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Fluorescent tools for the imaging of dopamine D2-like receptors

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Item Type:Article
Title:Fluorescent tools for the imaging of dopamine D2-like receptors
Creators Name:Nagl, M. and Moennich, D. and Rosier, N. and Schihada, H. and Sirbu, A. and Konar, N. and Reyes-Resina, I. and Navarro, G. and Franco, R. and Kolb, P. and Annibale, P. and Pockes, S.
Abstract:The family of dopamine D2-like receptors represent an interesting target for a variety of neurological diseases, e.g. Parkinson's disease (PD), addiction or schizophrenia. In this study we describe the synthesis of a new set of fluorescent ligands as tools for visualization of dopamine D2-like receptors. Pharmacological characterization in radioligand binding studies identified UR-MN212 (20) as a high-affinity ligand for D2-like receptors (pKi (D2longR) = 8.24, pKi (D3R) = 8.58, pKi (D4R) = 7.78) with decent selectivity towards D1-like receptors. Compound 20 is a neutral antagonist in a Go1 activation assay at the D2longR, D3R and D4R, which is an important feature for studies using whole cells. The neutral antagonist 20, equipped with a 5-TAMRA dye, displayed rapid association to the D2longR in binding studies using confocal microscopy demonstrating its suitability for fluorescence microscopy. Furthermore, in molecular brightness studies, the ligand's binding affinity could be determined in a single-digit nanomolar range that was in good agreement with radioligand binding data. Therefore, the fluorescent compound can be used for quantitative characterization of native D2-like receptors in a broad variety of experimental setups.
Keywords:Dopamine Receptors, Fluorescent Ligands, D(2)-Like Receptors, Confocal Microscopy, Molecular Brightness
Page Range:e202300659
Date:15 January 2024
Official Publication:https://doi.org/10.1002/cbic.202300659
PubMed:View item in PubMed

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