Total synthesis and evaluation of [18F] MHMZ

Publication type:
Journal article
Metadata:
Autoren
  • Matthias M Herth
  • Fabian Debus
  • Markus Piel
  • Mikael Palner
  • Gitte M Knudsen
  • Hartmut Lueddens
  • Frank Roesch
Autoren-URL
https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000254180000052&DestLinkType=FullRecord&DestApp=WOS_CPL
DOI
10.1016/j.bmcl.2007.12.054
eISSN
1464-3405
Externe Identifier
  • Clarivate Analytics Document Solution ID: 276YQ
  • PubMed Identifier: 18187324
ISSN
0960-894X
Ausgabe der Veröffentlichung
4
Zeitschrift
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Schlüsselwörter
  • [F-18] MHMZ
  • MDL 100907
  • [F-18] altanserin
  • 5-HT2A
  • antagonist
  • positron emission tomography
  • autoradiography
Paginierung
1515 - 1519
Datum der Veröffentlichung
2008
Status
Published
Titel
Total synthesis and evaluation of [<SUP>18</SUP>F] MHMZ
Sub types
  • Article
Ausgabe der Zeitschrift
18

Data source: Web of Science (Lite)

Other metadata sources:
Autoren
  • Matthias M Herth
  • Fabian Debus
  • Markus Piel
  • Mikael Palner
  • Gitte M Knudsen
  • Hartmut Lüddens
  • Frank Rösch
DOI
10.1016/j.bmcl.2007.12.054
ISSN
0960-894X
Ausgabe der Veröffentlichung
4
Zeitschrift
Bioorganic &amp; Medicinal Chemistry Letters
Sprache
en
Paginierung
1515 - 1519
Datum der Veröffentlichung
2008
Status
Published
Herausgeber
Elsevier BV
Herausgeber URL
http://dx.doi.org/10.1016/j.bmcl.2007.12.054
Datum der Datenerfassung
2019
Titel
Total synthesis and evaluation of [18F]MHMZ
Ausgabe der Zeitschrift
18

Data source: Crossref

Abstract
Radiochemical labeling of MDL 105725 using the secondary labeling precursor 2-[(18)F]fluoroethyltosylate ([(18)F]FETos) was carried out in yields of approximately 90% synthesizing [(18)F]MHMZ in a specific activity of approximately 50MBq/nmol with a starting activity of approximately 3GBq. Overall radiochemical yield including [(18)F]FETos synthon synthesis, [(18)F]fluoroalkylation and preparing the injectable [(18)F]MHMZ solution was 42% within a synthesis time of approximately 100 min. The novel compound showed excellent specific binding to the 5-HT(2A) receptor (K(i)=9.0 nM) in vitro and promising in vivo characteristics.
Addresses
  • Institute of Nuclear Chemistry, University of Mainz, Fritz-Strassmann-Weg 2, 55128 Mainz, Germany.
Autoren
  • Matthias M Herth
  • Fabian Debus
  • Markus Piel
  • Mikael Palner
  • Gitte M Knudsen
  • Hartmut Lüddens
  • Frank Rösch
DOI
10.1016/j.bmcl.2007.12.054
eISSN
1464-3405
Externe Identifier
  • PubMed Identifier: 18187324
Open access
false
ISSN
0960-894X
Ausgabe der Veröffentlichung
4
Zeitschrift
Bioorganic & medicinal chemistry letters
Schlüsselwörter
  • Brain
  • Animals
  • Rats
  • Fluorine Radioisotopes
  • Fluorobenzenes
  • Piperidines
  • Ketanserin
  • Receptor, Serotonin, 5-HT2A
  • Serotonin Antagonists
  • Radiopharmaceuticals
  • Radionuclide Imaging
  • Radioligand Assay
  • Isotope Labeling
  • Binding, Competitive
  • Kinetics
  • Serotonin 5-HT2 Receptor Antagonists
Sprache
eng
Medium
Print-Electronic
Online publication date
2007
Paginierung
1515 - 1519
Datum der Veröffentlichung
2008
Status
Published
Datum der Datenerfassung
2008
Titel
Total synthesis and evaluation of [18F]MHMZ.
Sub types
  • Research Support, Non-U.S. Gov't
  • Journal Article
Ausgabe der Zeitschrift
18

Data source: Europe PubMed Central

Abstract
Radiochemical labeling of MDL 105725 using the secondary labeling precursor 2-[(18)F]fluoroethyltosylate ([(18)F]FETos) was carried out in yields of approximately 90% synthesizing [(18)F]MHMZ in a specific activity of approximately 50MBq/nmol with a starting activity of approximately 3GBq. Overall radiochemical yield including [(18)F]FETos synthon synthesis, [(18)F]fluoroalkylation and preparing the injectable [(18)F]MHMZ solution was 42% within a synthesis time of approximately 100 min. The novel compound showed excellent specific binding to the 5-HT(2A) receptor (K(i)=9.0 nM) in vitro and promising in vivo characteristics.
Date of acceptance
2007
Autoren
  • Matthias M Herth
  • Fabian Debus
  • Markus Piel
  • Mikael Palner
  • Gitte M Knudsen
  • Hartmut Lüddens
  • Frank Rösch
Autoren-URL
https://www.ncbi.nlm.nih.gov/pubmed/18187324
DOI
10.1016/j.bmcl.2007.12.054
eISSN
1464-3405
Ausgabe der Veröffentlichung
4
Zeitschrift
Bioorg Med Chem Lett
Schlüsselwörter
  • Animals
  • Binding, Competitive
  • Brain
  • Fluorine Radioisotopes
  • Fluorobenzenes
  • Isotope Labeling
  • Ketanserin
  • Kinetics
  • Piperidines
  • Radioligand Assay
  • Radionuclide Imaging
  • Radiopharmaceuticals
  • Rats
  • Receptor, Serotonin, 5-HT2A
  • Serotonin 5-HT2 Receptor Antagonists
  • Serotonin Antagonists
Sprache
eng
Country
England
Paginierung
1515 - 1519
PII
S0960-894X(07)01513-2
Datum der Veröffentlichung
2008
Status
Published
Datum, an dem der Datensatz öffentlich gemacht wurde
2008
Titel
Total synthesis and evaluation of [18F]MHMZ.
Sub types
  • Journal Article
  • Research Support, Non-U.S. Gov't
Ausgabe der Zeitschrift
18

Data source: PubMed

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