Laboratory of Neuroreceptors and Neuroregulators, Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow, Russia.
Ann Neurol. 2010 May;67(5):680-3. doi: 10.1002/ana.21949.
P2X3 purinoreceptors expressed in mammalian sensory neurons play a key role in several processes, including pain perception. From the venom of the Central Asian spider Geolycosa sp., we have isolated a novel peptide, named purotoxin-1 (PT1), which is to our knowledge the first natural molecule exerting powerful and selective inhibitory action on P2X3 receptors. PT1 dramatically slows down the removal of desensitization of these receptors. The peptide demonstrates potent antinociceptive properties in animal models of inflammatory pain.
在哺乳动物感觉神经元中表达的 P2X3 嘌呤能受体在包括痛觉感知在内的多种过程中发挥关键作用。从中亚地区蜘蛛 Geolycosa sp 的毒液中，我们分离出一种新型肽，命名为 purotoxin-1（PT1），据我们所知，它是第一个对 P2X3 受体产生强大和选择性抑制作用的天然分子。PT1 显著减缓这些受体脱敏的消除。该肽在炎症性疼痛的动物模型中表现出强大的镇痛特性。
