Preliminary in vivo and ex vivo evaluation of the 5-HT2A imaging probe [18F] MH. MZ
- Publikationstyp:
- Zeitschriftenaufsatz
- Metadaten:
-
- Autoren
- Matthias M Herth
- Markus Piel
- Fabian Debus
- Ulrich Schmitt
- Hartmut Lueddens
- Frank Roesch
- Autoren-URL
- https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000266146700014&DestLinkType=FullRecord&DestApp=WOS_CPL
- DOI
- 10.1016/j.nucmedbio.2009.01.012
- eISSN
- 1872-9614
- Externe Identifier
- Clarivate Analytics Document Solution ID: 446UM
- PubMed Identifier: 19423013
- ISSN
- 0969-8051
- Ausgabe der Veröffentlichung
- 4
- Zeitschrift
- NUCLEAR MEDICINE AND BIOLOGY
- Schlüsselwörter
- MDL 100907
- Altanserin
- MH.MZ
- PET
- Fluorine-18
- 5-HT2A receptor
- Paginierung
- 447 - 454
- Datum der Veröffentlichung
- 2009
- Status
- Published
- Titel
- Preliminary in vivo and ex vivo evaluation of the 5-HT<sub>2A</sub> imaging probe [<SUP>18</SUP>F]MH.MZ
- Sub types
- Article
- Ausgabe der Zeitschrift
- 36
Datenquelle: Web of Science (Lite)
- Andere Metadatenquellen:
-
- Autoren
- Matthias M Herth
- Markus Piel
- Fabian Debus
- Ulrich Schmitt
- Hartmut Lüddens
- Frank Rösch
- DOI
- 10.1016/j.nucmedbio.2009.01.012
- ISSN
- 0969-8051
- Ausgabe der Veröffentlichung
- 4
- Zeitschrift
- Nuclear Medicine and Biology
- Sprache
- en
- Paginierung
- 447 - 454
- Datum der Veröffentlichung
- 2009
- Status
- Published
- Herausgeber
- Elsevier BV
- Herausgeber URL
- http://dx.doi.org/10.1016/j.nucmedbio.2009.01.012
- Datum der Datenerfassung
- 2023
- Titel
- Preliminary in vivo and ex vivo evaluation of the 5-HT2A imaging probe [18F]MH.MZ
- Ausgabe der Zeitschrift
- 36
Datenquelle: Crossref
- Abstract
- <h4>Introduction</h4>The 5-HT(2A) receptor is one of the most interesting targets within the serotonergic system because it is involved in a number of important physiological processes and diseases.<h4>Methods</h4>[(18)F]MH.MZ, a 5-HT(2A) antagonistic receptor ligand, is labeled by (18)F-fluoroalkylation of the corresponding desmethyl analogue MDL 105725 with 2-[(18)F]fluoroethyltosylate ([(18)F]FETos). In vitro binding experiments were performed to test selectivity toward a broad spectrum of neuroreceptors by radioligand binding assays. Moreover, first micro-positron emission tomography (microPET) experiments, ex vivo organ biodistribution, blood cell and protein binding and brain metabolism studies of [(18)F]MH.MZ were carried out in rats.<h4>Results</h4>[(18)F]MH.MZ showed a K(i) of 3 nM toward the 5-HT(2A) receptor and no appreciable affinity for a variety of receptors and transporters. Ex vivo biodistribution as well as microPET showed highest brain uptake at approximately 5 min p.i. and steady state after approximately 30 min p.i. While [(18)F]MH.MZ undergoes extensive first-pass metabolism which significantly reduces its bioavailability, it is insignificantly metabolized within the brain. The binding potential in the rat frontal cortex is 1.45, whereas the cortex to cerebellum ratio was determined to be 2.7 after approximately 30 min.<h4>Conclusion</h4>Results from microPET measurements of [(18)F]MH.MZ are in no way inferior to data known for [(11)C]MDL 100907 at least in rats. [(18)F]MH.MZ appears to be a highly potent and selective serotonergic PET ligand in small animals.
- Addresses
- Institute of Nuclear Chemistry, Johannes Gutenberg-University Mainz, D-55128 Mainz, Germany. herthm@uni-mainz.de
- Autoren
- Matthias M Herth
- Markus Piel
- Fabian Debus
- Ulrich Schmitt
- Hartmut Lüddens
- Frank Rösch
- DOI
- 10.1016/j.nucmedbio.2009.01.012
- eISSN
- 1872-9614
- Externe Identifier
- PubMed Identifier: 19423013
- Funding acknowledgements
- NIMH NIH HHS: N01MH32004
- Open access
- false
- ISSN
- 0969-8051
- Ausgabe der Veröffentlichung
- 4
- Zeitschrift
- Nuclear medicine and biology
- Schlüsselwörter
- Brain
- Animals
- Humans
- Rats
- Fluorobenzenes
- Piperidines
- Receptor, Serotonin, 5-HT2A
- Positron-Emission Tomography
- Autoradiography
- Tissue Distribution
- Radioactivity
- Male
- Sprache
- eng
- Medium
- Print-Electronic
- Online publication date
- 2009
- Paginierung
- 447 - 454
- Datum der Veröffentlichung
- 2009
- Status
- Published
- Datum der Datenerfassung
- 2009
- Titel
- Preliminary in vivo and ex vivo evaluation of the 5-HT2A imaging probe [(18)F]MH.MZ.
- Sub types
- Research Support, Non-U.S. Gov't
- Journal Article
- Research Support, N.I.H., Extramural
- Ausgabe der Zeitschrift
- 36
Datenquelle: Europe PubMed Central
- Abstract
- INTRODUCTION: The 5-HT(2A) receptor is one of the most interesting targets within the serotonergic system because it is involved in a number of important physiological processes and diseases. METHODS: [(18)F]MH.MZ, a 5-HT(2A) antagonistic receptor ligand, is labeled by (18)F-fluoroalkylation of the corresponding desmethyl analogue MDL 105725 with 2-[(18)F]fluoroethyltosylate ([(18)F]FETos). In vitro binding experiments were performed to test selectivity toward a broad spectrum of neuroreceptors by radioligand binding assays. Moreover, first micro-positron emission tomography (microPET) experiments, ex vivo organ biodistribution, blood cell and protein binding and brain metabolism studies of [(18)F]MH.MZ were carried out in rats. RESULTS: [(18)F]MH.MZ showed a K(i) of 3 nM toward the 5-HT(2A) receptor and no appreciable affinity for a variety of receptors and transporters. Ex vivo biodistribution as well as microPET showed highest brain uptake at approximately 5 min p.i. and steady state after approximately 30 min p.i. While [(18)F]MH.MZ undergoes extensive first-pass metabolism which significantly reduces its bioavailability, it is insignificantly metabolized within the brain. The binding potential in the rat frontal cortex is 1.45, whereas the cortex to cerebellum ratio was determined to be 2.7 after approximately 30 min. CONCLUSION: Results from microPET measurements of [(18)F]MH.MZ are in no way inferior to data known for [(11)C]MDL 100907 at least in rats. [(18)F]MH.MZ appears to be a highly potent and selective serotonergic PET ligand in small animals.
- Date of acceptance
- 2009
- Autoren
- Matthias M Herth
- Markus Piel
- Fabian Debus
- Ulrich Schmitt
- Hartmut Lüddens
- Frank Rösch
- Autoren-URL
- https://www.ncbi.nlm.nih.gov/pubmed/19423013
- DOI
- 10.1016/j.nucmedbio.2009.01.012
- eISSN
- 1872-9614
- Funding acknowledgements
- NIMH NIH HHS: N01MH32004
- Ausgabe der Veröffentlichung
- 4
- Zeitschrift
- Nucl Med Biol
- Schlüsselwörter
- Animals
- Autoradiography
- Brain
- Fluorobenzenes
- Humans
- Male
- Piperidines
- Positron-Emission Tomography
- Radioactivity
- Rats
- Receptor, Serotonin, 5-HT2A
- Tissue Distribution
- Sprache
- eng
- Country
- United States
- Paginierung
- 447 - 454
- PII
- S0969-8051(09)00036-5
- Datum der Veröffentlichung
- 2009
- Status
- Published
- Datum, an dem der Datensatz öffentlich gemacht wurde
- 2009
- Titel
- Preliminary in vivo and ex vivo evaluation of the 5-HT2A imaging probe [(18)F]MH.MZ.
- Sub types
- Journal Article
- Research Support, N.I.H., Extramural
- Research Support, Non-U.S. Gov't
- Ausgabe der Zeitschrift
- 36
Datenquelle: PubMed
- Autoren
- Matthias M Herth
- Markus Piel
- Fabian Debus
- Ulrich Schmitt
- Hartmut Lüddens
- Frank Rösch
- Zeitschrift
- Nuclear medicine and biology
- Artikelnummer
- 4
- Paginierung
- 447 - 454
- Datum der Veröffentlichung
- 2009
- Herausgeber
- Elsevier
- Datum der Datenerfassung
- 2021
- Titel
- Preliminary in vivo and ex vivo evaluation of the 5-HT2A imaging probe [18F] MH. MZ
- Sub types
- article
- Ausgabe der Zeitschrift
- 36
Datenquelle: Manual
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