Maximum tolerant dose and analgesic activity of PT1 peptide

Abstract

Introduction: The article presents the results of the study of the maximum tolerant dose (MTD) and the analgesic activity of peptide PT1 isolated from Alopecosa marikovskyi spider venom. PT1 is the first compound of polypeptide nature, capable of exerting a selective modulating effect on purinergic P2X3 receptors. Materials and methods: The study was conducted on 174 ICR mice. The analgesic activity of the peptide was evaluated in a thermal hypersensitivity test triggered by CFA and in a model of chemical irritation. Results and discussion: The determined MTD for the peptide PT1 when administered intravenously provides evidence to attribute it to low-toxic compounds. The maximum analgesic activity of PT1 using the biomodel of hypersensitivity induced by CFA when tested 15 minutes after the administration was recorded at doses of 0.1 and 0.5 mg/kg. In the visceral pain test, the maximum analgesic activity 15 minutes after the administration of the chemical stimulus was observed at a dose of 0.01 mg/kg. Conclusions: According to the results of testing peptide PT1, it is shown that it belongs to low-toxic compounds, has a pronounced analgesic activity in a wide range of doses of 0.0001–10 mg/kg.

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“…In another work, GYCAEKGIRCDDIHCCTGLKCKCNASGYNCV CRKK peptide, isolated from Alopecosa marikovskyi spider venom, was found to possess analgesic activity by influencing purinergic P2X3 receptors. The maximum bioactivity of the peptide, studied by thermal hypersensitivity test, was 0.5 mg.kg -1 when administered intravenously (Palikova et al 2019). ZRCCNGGCSSRWCRDHSRCC peptide (SIIIA) and similar structures are expected to be potent blocking agents of TTX-R and TTX-S sodium channels (Bulaj et al 2005;Green et al 2007).…”