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

α - 7烟碱乙酰胆碱受体的变质调节剂作为针对阿尔茨海默病和精神分裂症的注意力缺陷的药物具有很好的前景，但其潜在的调节机制尚不清楚。该项目旨在确定其结合位点，并开发一种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用于正电子发射断层扫描（PET）的配体，这将有助于BNC375以及其他alpha7调制器的开发。

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.