Study Into Antinociceptive Activity of a New Molecule from the Class of Hexaazaizowurzitane

E. A. Kiseleva, S. Krylova, T. N. Povet`eva, Y. Nesterova, O. G. Afanas`eva, P. V. Kul`pin, D. A. Kulagina, E. Zueva, N. Suslov, V. V. Eremina, O. Baibakova, S. Sysolyatin, V. V. Zhdanov
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Abstract

In this work, we studied the pharmacological activity of a newly-synthesized compound 4-(3,4- dibromothiophenylcarbonyl)-10-(2-ethoxyacetyl)-2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,0,03,11,05,9]dodecane (M3) using somatogenic pain models of various genesis (thermal and visceral pain, mechanical compression of a paw). The compound showed a high antinociceptive efficacy, comparable to or exceeding that of tramadol. It was shown that the new molecule from the class of hexaazaisowurtzitane effectively blocks nociceptive reactions at the supraspinal and peripheral levels of pain sensitivity organization. The results obtained confirm the possibility of creating new pharmacologically active molecules based on the high-energy substance of hexaazaisowurtzitane, which is a priority in domestic pharmaceutical production.
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六氮杂唑脲酮类新分子抗伤性的研究
在这项工作中,我们研究了新合成的化合物4-(3,4-二溴噻吩羰基)-10-(2-乙氧基乙酰基)-2,6,8,12-四乙酰基-2,4,6,8,10,12-六氮杂四环[5,5,0,03,11,05,9]十二烷(M3)的药理活性,并利用不同原因的体源性疼痛模型(热痛和内脏痛,机械压迫爪子)。该化合物显示出很高的抗伤感受力,与曲马多相当或超过曲马多。结果表明,六氮杂索乌兹坦类的新分子有效地阻断了疼痛敏感组织的棘上和外周水平的伤害性反应。研究结果证实了以六氮杂索乌尔齐坦的高能物质为基础制备新型药理活性分子的可能性,这是国内制药生产的重点。
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