Current radiosynthesis strategies for 5-HT2A receptor PET tracers

被引：14
作者：
Herth, Matthias M. [1 ,2 ,3 ]
Knudsen, Gitte M. [1 ,2 ]
机构：
[1] Rigshosp, Ctr Integrated Mol Brain Imaging, DK-2100 Copenhagen, Denmark
[2] Univ Copenhagen, DK-2100 Copenhagen, Denmark
[3] Univ Copenhagen, Dept Drug Design & Pharmacol, DK-2100 Copenhagen, Denmark
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2015年 / 58卷 / 07期
关键词：
C-11]MDL 100907; F-18]MH; MZ; (R)-[F-18]MH; F-18]MDL 100907 [F-18]altanserin; F-18]deuteroaltanserin; F-18]fananserin; F-18]RP62203; C-11]Cimbi-36; PET; 5-HT2A; tracer development; POSITRON-EMISSION-TOMOGRAPHY; SEROTONIN RECEPTORS; IN-VIVO; PHARMACOLOGICAL CHARACTERIZATION; PRACTICAL SYNTHESIS; H-3; RP-62203; HUMAN BRAIN; MDL; 100907; RAT-BRAIN; BINDING;
D O I：
10.1002/jlcr.3288
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
Serotonin 2A receptors have been implicated in various psychophysiological functions and disorders such as depression, Alzheimer's disease, or schizophrenia. Therefore, neuroimaging of this specific receptor is of significant clinical interest, and it is not surprising that many attempts have been made to develop a suitable 5-HT2AR positron emission tomography-tracer. In this review, we give an overview on the precursor, reference compound synthesis, and the preparation of promising 5-HT2AR radiopharmaceuticals applied in positron emission tomography. We also highlight possible learning outcomes that can be made from these tracer development processes.
引用
收藏
页码：265 / 273
页数：9
相关论文
共 73 条
[1]   Development of central 5-HT2A receptor radioligands for PET: Comparison of [H-3]RP 62203 and [H-3]SR 46349B kinetics in rat brain [J].
Ashworth, S ;
Hume, SP ;
Lammertsma, AA ;
OpackaJuffry, J ;
Shah, F ;
Pike, VW .
NUCLEAR MEDICINE AND BIOLOGY, 1996, 23 (03) :245-250
[2]  
BARON JC, 1985, REV NEUROL-FRANCE, V141, P537
[3]   Specific in vivo binding in the rat brain of [F-18]RP 62203: A selective 5-HT2A receptor radioligand for positron emission tomography [J].
Besret, L ;
Dauphin, F ;
Huard, C ;
Lasne, MC ;
Vivet, R ;
Mickala, P ;
Barbelivien, A ;
Baron, JC .
NUCLEAR MEDICINE AND BIOLOGY, 1996, 23 (02) :169-171
[4]   [F-18]SETOPERONE - A NEW HIGH-AFFINITY LIGAND FOR POSITRON EMISSION TOMOGRAPHY STUDY OF THE SEROTONIN-2 RECEPTORS IN BABOON BRAIN INVIVO [J].
BLIN, J ;
PAPPATA, S ;
KIYOSAWA, M ;
CROUZEL, C ;
BARON, JC .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1988, 147 (01) :73-82
[5]   18F-Labeling and evaluation of novel MDL 100907 derivatives as potential 5-HT2A antagonists for molecular imaging [J].
Debus, Fabian ;
Herth, Matthias M. ;
Piel, Markus ;
Buchholz, Hans-Georg ;
Bausbacher, Nicole ;
Kramer, Vasko ;
Lueddens, Hartmut ;
Roesch, Frank .
NUCLEAR MEDICINE AND BIOLOGY, 2010, 37 (04) :487-495
[6]   PHARMACOLOGICAL CHARACTERIZATION OF RP-62203, A NOVEL 5-HYDROXYTRYPTAMINE 5-HT2 RECEPTOR ANTAGONIST [J].
DOBLE, A ;
GIRDLESTONE, D ;
PIOT, O ;
ALLAM, D ;
BETSCHART, J ;
BOIREAU, A ;
DUPUY, A ;
GUEREMY, C ;
MENAGER, J ;
ZUNDEL, JL ;
BLANCHARD, JC .
BRITISH JOURNAL OF PHARMACOLOGY, 1992, 105 (01) :27-36
[7]   Serotonin 2A receptor agonist binding in the human brain with [11C]Cimbi-36 [J].
Ettrup, Anders ;
da Cunha-Bang, Sophie ;
McMahon, Brenda ;
Lehel, Szabolcs ;
Dyssegaard, Agnete ;
Skibsted, Anine W. ;
Jorgensen, Louise M. ;
Hansen, Martin ;
Baandrup, Anders O. ;
Bache, Soren ;
Svarer, Claus ;
Kristensen, Jesper L. ;
Gillings, Nic ;
Madsen, Jacob ;
Knudsen, Gitte M. .
JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM, 2014, 34 (07) :1188-1196
[8]   Preclinical Safety Assessment of the 5-HT2A Receptor Agonist PET Radioligand [11C]Cimbi-36 [J].
Ettrup, Anders ;
Holm, Soren ;
Hansen, Martin ;
Wasim, Muhammad ;
Santini, Martin Andreas ;
Palner, Mikael ;
Madsen, Jacob ;
Svarer, Claus ;
Kristensen, Jesper Langgaard ;
Knudsen, Gitte Moos .
MOLECULAR IMAGING AND BIOLOGY, 2013, 15 (04) :376-383
[9]   Radiosynthesis and in vivo evaluation of a series of substituted 11C-phenethylamines as 5-HT2A agonist PET tracers [J].
Ettrup, Anders ;
Hansen, Martin ;
Santini, Martin A. ;
Paine, James ;
Gillings, Nic ;
Palner, Mikael ;
Lehel, Szabolcs ;
Herth, Matthias M. ;
Madsen, Jacob ;
Kristensen, Jesper ;
Begtrup, Mikael ;
Knudsen, Gitte M. .
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2011, 38 (04) :681-693
[10]   In vivo evaluation of a series of substituted 11C-phenetylamines as 5-HT2A agonist PET tracers [J].
Ettrup, Anders ;
Hansen, Martin ;
Santini, Martin A. ;
Paine, James ;
Gillings, Nic ;
Palner, Mikael ;
Lehel, Szabolcs ;
Madsen, Jacob ;
Begtrup, Mikael ;
Knudsen, Gitte M. .
NEUROIMAGE, 2010, 52 :S48-S48
12345678