Pharmacokinetics

The pharmacokinetics of phenylpiracetam in humans are unpublished. In contrast to piracetam and most other racetams however, phenylpiracetam contains β-phenylethylamine within its chemical structure and hence can additionally be conceptualized as a substituted phenethylamine.

Phenylpiracetam is a racemic mixture of (R)- and (S)-enantiomers, (R)-phenylpiracetam (MRZ-9547) and (S)-phenylpiracetam. Cebaracetam (CGS-25248; ZY-15119) is a derivative of RGPU-95 in which the terminal amide has been replaced with a 2-piperazinone moiety.

Methylphenylpiracetam, including all four of its stereoisomers (especially the (4R,5S)-enantiomer E1R), is a positive allosteric modulator of the sigma σ<sub>1</sub> receptor. It is currently the only known racetam demonstrating σ<sub>1</sub> receptor modulation.

Other derivatives of phenylpiracetam have also been developed and studied. Subsequently, it became available as a prescription drug in Russia. It was approved in 2003 for treatment of various conditions.

Manufacturer

Phenylpiracetam is manufactured by the pharmaceutical companies Valenta Pharm and Pharmstandard (Pharmstandart) in Russia. As a result, it is on the list of stimulants banned for in-competition use by the World Anti-Doping Agency (WADA). However, no recent development has been reported.