Volgograd Journal of Medical Research
Quarterly Journal of Science and Practice

UDK: 615.214.2:547.466.3

Anxiolytic activity of optical isomers of 3-substituted 4- (1N-tetrazol-1-YL) butanoic acids

N. S. Kovalev, D. A. Bakulin, L. A. Sablina, M. Yu. Vorontsov, A. S. Bykova, A. N. Reznikov, Yu. N. Klimochkin

Волгоградский государственный медицинский университет, России, Научный центр инновационных лекарственных средств; Самарский государственный технический университет, Россия, кафедра органической химии


Racemate of 3-para-tolyl-substituted GABA (tolibut) has neuroprotective, analgesic, muscle relaxant, anti-anxiety and anticonvulsant effects. The clinical application of tolibut is limited by a narrow therapeutic range. One of the ways to reduce its toxicity can be the approach of modifying the structure of GABA, in particular, replacing the amino group with a tetrazole fragment. The tetrazolyl substituent can be used as a bioisosteric analogue of various functional groups. The aim of this work is to study the anxiolytic activity of tetrazolyl derivatives of GABA with tolyl and phenyl radicals in the be- ta position. The study was performed on Wistar rats. The anxiolytic action of the (R)- and (S)-enantiomers of 3-aryl- substituted 4-(1H-tetrazol-1-yl) butanoic acids was evaluated. According to the results of the study, the presence of an- xiolytic activity in the (R) -isomer of 3-(4-methylphenyl) -4-(1H-tetrazol-1-yl) butanoic acid in a conflict situation was noted, comparable to that in tolibut and phenibut.


GABA, tolibut, phenibut, enantiomers, anxiolytic activity, rats