Total synthesis and evaluation of [18F] MHMZ

被引：29

作者：

Herth, Matthias M. ^{[1
]}

Debus, Fabian ^{[2
]}

Piel, Markus ^{[1
]}

Palner, Mikael ^{[3
]}

Knudsen, Gitte M. ^{[3
]}

Lueddens, Hartmut ^{[2
]}

Roesch, Frank ^{[1
]}

机构：

[1] Johannes Gutenberg Univ Mainz, Inst Nucl Chem, D-55128 Mainz, Germany

[2] Clin Res Grp, Dept Psychiat, D-55131 Mainz, Germany

[3] Rigshosp, Ctr Integrated Mol Brain Imaging, DK-2100 Copenhagen, Denmark

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 04期

关键词：

F-18] MHMZ; MDL; 100907; F-18] altanserin; 5-HT2A; antagonist; positron emission tomography; autoradiography;

D O I：

10.1016/j.bmcl.2007.12.054

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Radiochemical labeling of MDL 105725 using the secondary labeling precursor 2-[F-18] fluoroethyltosylate ([F-18] FETos) was carried out in yields of similar to 90% synthesizing [F-18] MHMZ in a specific activity of similar to 50 MBq/ nmol with a starting activity of similar to 3 GBq. Overall radiochemical yield including [F-18] FETos synthon synthesis, [F-18] fluoroalkylation and preparing the injectable [ 18 F] MHMZ solution was 42% within a synthesis time of similar to 100 min. The novel compound showed excellent specific binding to the 5-HT2A receptor (K-i = 9.0 nM) in vitro and promising in vivo characteristics. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：1515 / 1519

页数：5

共 50 条

[1] Synthesis and initial biological evaluation of [18F] fluorotryptophans ([18F]FTrps)
Zlatopolskiy, B. D.
Zischler, J.
Endepols, H.
Guliyev, M.
Shaefer, D.
Urusova, E. A.
Neumaier, B.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2017, 44 : S381 - S381
[2] SYNTHESIS OF [18F]FLUOROMETHYLSPIPERONE ([18F]FMSP) VIA [18F]FLUOROMETHYL TRIFLATE SYNTHESIS
Kim, H. W.
Jeong, J. M.
Lee, H. J.
Chung, K. H.
Oh, C. H.
Cho, J-H
Lee, D. S.
Chung, J-K
Lee, M. C.
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2005, 48 : S231 - S231
[3] Development of automatic synthesis system and basic evaluation of [18F]FBPA synthesis from [18F]HF ([18F-]).
Kanai, Y.
Watanabe, T.
Hattori, Y.
Ohta, Y.
Naka, S.
Sakai, T.
Ono, K.
Kirihata, M.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2024, 51 : S817 - S817
[4] Quantification of 5HT2A-Receptors in the Human Brain with [18F]MHMZ
Kramer, V.
Herth, M.
Hernandez, E.
Juri, C.
Pruzzo, R.
Roesch, F.
Amaral, H.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2015, 42 : S545 - S546
[5] Synthesis and evaluation of Androgen Receptor radioligand [18F]enzalutamide: comparison with [18F]FDHT
Antunes, I. F.
Dost, R.
van Waarde, A.
Dierckx, R.
Samplonius, D.
Helfrich, W.
Burg, D.
de Vries, E.
de Jong, I.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2015, 42 : S260 - S261
[6] A robotic synthesis of [18F]fluoromisonidazole ([18F]FMISO)
Chang, C. W.
Chou, T. K.
Liu, R. S.
Wang, S. J.
Lin, W. J.
Chen, C. H.
Wang, H. E.
APPLIED RADIATION AND ISOTOPES, 2007, 65 (06) : 682 - 686
[7] Synthesis and evaluation of the Estrogen Receptor β selective radioligand [18F]FHNP: comparison with [18F]FES
Antunes, I. Farinha
van Waarde, A.
Dierckx, R. A. J. O.
de Vries, E. G. E.
Hospers, G. A. P.
Vries, E. F. J. de
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2014, 41 : S273 - S274
[8] Synthesis and Pre-clinical Evaluation of (S)-[18F]Fluoro Hydroxybutyrate ([18F]FHB)
Horikawa, Mami
Witek, Jason
Brooks, Allen
Sanford, Melanie
Scott, Peter
JOURNAL OF NUCLEAR MEDICINE, 2024, 65
[9] Automated synthesis of [18F]Raltegravir through [18F]fluorobenzylamine
Blecha, Joseph
Neumann, Kiel
VanBrocklin, Henry
JOURNAL OF NUCLEAR MEDICINE, 2018, 59
[10] Synthesis and initial biological evaluation of 7-[18F]fluorotryptophan (7-[18F]FTrp)
Zlatopolskiy, Boris D.
Zischler, Johannes
Endepols, Heike
Guliyev, Mehrab
Schaefer, Dominique
Urusova, Elizaveta
Neumaier, Bernd
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2017, 60 : S415 - S415

← 1 2 3 4 5 →