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

[21] Evaluation of 5-[18F] fluoro-2′-deoxycytidine as a tumor imaging agent: A comparison of [18F]FdUrd, [18F]FLT and [18F]FDG
Yu, Hung-Man
Chiu, Ching-Hung
Chen, Wei-Ting
Wu, Chi-Han
Lin, Pei-Yao
Huang, Ya-Yao
Chen, Jyun-Hong
Tzen, Kai-Yuan
Shiue, Chyng-Yann
Lin, Wuu-Jyh
APPLIED RADIATION AND ISOTOPES, 2019, 148 : 152 - 159
[22] Synthesis and evaluation of 4-[18F] fluoropropoxy-3-iodobenzylguanidine ([18F]FPOIBG): A novel 18F-labeled analogue of MIBG
Vaidyanathan, Ganesan
McDougald, Darryl
Koumarianou, Eftychia
Choi, Jaeyeon
Hens, Marc
Zalutsky, Michael R.
NUCLEAR MEDICINE AND BIOLOGY, 2015, 42 (08) : 673 - 684
[23] Gas Phase Synthesis of [18F]Fluoroform from NCA [18F]Fluoromethane
Yang, Bo Yeun
Haskali, Mohammad B.
Telu, Sanjay
Morse, Cheryl L.
Pike, Victor W.
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2017, 60 : S263 - S263
[24] Automated synthesis of 18F analogue of paclitaxel (PAC):: [18F]Paclitaxel (FPAC)
Kalen, Joseph D.
Hirsch, Jerry I.
Kurdziel, Karen A.
Eckelman, William C.
Kiesewetter, Dale O.
APPLIED RADIATION AND ISOTOPES, 2007, 65 (06) : 696 - 700
[25] Evaluation of Different Ranges of [18F]Fluoride for Production of [18F]F-FAPI-74
Morisco, A.
Maisto, C.
de Marino, R.
D'Ambrosio, L.
Squame, E.
Recchimuzzo, M. Buonanno
Esposito, A.
Aurilio, M.
Gaballo, P.
Lastoria, S.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2023, 50 (SUPPL 1) : S756 - S757
[26] Microfluidic synthesis of [18F]FLT
Akula, Murthy
Collier, Thomas
Kabalka, George
Wall, Jonathan
Kennel, Steve
Stuckey, Alan
LeBlanc, Amy
JOURNAL OF NUCLEAR MEDICINE, 2010, 51
[27] Rapid and efficient synthesis of [18F]fluoronicotinamides, [18F]fluoroisonicotinamides and [18F]fluorobenzamides as potential pet radiopharmaceuticals for melanoma imaging
Al Jammaz, I.
Al-Otaibi, B.
Okarvi, S.
Amartey, J.
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2011, 54 (06): : 312 - 317
[28] Automated synthesis and PET evaluation of both enantiomers of [18F]FMISO
Revunov, Evgeny
Jorgensen, Jesper T.
Jensen, Andreas Ingemann
Hansen, Anders E.
Severin, Gregory W.
Kjaer, Andreas
Zhuravlev, Fedor
NUCLEAR MEDICINE AND BIOLOGY, 2015, 42 (04) : 413 - 419
[29] Tritium in [18O]water containing [18F]fluoride for [18F]FDG synthesis
Ito, S
Saze, T
Sakane, H
Ito, S
Ito, S
Nishizawa, K
APPLIED RADIATION AND ISOTOPES, 2004, 61 (06) : 1179 - 1183
[30] Synthesis and application of [18F]fluorobenziodoxole
Gonzalez, Miguel Cortes
Nordeman, Patrik
Gomez, Antonio Bermejo
Meyer, Denise
Antoni, Gunnar
Schou, Magnus
Szabo, Kalman
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2019, 62 : S160 - S161

← 1 2 3 4 5 →