UDK: 615.214.2:547.466.3:616-092.4

COMPARISON OF THE NEURO PSYCHOTROPIC PROPERTIES OF THE (R)-ISOMER AND THE RACEMIC FORM OF THE TOLIBUT

N.S. Kovalev1, D.A. Bakulin3, D.V. Kurkin3, V.E. Pustynnikov1, A.N. Reznikov2, Yu.N. Klimochkin2

1ФГБОУ ВО «Волгоградский государственный медицинский университет» Минздрава России, кафедра фармакологии и фармации ИНМФО; 2ФГБОУ ВО «Самарский государственный технический университет», кафедра органической химии; 3Научный центр инновационных лекарственны

Abstract

The use of biologically active enantiomers instead of racemic forms is currently a promising approach to improving the properties of known drugs. In such derivatives of GABA as phenibut and baclofen, the pharmacological activity is determined by the (R)-isomer. The potential for the possible clinical use of tolibut is limited by a narrow spectrum of therapeutic action. One of the ways to expand it may be the approach of isolating and studying the active enantiomer. The sedative, anxiolytic, nootropic, antihypoxic effects, as well as the toxicity of the (R)-isomer and racemate of tolibut were evaluated. The performed study showed that the (R)-isomer of tolibut has a more pronounced muscle relaxant, antihypoxic effect, exhibits less pronounced anxiolytic activity and less toxicity compared to racemate.

Keywords

GABA, tolibut, enantiomers, anxiolytic activity, rats.

Contacts

Бакулин Дмитрий Александрович – к. м. н., доцент кафедры клинической фармакологии и интенсивной терапии, Волгоградский государственный медицинский университет, e-mail: mbfdoc@gmail.com