S-phenylpiracetam, a selective DAT inhibitor, reduces body weight gain without influencing locomotor activity

Summary: The study found that S-phenylpiracetam, a selective dopamine transporter inhibitor, significantly decreased body weight gain, fat mass, and plasma glucose and leptin levels in both obese Zucker rats and Western diet-fed mice, without affecting their locomotor activity. These results suggest that S-phenylpiracetam could be a promising treatment for obesity in patients with metabolic syndrome, potentially offering fewer side effects compared to other weight-loss drugs.

Link: ScienceDirect

New synthesis of β-aryl-GABA drugs

Summary: Researchers have developed a new method to synthesize β-aryl-GABA drugs using a novel cascade radical reaction to create key intermediates, such as unsaturated β-aryl-γ-lactams. This approach not only simplifies the production process but also allows for the creation of drugs like rolipram, phenylpiracetam, and its hydrazide form.

Link: ScienceDirect

Neuroprotective and anti-inflammatory activity of DAT inhibitor R-phenylpiracetam in experimental models of inflammation in male mice

Summary: R-phenylpiracetam (R-PhP) was found to have neuroprotective and anti-inflammatory effects in male mice by interacting with the dopamine transporter (DAT). The study showed that R-PhP reduced inflammation and nociceptive responses in various tests, indicating its potential as a therapeutic agent targeting the dopaminergic system.

Link: Latvian Institute of Organic Synthesis

Stereochemistry of phenylpiracetam and its methyl derivative: improvement of the pharmacological profile

Summary: This study reviews the latest decade of research on two specific compounds, (R)-phenylpiracetam and E1R, derived from piracetam, which have shown potential in improving memory and cognitive functions. It highlights the importance of the molecular configuration in determining their biological effectiveness, supporting the need for purifying drugs to isolate the most effective stereoisomers.

Link: Latvian Institute of Organic Synthesis

Single Enantiomer’s Urge to Crystallize in Centrosymmetric Space Groups: Solid Solutions of Phenylpiracetam

Summary: This study analyzed the thermochemical and structural properties of phenylpiracetam enantiomers, discovering two polymorphs, enant-A and enant-B, and noting their ability to form solid solutions due to structural factors. Findings revealed that these polymorphs crystallize in different space groups and the structures exhibit quasi centrosymmetry, explaining the absence of enantioselectivity in the solid state.

Link: Max Planck Institute for Dynamics of Complex Technical Systems

On the formation of phenylpiracetam solid solutions: thermodynamic and structural considerations

Summary: This study discovered two rare types of solid solutions formed by the drug phenylpiracetam, called 𝛼 and 𝛽, with distinct properties and temperatures at which they transition between forms. 𝛼 is fully miscible in the solid state, while 𝛽 is only partially miscible near its pure enantiomer composition above the transition temperature, and the research delves into the structural reasons behind these formations.

Link: University of Latvia