• Article

A novel nicotinic acetylcholine receptor antagonist radioligand for PET studies


Ding, Y. S., Kil, K., Lin, K. S., Ma, W., Yokota, Y., & Carroll, F. (2006). A novel nicotinic acetylcholine receptor antagonist radioligand for PET studies. Bioorganic and Medicinal Chemistry Letters, 16(4), 1049-1053. DOI: 10.1016/j.bmcl.2005.10.075


Using positron emission tomography (PET) with a specific and selective radioligand targeting nicotinic acetylcholine receptor (nAChR) would allow us to better understand various nAChR related CNS disorders. The use of radiolabeled nAChR antagonists would provide a much safer pharmacological profile, avoiding most peripheral side effects that might be generated from radiolabeled nAChR agonists even at the tracer level; thus, PET imaging with nAChR antagonists would facilitate clinical application. A potent and selective nAChR antagonist was labeled and characterized with PET in non-human primates. Its high brain uptake, high signal-to-noise ratio, and high specific binding strongly suggest a great potential to carry out imaging studies in humans. In addition, the use of a C-11 radiotracer would allow us to perform multiple PET studies in the same individual within a short time frame. The presence of an iodine atom in the molecule also allows the possibility to label with radioiodine for SPECT studies.