title: Comparison of Nootropic and Neuroprotective Features of Aryl-Substituted Analogs of Gamma-Aminobutyric Acid.
abstract: 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.
authors.affiliation: Volgograd State Medical University, Volgograd, Russia.
authors.forename: I N
authors.initials: IN
authors.lastname: Tyurenkov
authors.affiliation: Volgograd State Medical University, Volgograd, Russia.
authors.forename: L E
authors.initials: LE
authors.lastname: Borodkina
authors.affiliation: Volgograd State Medical University, Volgograd, Russia. vvbagmetova@gmail.ru.
authors.forename: V V
authors.initials: VV
authors.lastname: Bagmetova
authors.affiliation: A. I. Herzen State Pedagogical University of Russia, St. Petersburg, Russia.
authors.forename: V M
authors.initials: VM
authors.lastname: Berestovitskaya
authors.affiliation: A. I. Herzen State Pedagogical University of Russia, St. Petersburg, Russia.
authors.forename: O S
authors.initials: OS
authors.lastname: Vasil'eva
mesh_terms: D000647:Amnesia / Q000139:chemically induced / Q000188:drug therapy*; D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology; D001362:Avoidance Learning / Q000187:drug effects*; D001418:Baclofen / Q000494:pharmacology; D002934:Cinnamates / Q000494:pharmacology; D003128:Coma / Q000188:drug therapy*; D004597:Electroshock / Q000009:adverse effects; D008297:Male; D018696:Neuroprotective Agents / Q000494:pharmacology*; D018697:Nootropic Agents / Q000494:pharmacology*; D051381:Rats; D012601:Scopolamine; D005680:gamma-Aminobutyric Acid / Q000031:analogs & derivatives* / Q000494:pharmacology*
chemical_list: D000927:Anticonvulsants; D002934:Cinnamates; D018696:Neuroprotective Agents; D018697:Nootropic Agents; C051791:tolibut; D005680:gamma-Aminobutyric Acid; D012601:Scopolamine; D001418:Baclofen; C008842:4-amino-3-phenylbutyric acid
keywords: GABA; baclofen; nootropic and neuroprotective properties; phenibut; tolibut