| Literature DB >> 27190597 |
J S Dileep Kumar1, Mark D Underwood2, Norman R Simpson3, Suham A Kassir3, Jaya Prabhakaran4, Vattoly J Majo4, Mihran J Bakalian3, Ramin V Parsey5, J John Mann2, Victoria Arango2.
Abstract
[(18)F]FECUMI-101 ([(18)F]1) is a 5HT1AR ligand demonstrating specific binding in brain regions corresponding to the distribution of 5-HT1AR in baboons. However, we detected moderate uptake of [(18)F]1 in baboon thalamus, a brain region lacking 5-HT1AR. We sought to investigate the relative binding of [(18)F]1 to 5-HT1AR, α1R, and 5-HT7R in vitro. Using autoradiography in human brain sections, specific binding of [(18)F]1 to 5-HT1AR was confirmed. However, [(18)F]1 also showed 26% binding to α1R in PFC. The hippocampal formation exhibited 51% and 92% binding of [(18)F]1 to α1R and 5-HT1AR, respectively. Thalamus and cerebellum showed very little binding. There is no measurable specific binding of [(18)F]1 to 5-HT7R and no effect of temperature on [(18)F]1 specific binding to 5-HT1AR or α1R. These results indicate that, while [(18)F]FECUMI-101 is not a completely selective 5-HT1AR ligand for receptor quantification, it may be useful for occupancy measurements of drugs acting at 5-HT1AR in vivo.Entities:
Keywords: 5-HT1AR; PET; autoradiography; hippocampus; radiotracer; α1R
Year: 2016 PMID： 27190597 PMCID： PMC4867482 DOI： 10.1021/acsmedchemlett.5b00499
Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345