dream potentiation
- Irritability
- Cognitive dysphoria - This effect typically only occurs at extremely high dosages.
After effects
Experience reports
Anecdotal reports which describe the effects of its parent compound phenylpiracetam within our experience index include:
Additional experience reports can be found here:
Toxicity and harm potential
Several studies suggest that this substance is safe even when high doses are consumed for a long period of time[8] although it is worth noting that the exact toxic dosage is unknown. Anecdotal evidence from those within the community who have tried phenylpiracetam suggest that there do not seem to be any negative health effects attributed to simply trying this drug at low to moderate doses by itself and using it sparingly (but nothing can be completely guaranteed).
It is strongly recommended that one use harm reduction practices when using this drug.
Lethal dosage
The median lethal dosage (LD50) of RGPU-95 has not been officially published as it has low abuse potential, but is not known to be harmful when exceeding the recommended dosage range.
Tolerance and addiction potential
The chronic use of RGPU-95 can be considered as non-addictive with a low potential for abuse. It does not seem to be capable of causing psychological dependence among users, although this fact has not been corroborated by clinical studies. Tolerance to many of the effects of RGPU-95 develops with prolonged and repeated use. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). RGPU-95 may present cross-tolerance with all racetam nootropics, meaning that after the consumption of RGPU-95 certain nootropics such as phenylpiracetam, aniracetam and piracetam may have a reduced effect.
Legal status
This legality section is a stub. As such, it may contain incomplete or wrong information. You can help by expanding it. |
RGPU-95, being a member of the racetam family, currently is legally available to buy and sell in most countries, but may still vary by region.
- United Kingdom - It is illegal to produce, supply, or import this drug under the Psychoactive Substance Act, which came into effect on May 26th, 2016.[9]
See also
External links
References
- ↑ Zvejniece, L., Svalbe, B., Veinberg, G., Grinberga, S., Vorona, M., Kalvinsh, I., Dambrova, M. (November 2011). "Investigation into stereoselective pharmacological activity of phenotropil". Basic & Clinical Pharmacology & Toxicology. 109 (5): 407–412. doi:10.1111/j.1742-7843.2011.00742.x. ISSN 1742-7843.
- ↑ 2.0 2.1 Savchenko, A. I., Zakharova, N. S., Stepanov, I. N. (2005). "[The phenotropil treatment of the consequences of brain organic lesions]". Zhurnal Nevrologii I Psikhiatrii Imeni S.S. Korsakova. 105 (12): 22–26. ISSN 1997-7298.
- ↑ 3.0 3.1 Firstova, Yu. Yu., Abaimov, D. A., Kapitsa, I. G., Voronina, T. A., Kovalev, G. I. (1 June 2011). "The effects of scopolamine and the nootropic drug phenotropil on rat brain neurotransmitter receptors during testing of the conditioned passive avoidance task". Neurochemical Journal. 5 (2): 115–125. doi:10.1134/S1819712411020048. ISSN 1819-7132.
- ↑ Zvejniece, L; Zvejniece, B; Videja, M; Stelfa, G; Vavers, E; Grinberga, S; Svalbe, B; Dambrova, M (October 2020). "Neuroprotective and anti-inflammatory activity of DAT inhibitor R-phenylpiracetam in experimental models of inflammation in male mice". Inflammopharmacology. 28 (5): 1283–1292. doi:10.1007/s10787-020-00705-7. PMID 32279140.
- ↑ 5.0 5.1 Zvejniece, L; Svalbe, B; Vavers, E; Makrecka-Kuka, M; Makarova, E; Liepins, V; Kalvinsh, I; Liepinsh, E; Dambrova, M (September 2017). "S-phenylpiracetam, a selective DAT inhibitor, reduces body weight gain without influencing locomotor activity". Pharmacology, biochemistry, and behavior. 160: 21–29. doi:10.1016/j.pbb.2017.07.009. PMID 28743458.
- ↑ Gustov, A. A., Smirnov, A. A., Korshunova, I. A., Andrianova, E. V. (2006). "[Phenotropil in the treatment of vascular encephalopathy]". Zhurnal Nevrologii I Psikhiatrii Imeni S.S. Korsakova. 106 (3): 52–53. ISSN 1997-7298.
- ↑ Lybzikova, G. N., Iaglova, Z. S., Kharlamova, I. S. (2008). "[The efficacy of phenotropil in the complex treatment of epilepsy]". Zhurnal Nevrologii I Psikhiatrii Imeni S.S. Korsakova. 108 (2): 69–70. ISSN 1997-7298.
- ↑ Malykh, A. G., Sadaie, M. R. (1 February 2010). "Piracetam and Piracetam-Like Drugs". Drugs. 70 (3): 287–312. doi:10.2165/11319230-000000000-00000. ISSN 1179-1950.
- ↑ Psychoactive Substances Act 2016