Engineered extrasynaptic GABAA receptors: Towards novel analgesics

工程化突触外 GABAA 受体：迈向新型镇痛药

• 批准号: LP160100560
• 负责人: Prof Thomas Balle
• 金额: $ 36.43万
• 依托单位: The University of Sydney
• 依托单位国家: 澳大利亚
• 项目类别: Linkage Projects
• 财政年份: 2017
• 资助国家: 澳大利亚
• 起止时间: 2017-05-01 至 2020-12-31
• 项目状态: 已结题
• 来源: https://dataportal.arc.gov.au/RGS/Web/Grants/LP160100560
• 关键词: Engineered; extrasynaptic; GABAA; receptors; Towards

Engineered extrasynaptic GABAA receptors: Towards novel analgesics. This project intends to alleviate neuropathic pain by developing drugs and good tool molecules targeting GABA-A receptors. About 20% of Australian adults suffer from neuropathic pain. Delta-containing GABA-A receptors represent attractive and novel targets for developing non-opioid analgesics. However, no drugs or good tool molecules target these receptors. This project intends to develop the needed enabling technologies, including screening assays, tool molecules and radioligands; and perform brain slice electrophysiology to confirm activity in neuronal cells. This project is expected to benefit the research community and future rational drug-discovery endeavours for drugs that modulate delta-containing receptors.

工程突触外GABAA受体：迈向新型镇痛药。本项目旨在通过开发靶向GABA-A受体的药物和良好的工具分子来缓解神经性疼痛。大约20%的澳大利亚成年人患有神经性疼痛。含有δ的GABA-A受体是开发非阿片类镇痛药的新靶点。然而，没有药物或好的工具分子靶向这些受体。该项目旨在开发所需的支持技术，包括筛选分析、工具分子和放射性配体；并进行脑切片电生理学来确认神经元细胞的活动。该项目预计将有利于研究界和未来合理的药物发现工作，以调节含delta受体的药物。