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Fluorescent tools for the imaging of dopamine D2-like receptors
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dc.contributor.author | Nagl, Martin | |
dc.contributor.author | Mönnich, Denise | |
dc.contributor.author | Rosier, Niklas | |
dc.contributor.author | Schihada, Hannes | |
dc.contributor.author | Sirbu, Alexei | |
dc.contributor.author | Konar, Nergis | |
dc.contributor.author | Reyes-Resina, Irene | |
dc.contributor.author | Navarro, Gemma | |
dc.contributor.author | Franco, Rafael | |
dc.contributor.author | Kolb, Peter | |
dc.contributor.author | Annibale, Paolo | |
dc.contributor.author | Pockes, Steffen | |
dc.date.accessioned | 2023-11-21T11:30:01Z | |
dc.date.available | 2023-11-21T11:30:01Z | |
dc.date.issued | 2023-11-20 | |
dc.identifier | 296368073 | |
dc.identifier | 1e463ec9-377a-4357-9e4f-866e8bbd1cc8 | |
dc.identifier | 85177226793 | |
dc.identifier.citation | Nagl , M , Mönnich , D , Rosier , N , Schihada , H , Sirbu , A , Konar , N , Reyes-Resina , I , Navarro , G , Franco , R , Kolb , P , Annibale , P & Pockes , S 2023 , ' Fluorescent tools for the imaging of dopamine D 2 -like receptors ' , ChemBioChem , vol. Early View , e202300659 . https://doi.org/10.1002/cbic.202300659 | en |
dc.identifier.issn | 1439-7633 | |
dc.identifier.other | RIS: urn:30BF0BFD16728BCAA6EAFE9064B3795C | |
dc.identifier.other | ORCID: /0000-0003-3208-5347/work/146964128 | |
dc.identifier.uri | https://hdl.handle.net/10023/28737 | |
dc.description | Funding: S.P. was supported by the Fonds der Chemischen Industrie (No. 661688) and the University of Regensburg (Academic Research Sabbatical Program). Financial support by the graduate school “Receptor Dynamics: Emerging Paradigms for Novel Drugs (K-BM-2013-247)” of the Elite Network of Bavaria (ENB) for S.P., N.R., M.N. and H.S. is gratefully acknowledged. We would like to thank the Deutsche Forschungsgemeinschaft (DFG) for support through project 421152132 SFB1423 subproject C03 (P.A.) and SFB 1470 subproject A01 (P.A.). R.F., as PI, was funded by Spanish MCIN/AEI/10.13039/501100011033 (grant PID2021-126600OB-I00) and by the European Union Next Generation EU/PRTR (ERDF A way of making Europe). Open Access funding enabled and organized by Projekt DEAL. | en |
dc.description.abstract | The family of dopamine D2-like receptors represents 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. | |
dc.format.extent | 15 | |
dc.format.extent | 5952738 | |
dc.language.iso | eng | |
dc.relation.ispartof | ChemBioChem | en |
dc.subject | Confocal microscopy | en |
dc.subject | D2-like receptors | en |
dc.subject | Dopamine receptors | en |
dc.subject | Fluorescent ligands | en |
dc.subject | Molecular brightness | en |
dc.subject | QC Physics | en |
dc.subject | NDAS | en |
dc.subject.lcc | QC | en |
dc.title | Fluorescent tools for the imaging of dopamine D2-like receptors | en |
dc.type | Journal article | en |
dc.contributor.institution | University of St Andrews. School of Physics and Astronomy | en |
dc.identifier.doi | https://doi.org/10.1002/cbic.202300659 | |
dc.description.status | Peer reviewed | en |
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