Synthesis and pre-clinical evaluation of a potential radiotracer for PET imaging of the dopamine D3 receptor
作者： Megan N. Stewart , Xia Shao , Timothy J. Desmond , Taylor J. Forrest , Janna Arteaga
DOI: 10.1039/C8MD00094H
关键词: Chemistry 、 Receptor 、 Radiosynthesis 、 Biophysics 、 Positron emission tomography 、 Preclinical imaging 、 Ligand (biochemistry) 、 Ex vivo 、 Dopamine receptor D2 、 Dopamine receptor D3
摘要: There is considerable interest in using positron emission tomography (PET) imaging to understand the function of dopamine D3 receptors. Due high sequence homology with D2 receptors, development D3-selective PET radiotracers has been challenging. In an effort overcome this issue, we report radiosynthesis a new selective ligand carbon-11 ([11C]1), and its initial preclincial evaluation as potential radiotracer for vivo [11C]1 was prepared via [11C]CO2 fixation 0.1% non-corrected radiochemical yield, good purity (>95%) specific activity (>2000 Ci mmol−1). exhibited binding receptors ex autoradiography experiments rat brain, but only 14-fold selectivity over which lower than 1400-fold value reported previously cell studies. Rodent revealed reasonable uptake areas brain known be rich
rsc.org
sci-hub.se 参考文章(45)
J SOVAGO, Positron emission tomographic evaluation of the putative dopamine-D3 receptor ligand, [11C]RGH-1756 in the monkey brain Neurochemistry International. ,vol. 45, pp. 609- 617 ,(2004) , 10.1016/J.NEUINT.2004.04.004
Jean-Martin Beaulieu, Stefano Espinoza, Raul R Gainetdinov, Dopamine receptors – IUPHAR Review 13 British Journal of Pharmacology. ,vol. 172, pp. 1- 23 ,(2015) , 10.1111/BPH.12906
Jogeshwar Mukherjee, Cristian C. Constantinescu, Angela T. Hoang, Taleen Jerjian, Divya Majji, Min-Liang Pan, Dopamine D3 receptor binding of (18)F-fallypride: Evaluation using in vitro and in vivo PET imaging studies. Synapse. ,vol. 69, pp. 577- 591 ,(2015) , 10.1002/SYN.21867
Chiara Bianca Maria Platania, Salvatore Salomone, Gian Marco Leggio, Filippo Drago, Claudio Bucolo, Homology Modeling of Dopamine D2 and D3 Receptors: Molecular Dynamics Refinement and Docking Evaluation PLoS ONE. ,vol. 7, pp. e44316- 12 ,(2012) , 10.1371/JOURNAL.PONE.0044316
Pierre Sokoloff, Bruno Giros, Marie-Pascale Martres, Marie-Louise Bouthenet, Jean-Charles Schwartz, Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. Nature. ,vol. 347, pp. 146- 151 ,(1990) , 10.1038/347146A0
A. Schotte, P. F. M. Janssen, P. Bonaventure, J. E. Leysen, Endogenous dopamine limits the binding of antipsychotic drugs to D3 receptors in the rat brain: a quantitative autoradiographic study. Histochemical Journal. ,vol. 28, pp. 791- 799 ,(1996) , 10.1007/BF02272152
Håkan Hall, Göran Sedvall, Olle Magnusson, Jutta Kopp, Christer Halldin, Lars Farde, Distribution of D1- and D2-dopamine receptors, and dopamine and its metabolites in the human brain. Neuropsychopharmacology. ,vol. 11, pp. 245- 256 ,(1994) , 10.1038/SJ.NPP.1380111
Natascha Nebel, Simone Maschauer, Amelie L. Bartuschat, Stefanie K. Fehler, Harald Hübner, Peter Gmeiner, Torsten Kuwert, Markus R. Heinrich, Olaf Prante, Carsten Hocke, Synthesis and evaluation of fluoro substituted pyridinylcarboxamides and their phenylazo analogues for potential dopamine D3 receptor PET imaging. Bioorganic & Medicinal Chemistry Letters. ,vol. 24, pp. 5399- 5403 ,(2014) , 10.1016/J.BMCL.2014.10.043
Marie-Louise Bouthenet, Evelyne Souil, Marie-Pascale Martres, Pierre Sokoloff, Bruno Giros, Jean-Charles Schwartz, Localization of dopamine D3 receptor mRNA in the rat brain using in situ hybridization histochemistry: comparison with dopamine D2 receptor mRNA. Brain Research. ,vol. 564, pp. 203- 219 ,(1991) , 10.1016/0006-8993(91)91456-B
Montford F. Piercey, Erika L. Walker, D.L. Feldpausch, Marlene Camacho-Ochoa, High affinity binding for pramipexole, a dopamine D3 receptor ligand, in rat striatum Neuroscience Letters. ,vol. 219, pp. 138- 140 ,(1996) , 10.1016/S0304-3940(96)90002-6