Anxiolytic activity of optical isomers of 3-substituted 4- (1n-tetrazol-1-yl) butanoic acids

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 beta 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 anxiolytic 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.