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PRL-8-53 – 0.5g powder

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CAS: 51352-88-6
IUPAC name: Methyl 3-[2-[benzyl(methyl)amino]ethyl]benzoate

Description
PRL-8-53 – 0.5g powder

PRL-8-53 is a research chemical derived from phenylmethylamine and benzoic acid with a chemical formula of C18H21NO2. It was synthesized in the 1970s and most of the research was conducted in the 1970s. It is a nootropic compound with the studies showing properties of improving cognition and memory (Hansl and Mead, 1978).

 

Mechanism of Action

In an earlier study scientists argued that its structure helps to interact with cholinergic receptors producing a cholinergic response in model animals. The structure of the compound helps to interact with cholinergic receptors. They function in the transduction of signals in the somatic and autonomic nervous systems, a system that controls the homeostatic environment of the body (Carlson & Kraus, 2021).

The compound potentiates dopamine which is thought to be a reason for a possible shift in the balance of neurotransmitters resulting in improved memory and cognitive function. (Hansl, 1973). Dopamine is a chemical messenger that plays an important role in the ability to think, focus, motivation, and pleasure (Schultz, 2007).

PRL-8-53 belongs to the cholinergic family of nootropic compounds. Researchers believed that the enhanced integrity of neuronal membranes involves phospholipid metabolism by such compounds (Wignall & Brown, 2014). In another article, scientists argued about effect of such cholinergic compounds to enhance memory in neurodegenerative diseases (Spiers & Hochanadel, 1999)

 

Animal studies

In an early study, at the dose of 4mg/Kg, apomorphine-induced gnawing was increased, and conditioned avoidance learning was improved in rats which indicates its function as a dopamine agonist. For each set of experiments 12-20 animals were used and conditioned avoidance learning was improved statically significant.  It was also observed that PRL-8-53 also reversed catatonia and ptosis by reserpine-induced mechanism (Hansl, 1974b).

 

Human studies

There is only one study involving humans as test subjects. In this double-blind placebo study, 47 healthy individuals were selected who were either given a 5mg dosage of PRL-8-53 or placebo, 2-2.5 hours before performing a task. To determine the effect, a verbal test of word recall was presented in an audio form to individuals. After 24 hours and then 4 days, they were instructed to write all words they can recall, preferably in a correct sequence within 5 minutes. The whole population of subjects under study were divided into subgroups according to their achievement to recall the words.

Results of this study indicated that administering 5mg of PRL-8-53 showed an improvement in acquisition and retention score which was indicated as a partial restoration of intellect, increased cognition, and improved memory. Statical analysis showed only slight significance on the acquisition, but retention improvement was quite significant with an 87-105% increase in this factor, after 24-h and 1-week retention. The group of high achievers did not show much improvement, but other sub-groups did well after administering PRL-8-53. It was nearly impossible to obtain significant improvement in this group as they have started with nearly perfect control performance.

Looking at the age factor, subjects with the age of 30 years or above showed 31 percent improvement in their responses while improvement in retention scores was around 108-152 %, after administering the 5 mg of PRL-8-53. The visual reaction showed minor improvements which are statically not significant. Furthermore, a slight improvement in motor control was observed but it did not have any statistical significance as well (Hansel and Mead, 1978).

 

Toxicity studies

In an earlier animal study showed an oral dose of 860 mg/kg PRL-8-53 exhibited low toxicity in mice however, dogs have tolerated the dose of 8 mg/kg without having any effect on their blood pressure while higher doses caused a drop in blood pressure for a short duration. A dose of 20 mg/kg did not cause any d-amphetamine effect in rats (Hansl, 1974a).

No side effects/adverse reactions were reported in any of 47 volunteers recruited for the only human study (Hansel & Mead, 1978).

 

References

Carlson, A.B. and Kraus, G.P (2021) Physiology, Cholinergic Receptors. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing. Source

Hansl, N (1973). Synthesis and biological activity of m-(2-aminoalkyl)-benzoic acid derivatives, Abst. Am. Chem. Soc. Med, 57

Hansl, N (1974a). Process for hydrolyzing 3-trifluoromethyl phenethylamines. U.S. Patent 3,792,048

Hansl, N.R (1974b). A novel spasmolytic and CNS active agent 3-(2-benzylmethylamino ethyl) benzoic acid methyl ester hydrochloride, Experientia, 30, 271–272. https://doi.org/10.1007/BF01934822

Hansl, N.R. and Mead, B.T. (1978), PRL-8-53: Enhanced learning and subsequent retention in humans as a result of low oral doses of new psychotropic agent, Psychopharmacology, 56, 249-253. https://doi.org/10.1007/BF00432846

Schultz, W (2007). Multiple Dopamine Functions at Different Time Courses, Annual Review of Neuroscience, 30(1), 259-288. https://doi.org/10.1146/annurev.neuro.28.061604.135722

Spiers, P.A. and Hochanadel, G (1999). Citicoline for traumatic brain injury: report of two cases, including my own, J Int Neuropsychol Soc, 1999, 5(3), 260-4. doi: 10.1017/s1355617799533092

Suliman, N. A., Mat Taib, C. N., Mohd Moklas, M. A., Adenan, M. I., Hidayat Baharuldin, M. T., & Basir, R. (2016). Establishing Natural Nootropics: Recent Molecular Enhancement Influenced by Natural Nootropic. Evidence-based complementary and alternative medicine : eCAM, 4391375. DOI: 10.1155/2016/4391375

Wignall, N. D. and Brown, E.S (2014). Citicoline in addictive disorders: a review of the literature, Am J Drug Alcohol Abuse, 40(4), 262-8. doi: 10.3109/00952990.2014.925467

MATERIAL FACTS
CAS code: 51352-88-6
Molecular formula: C18H21NO2
Molar mass: 283.371 g/mol
IUPAC name: Methyl 3-[2-[benzyl(methyl)amino]ethyl]benzoate
Synonyms: PRL-8-53; Methyl 3-(2-(benzylmethylamino)ethyl)benzoate hydrochloride; 3-(2-(Methyl(phenylmethyl)amino)ethyl)benzoic acid methyl ester hydrochloride; 3-(2-(Methyl(phenylmethyl)amino)ethyl)benzoic acid methyl ester hydrochloride
Storage: Store in a cool and dry place. Keep away from direct sunlight, heat, moisture. Keep away from children.
Physical form: White powder

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