Experimental Substantiation of the Use of Phenibut Combinations with Salicylic, Nicotinic, and Glutamic Acids in Cerebral Ischemia.

Abstract

BACKGROUND:

One of the possible ways to increase the effectiveness of drugs based on gamma-aminobutyric acid derivatives is to introduce biologically active acids into their structure. In this regard, the compositions of phenibut with organic acids, which have a more pronounced psychotropic activity, low toxicity, and good tolerability, are of interest. The purpose of this study is to experimentally substantiate the use of phenibut combinations with organic acids in various forms of cerebral ischemia.

METHODS:

The study was performed on 1210 male Wistar rats weighing 180-220 g each. The cerebroprotective activities of phenibut combinations with salicylic acid (2:1, doses of 15, 30, and 45 mg/kg), nicotinic acid (2:1, doses of 25, 50, and 75 mg/kg), and glutamic acid (2:1, doses of 25, 50, and 75 mg/kg) have been studied. The study involved a single prophylactic administration of phenibut combinations with organic acids and a 7 days course of the combination treatment administered at doses that proved the most effective according to the results of a single prophylactic administration. The rate of local cerebral blood flow and the vasodilating function of cerebral endothelium were measured, and the researchers evaluated the effects of the studied phenibut combinations on biochemical parameters in rats with focal ischemia.

RESULTS:

Compositions of phenibut with salicylic, nicotinic, and glutamic acids in subtotal and transient cerebral ischemia were found to have the most pronounced cerebroprotective effect in doses of 30, 50 and 50 mg/kg, respectively. Under reversible 10 min occlusion of the common carotid arteries, prophylactic administration of the studied phenibut compositions prevented a decrease in cerebral blood flow during ischemia and reduced the severity of postischemic hypoperfusion and hyperperfusion. At a course of 7 days of therapeutic administration of compounds, their pronounced cerebroprotective effect was observed.

CONCLUSIONS:

The data obtained can be considered as promising the pharmacological search in this series of substances for the treatment of patients with cerebrovascular disease.

• Authors: Dimitar Monov, Olga Pashanova
• Journal: Neurocritical care (Neurocrit Care) Vol. 39 Issue 2 Pg. 464-477 (10 2023) ISSN: 1556-0961 [Electronic] United States
• PMID: 37100977 (Publication Type: Journal Article)
• Copyright: © 2023. Springer Science+Business Media, LLC, part of Springer Nature and Neurocritical Care Society.

Chemical References

• 4-amino-3-phenylbutyric acid
• gamma-Aminobutyric Acid
• Glutamic Acid

Topics

• Humans
• Rats
• Male
• Animals
• Rats, Wistar
• Brain Ischemia (drug therapy)
• gamma-Aminobutyric Acid (chemistry, pharmacology)
• Cerebral Infarction
• Glutamic Acid