Methods for Assessing the Anxiolytic Activity of Derivatives of the Synthetic Active Substance 1,3,4-Oxadiazole

Anxiolytic Climbing plus maze test Open space test ladder (ladder) test Social isolation test Kick test 3R In Silico in vitro in vivo

Authors

  • S. A. Sultanov Basic doctoral student at the Institute of Chemistry of Plant Substances named after Academician S.Y. Yunusov, Assistant Professor, Department of Pharmacology, and Tashkent State Medical University
  • Z. I. Sanoev PhD, Associate Professor, Department of Pharmacology, Tashkent State Medical University
November 30, 2025

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We created a class of 1,2,4-oxadiazole derivatives with mGlu4 receptor positive allosteric modulatory activity in consideration of the allosteric modulation of mGlu receptors for possible therapeutic uses. The elevated plus-maze (EPM) and the light-dark box test, which gauge an animal's preference for open vs closed areas, are two in vivo animal models used to evaluate the anxiolytic effect of 1,3,4-oxadiazole derivatives. Increased time spent in the light compartment of the light-dark box or entries into the open arms of the plus-maze are indicators of anxiolytic activity in these tests. Other popular techniques include using in vitro binding assays to look for interactions with receptors like the GABA-A receptor and assessing the effect on anticonvulsant models like the pentylenetetrazole (PTZ) and maximal electroshock (MES) tests, since anxiolytic and anticonvulsant effects can be related. The present study synthesized novel 1,3,4-thiadiazole derivatives and examined their antinociceptive effects on nervous system nociceptive pathways. Tail-clip, hot-plate, and acetic acid-induced writhing tests were used to assess these compounds' responses to mechanical, thermal, and chemical stimuli, respectively. Additionally, an activity cage was used to measure the animals' locomotor activity. Compounds 3b, 3c, 3d, 3e, 3g, and 3h were shown to have centrally mediated antinociceptive activity by increasing mice's reaction times in both the hot-plate and tail-clip tests. Furthermore, the treatment of compounds 3a, 3c, 3e, and 3f significantly reduced the amount of writhing behaviors, indicating that these four compounds elicited peripherally mediated antinociceptive activity. Compounds 3a, 3c, and 3f considerably reduced the mice's horizontal and vertical locomotor activity, according to the activity cage tests. These three substances may exhibit non-specific antinociceptive behavior due to potential sedative effects or motor limitations.

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