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Abstract <p>It was previously shown that the original dipeptide mimetic of the 4th loop of neurotrophin-3 (NT-3) hexamethylenediamide bis-(<i>N</i>-monosuccinyl-L-asparaginyl-L-asparagine) (GTS-301), like the full-length neurotrophin, predominantly activates the tyrosine kinase receptor TrkC and has a neuroprotective effect in vitro at concentrations of 10<sup>–5</sup>–10<sup>–12</sup> M, as well as antidiabetic (0.1 and 0.5 mg/kg) and antidepressant (5 and 10 mg/kg) effects after systemic administration in rodents. In this work, the analgesic properties of GTS-301 were identified, which were manifested in the dose range of 0.01–10 mg/kg after acute intraperitoneal injection to rats in the “tail flick” test. Dipeptide GTS-301 increased the threshold of pain response by 20–30%; this effect persisted for at least 24 h after administration.</p>

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Analgesic Activity of the Low Molecular Weight Neurotrophin-3 Dipeptide Mimetic GTS-301

  • 期刊论文

  • 发表日期：

    2025年1月22日

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  • L. G. Kolik,
  • M. A. Konstantinopolsky,
  • N. M. Sazonova,
  • A. D. Durnev,
  • T. A. Gudasheva

摘要

Abstract

It was previously shown that the original dipeptide mimetic of the 4th loop of neurotrophin-3 (NT-3) hexamethylenediamide bis-(N-monosuccinyl-L-asparaginyl-L-asparagine) (GTS-301), like the full-length neurotrophin, predominantly activates the tyrosine kinase receptor TrkC and has a neuroprotective effect in vitro at concentrations of 10–5–10–12 M, as well as antidiabetic (0.1 and 0.5 mg/kg) and antidepressant (5 and 10 mg/kg) effects after systemic administration in rodents. In this work, the analgesic properties of GTS-301 were identified, which were manifested in the dose range of 0.01–10 mg/kg after acute intraperitoneal injection to rats in the “tail flick” test. Dipeptide GTS-301 increased the threshold of pain response by 20–30%; this effect persisted for at least 24 h after administration.