Investigations of painmechanism related to ATP receptors aiming at new analgesics for cancer pain

ATP受体相关疼痛机制研究，寻找新型癌痛镇痛药

• 批准号: 22591756
• 负责人: SATA Takeyoshi
• 金额: $ 2.83万
• 依托单位: University of Occupational and Environmental Health, Japan
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 2010
• 资助国家: 日本
• 起止时间: 2010 至 2012
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-22591756/
• 关键词: 疹痛管理学; ATP受容体; P2X7受容体; サブユニット選択的作用; 神経障害性疼痛; 疼痛発現機構; 新たな鎮痛薬開発; P2X_4受容体; P2X_7受容体; 鎮痛薬; 癌性疼痛; 全身麻酔薬; P2X受容体; アフリカツメガエル卵母細胞発現系

We investigated the effects of several analgesics on many subtypes of ATP receptors, and revealed that local anesthetics, lidocaine inhibited the function of P2×7,0ne of the ATP receptor subtypes. We demonstrated that this effect happen through direct effect of lidocaine on P2×_7 receptor, and is non-competitive inhibition. These results suggest that inhibition of P2×_7 function by lidocaine is one of the mechanisnls of analgesic effects by lidocaine for cancer pain, which are still unknown, and indicate the possibility of development of new analgesics for cancer pain by further research about this mechanism.

本文研究了几种镇痛药对多种ATP受体亚型的作用，发现局麻药利多卡因可抑制ATP受体亚型的P2× 7.0ne功能。利多卡因的这种作用是通过直接作用于P_2 ×_7受体而实现的，且为非竞争性抑制。提示利多卡因抑制P2×_7功能是其镇痛作用机制之一，但其机制尚不清楚。进一步研究利多卡因的镇痛机制，有可能开发新的癌痛镇痛药。