E. D. Goldberg Research Institute of Pharmacology and Regenerative Medicine, Tomsk National Research Medical Center, Russian Academy of Sciences, Tomsk, Russia.
Institute of Problems of Chemical and Energetic Technologies, Siberian Division of the Russian Academy of Sciences, Biysk, Russia.
Bull Exp Biol Med. 2022 Dec;174(2):230-235. doi: 10.1007/s10517-023-05679-4. Epub 2023 Jan 4.
Analysis of specific pharmacological activity evaluated high antinociceptive efficacy of the first synthesized compound 10-di(ethoxyacetyl)-2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo[5,5,0,0,0]dodecane (ethowurtzine) in models of somatogenic pain of different genesis (thermal, visceral pain, mechanical compression of paw).The new molecule from the class of hexaazaisowurtzitane effectively blocks nociceptive reactions at the supraspinal and peripheral levels of pain sensitivity organization. The effect of ethowurtzine was comparable or exceeded the effect of tramadol. The obtained results prove the possibility of creating new pharmacologically active molecules based on the high-energy substance hexaazaisowurtzitane.
分析特定的药理活性评价第一个合成化合物 10-二(乙氧羰基)-2,6,8,12-四乙酰基-2,4,6,8,10,12-六氮杂十六烷(乙氧哇嗪)在不同发病机制(热、内脏痛、爪子机械压迫)躯体痛觉模型中的高抗伤害效能。该新分子属于六氮杂异哇嗪类,能有效阻断痛觉感受组织的脊髓上和外周水平的伤害性反应。乙氧哇嗪的作用可与曲马多的作用相媲美或超过其作用。所得结果证明了基于高能物质六氮杂异哇嗪来创制新型药理活性分子的可能性。