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<p>Early studies have shown that extrarenal clearance of the studied GABA derivatives phenibut and mefebut was many times higher than renal clearance, indicating the prevalence of biotransformation processes of the studied compounds. The biotransformation prognosis suggests the formation of 8 metabolites for mefebut and 12 metabolites for phenibut. According to the prognosis, these GABA derivatives may be products of each other’s biotransformation. The studies have shown that no chromatographic peaks that could be identified as phenibut were detected in the analysis of blood plasma and brain samples after administration of mefebut at a dose of 25 mg/kg. If phenibut was present in these samples, its concentrations were low and below the detection limit of the analytical method. According to an <i>in silico</i> prognosis, most possible mefebut metabolites retained the methoxy group, despite other metabolic transformations of the original molecule. Phenibut is more susceptible to biotransformation processes. It can form two conjugates with glucuronic acid and one with sulfuric acid. Such metabolites have low lipophilicity and are quickly eliminated from the body.</p>

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Possible Biotransformation Pathways of GABA Derivatives Mefebut and Phenibut

  • 期刊论文

  • 发表日期：

    2025年10月1日

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  • L. A. Smirnova,
  • I. N. Tyurenkov,
  • D. A. Bakulin,
  • M. S. Zatyamina,
  • B. V. Kozlovskiy,
  • D. D. Samarkin

摘要

Early studies have shown that extrarenal clearance of the studied GABA derivatives phenibut and mefebut was many times higher than renal clearance, indicating the prevalence of biotransformation processes of the studied compounds. The biotransformation prognosis suggests the formation of 8 metabolites for mefebut and 12 metabolites for phenibut. According to the prognosis, these GABA derivatives may be products of each other’s biotransformation. The studies have shown that no chromatographic peaks that could be identified as phenibut were detected in the analysis of blood plasma and brain samples after administration of mefebut at a dose of 25 mg/kg. If phenibut was present in these samples, its concentrations were low and below the detection limit of the analytical method. According to an in silico prognosis, most possible mefebut metabolites retained the methoxy group, despite other metabolic transformations of the original molecule. Phenibut is more susceptible to biotransformation processes. It can form two conjugates with glucuronic acid and one with sulfuric acid. Such metabolites have low lipophilicity and are quickly eliminated from the body.