Pharmacological probes to facilitate preclinical development of modulators of a6 subunit containing nicotinic acetylcholine receptors

促进含烟碱乙酰胆碱受体的 a6 亚基调节剂临床前开发的药理学探针

• 批准号: LP140100781
• 负责人: Prof Thomas Balle
• 金额: $ 17.48万
• 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: 2015
• 资助国家: 澳大利亚
• 起止时间: 2015-01-01 至 2017-10-30
• 项目状态: 已结题
• 来源: https://dataportal.arc.gov.au/RGS/Web/Grants/LP140100781
• 关键词: Pharmacological; probes; facilitate; preclinical; development

Allosteric modulators of alpha7 nicotinic acetylcholine receptors have a promising future as drugs targeting attention deficits in Alzheimer’s disease and schizophrenia but the mechanisms underlying modulation are poorly understood. This project aims to determine its binding site and develop a radioactive labelled compound that competes with its binding. The radiolabelled compound and a deeper insight into the mode of action will enable development of ligands for positron emission tomography (PET) which will aid in the development of BNC375 as well as other alpha7 modulators.

α7 烟碱乙酰胆碱受体的变构调节剂作为治疗阿尔茨海默病和精神分裂症注意力缺陷的药物具有广阔的前景，但其调节机制尚不清楚。该项目旨在确定其结合位点并开发与其结合竞争的放射性标记化合物。放射性标记化合物和对作用模式的更深入了解将有助于开发正电子发射断层扫描 (PET) 配体，这将有助于 BNC375 以及其他 α7 调节剂的开发。