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. 2016 Mar 13;7(5):482-6.
doi: 10.1021/acsmedchemlett.5b00499. eCollection 2016 May 12.

Autoradiographic Evaluation of [(18)F]FECUMI-101, a High Affinity 5-HT1AR Ligand in Human Brain

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Autoradiographic Evaluation of [(18)F]FECUMI-101, a High Affinity 5-HT1AR Ligand in Human Brain

J S Dileep Kumar et al. ACS Med Chem Lett. .
Free PMC article

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.

Keywords: 5-HT1AR; PET; autoradiography; hippocampus; radiotracer; α1R.

Conflict of interest statement

The authors declare no competing financial interest.

Figures

Figure 1
Figure 1
Chemical structure of [18F]FECUMI-101.
Figure 2
Figure 2
Regional distribution of [18F]FECUMI-101 in post-mortem human brain sections at 37 °C.
Figure 3
Figure 3
In vitro selectivity of [18F]FECUMI-101 in slide mounted post-mortem human brain sections at 37 °C.
Figure 4
Figure 4
Autoradiograms of [18F]FECUMI-101 in human brain sections at 37 °C. (A) Total binding of [18F]FECUMI-101. (B) Displacement with 1 μM WAY100635. (C) Displacement with 1 μM prazosin.
Figure 5
Figure 5
Binding of [18F]FECUMI-101 in post-mortem human brain tissues at 37 °C and room temperature.

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