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[123I]-4-(2-(bis(4-fluorophenyl)methoxy)ethyl)-1-(4-iodobenzyl)piperidine

Development stage
Preclinical
Lead developer
Ghent University
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[123I]-4-(2-(bis(4-fluorophenyl)methoxy)ethyl)-1-(4-iodobenzyl)piperidine is a small molecule **radioligand** developed as a **selective dopamine transporter (DAT) imaging agent** for in vivo neuroimaging with SPECT (Single Photon Emission Computed Tomography)[1]. This compound exhibits **high nanomolar affinity for the dopamine transporter** and has greater selectivity over other monoamine transporters (serotonin and norepinephrine transporters) than certain established alternatives such as [123I]-FP-CIT and [123I]-PE2I. Despite favorable in vitro DAT selectivity, in vivo evaluation in rodents indicated behavior as a substrate for the P-glycoprotein (P-gp) efflux transporter and a **brain uptake/distribution pattern not correlating well with DAT distribution**, limiting its suitability for DAT mapping. However, the tracer may serve for in vivo imaging related to P-glycoprotein function[1]. Mechanistically, [123I]-4-(2-(bis(4-fluorophenyl)methoxy)ethyl)-1-(4-iodobenzyl)piperidine functions as a radiolabelled substrate for the dopamine transporter and p-glycoprotein.

Other names
[123I]-7
02

Targets

DAT (Dopamine plasma membrane transport protein)ABCB1 (P-glycoprotein)

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