Comparison of Nootropic and Neuroprotective Features of Aryl-Substituted Analogs of Gamma-Aminobutyric Acid

Bull Exp Biol Med. 2016 Feb;160(4):465-9. doi: 10.1007/s10517-016-3198-4. Epub 2016 Feb 23.


GABA analogs containing phenyl (phenibut) or para-chlorophenyl (baclofen) substituents demonstrated nootropic activity in a dose of 20 mg/kg: they improved passive avoidance conditioning, decelerated its natural extinction, and exerted antiamnestic effect on the models of amnesia provoked by scopolamine or electroshock. Tolyl-containing GABA analog (tolibut, 20 mg/kg) exhibited antiamnestic activity only on the model of electroshock-induced amnesia. Baclofen and, to a lesser extent, tolibut alleviated seizures provoked by electroshock, i.e. both agents exerted anticonvulsant effect. All examined GABA aryl derivatives demonstrated neuroprotective properties on the maximum electroshock model: they shortened the duration of coma and shortened the period of spontaneous motor activity recovery. In addition, these agents decreased the severity of passive avoidance amnesia and behavioral deficit in the open field test in rats exposed to electroshock. The greatest neuroprotective properties were exhibited by phenyl-containing GABA analog phenibut.

Keywords: GABA; baclofen; nootropic and neuroprotective properties; phenibut; tolibut.

MeSH terms

  • Amnesia / chemically induced
  • Amnesia / drug therapy*
  • Animals
  • Anticonvulsants / pharmacology
  • Avoidance Learning / drug effects*
  • Baclofen / pharmacology
  • Cinnamates / pharmacology
  • Coma / drug therapy*
  • Electroshock / adverse effects
  • Male
  • Neuroprotective Agents / pharmacology*
  • Nootropic Agents / pharmacology*
  • Rats
  • Scopolamine
  • gamma-Aminobutyric Acid / analogs & derivatives*
  • gamma-Aminobutyric Acid / pharmacology*


  • Anticonvulsants
  • Cinnamates
  • Neuroprotective Agents
  • Nootropic Agents
  • tolibut
  • gamma-Aminobutyric Acid
  • Scopolamine
  • Baclofen
  • 4-amino-3-phenylbutyric acid