Phenylpiracetam

Uses

A few small clinical studies have shown possible links between prescription of phenylpiracetam and improvement in a number of encephalopathic conditions, including lesions of cerebral blood pathways, traumatic brain injury and certain types of glioma.

Phenylpiracetam reverses the depressant effects of the benzodiazepine diazepam, increases operant behavior, inhibits post-rotational nystagmus, prevents retrograde amnesia, and has anticonvulsant properties.

Phenylpiracetam is typically prescribed as a general stimulant or to increase tolerance to extreme temperatures and stress.

Phenylpiracetam has been researched for the treatment of Parkinson's disease.

Animal Model Research

In Wistar rats with gravitational cerebral ischemia, Phenylpiracetam reduced the extent of neuralgic deficiency manifestations, retained the locomotor, research, and memory functions, increased the survival rate, and lead to the favoring of local cerebral flow restoration upon the occlusion of carotid arteries to a greater extent than did piracetam.

Operant behavior

Phenylpiracetam is known to increase operant behavior. In tests against a control, Sprague-Dawley rats given free access to less-preferred rat chow and trained to operate a lever repeatedly to obtain preferred rat chow performed additional work when given methylphenidate, d-amphetamine, and phenylpiracetam. Rats given 1 mg/kg amphetamine performed an average of 150% as much work and consumed 50% as much non-preferred rat chow than control rats; rats given 10 mg/kg Methylphenidate performed 170% as much work and consumed similarly; and rats given 100 mg/kg Phenylpiracetam performed an average of 375% as much work, and consumed little non-preferred rat chow.

Present data show that (R)-phenylpiracetam increases motivation, i.e., the work load, which animals are willing to perform to obtain more rewarding food. At the same time consumption of freely available normal food does not increase. Generally this indicates that (R)-phenylpiracetam increase motivation [...] The effect of (R)-phenylpiracetam is much stronger than that of methylphenidate and amphetamine.

Pharmacology

Phenylpiracetam binds to α4β2 nicotinic acetylcholine receptors in the mouse brain cortex with IC50 = 5.86 μM.

In rats, scopolamine is used to model memory impairment. It impairs performance in the conditioned passive avoidance reflex test, increases cortical nACh and hippocampal NMDA receptor densities, and decreases striatal D₁ and cortical benzodiazepine receptor densities. Phenylpiracetam demonstrates antiamnestic activity by restoring performance in the passive avoidance test and partially reversing each of these scopolamine-induced receptor density changes.

Experiments performed on Sprague-Dawley rats in a European patent for using Phenylpiracetam to treat sleep disorders showed an increase in extracellular dopamine levels after administration. The patent asserts discovery of phenypiracetam's action as a dopamine reuptake inhibitor as its basis.

The peculiarity of this invention compared to former treatment approaches for treating sleep disorders is the so far unknown therapeutic efficacy of (R)-phenylpiracetam, which is presumably based at least in part on the newly identified activity of (R)-phenylpiracetam as the dopamine re-uptake inhibitor

Phenylpiracetam may also act as a noradrenaline reuptake inhibitor, making it an NDRI.

Availability

While not prescribed as a pharmaceutical in the West, in Russia it is available as a prescription medicine under the name Phenotropil (but most drugstores sell it without prescriptions).

Phenylpiracetam is not scheduled by the DEA in the U.S.

Athlete doping

Because it increases physical stamina and provides improved tolerance to cold weather, it appears on the lists of stimulants banned for in-competition use by the World Anti-Doping Agency. This list is applicable in all Olympic sports.