GSK-215083 is a PET radioligand for the 5-HT6 receptor. GSK 215083 is tested for the treatment of Alzheimer's disease, and coupled with 11C, as a PET ligand for identification of occupancy of the 5HT6 receptor. GSK 215083 is a quinoline based compounds that acts by antagonising the 5-HT6 receptor. Preclinical studies conducted of the ligand indicated that it binds to receptors 5-hydroxytrypamine-6 (5HT6) in the striatum and 5-hydroxytryptamine-2A (5HT2A) in the frontal cortex. References: Parker CA, Rabiner EA, Gunn RN, Searle G, Martarello L, Comley RA, Davy M, Wilson AA, Houle S, Mizrahi R, Laruelle M, Cunningham VJ. Human Kinetic Modeling of the 5HT6 PET Radioligand 11C-GSK215083 and Its Utility for Determining Occupancy at Both 5HT6 and 5HT2A Receptors by SB742457 as a Potential Therapeutic Mechanism of Action in Alzheimer Disease. J Nucl Med. 2015 Dec;56(12):1901-9. doi: 10.2967/jnumed.115.162743. Epub 2015 Sep 17. PubMed PMID: 26383152.

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CAS：607742-80-3