Total synthesis and evaluation of [18F]MHMZ

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Standard

Total synthesis and evaluation of [18F]MHMZ. / Herth, Matthias M; Debus, Fabian; Piel, Markus; Palner, Mikael; Knudsen, Gitte M; Lüddens, Hartmut; Rösch, Frank.

In: Bioorganic & Medicinal Chemistry Letters, Vol. 18, No. 4, 2008, p. 1515-1519.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Herth, MM, Debus, F, Piel, M, Palner, M, Knudsen, GM, Lüddens, H & Rösch, F 2008, 'Total synthesis and evaluation of [18F]MHMZ', Bioorganic & Medicinal Chemistry Letters, vol. 18, no. 4, pp. 1515-1519. https://doi.org/10.1016/j.bmcl.2007.12.054

APA

Herth, M. M., Debus, F., Piel, M., Palner, M., Knudsen, G. M., Lüddens, H., & Rösch, F. (2008). Total synthesis and evaluation of [18F]MHMZ. Bioorganic & Medicinal Chemistry Letters, 18(4), 1515-1519. https://doi.org/10.1016/j.bmcl.2007.12.054

Vancouver

Herth MM, Debus F, Piel M, Palner M, Knudsen GM, Lüddens H et al. Total synthesis and evaluation of [18F]MHMZ. Bioorganic & Medicinal Chemistry Letters. 2008;18(4):1515-1519. https://doi.org/10.1016/j.bmcl.2007.12.054

Author

Herth, Matthias M ; Debus, Fabian ; Piel, Markus ; Palner, Mikael ; Knudsen, Gitte M ; Lüddens, Hartmut ; Rösch, Frank. / Total synthesis and evaluation of [18F]MHMZ. In: Bioorganic & Medicinal Chemistry Letters. 2008 ; Vol. 18, No. 4. pp. 1515-1519.

Bibtex

@article{74418ac09b8d11debc73000ea68e967b,
title = "Total synthesis and evaluation of [18F]MHMZ",
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.",
keywords = "Animals, Binding, Competitive, Brain, Fluorine Radioisotopes, Fluorobenzenes, Isotope Labeling, Ketanserin, Kinetics, Piperidines, Radioligand Assay, Radiopharmaceuticals, Rats, Receptor, Serotonin, 5-HT2A, Serotonin 5-HT2 Receptor Antagonists, Serotonin Antagonists",
author = "Herth, {Matthias M} and Fabian Debus and Markus Piel and Mikael Palner and Knudsen, {Gitte M} and Hartmut L{\"u}ddens and Frank R{\"o}sch",
year = "2008",
doi = "10.1016/j.bmcl.2007.12.054",
language = "English",
volume = "18",
pages = "1515--1519",
journal = "Bioorganic & Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Pergamon Press",
number = "4",

}

RIS

TY - JOUR

T1 - Total synthesis and evaluation of [18F]MHMZ

AU - Herth, Matthias M

AU - Debus, Fabian

AU - Piel, Markus

AU - Palner, Mikael

AU - Knudsen, Gitte M

AU - Lüddens, Hartmut

AU - Rösch, Frank

PY - 2008

Y1 - 2008

N2 - 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.

AB - 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.

KW - Animals

KW - Binding, Competitive

KW - Brain

KW - Fluorine Radioisotopes

KW - Fluorobenzenes

KW - Isotope Labeling

KW - Ketanserin

KW - Kinetics

KW - Piperidines

KW - Radioligand Assay

KW - Radiopharmaceuticals

KW - Rats

KW - Receptor, Serotonin, 5-HT2A

KW - Serotonin 5-HT2 Receptor Antagonists

KW - Serotonin Antagonists

U2 - 10.1016/j.bmcl.2007.12.054

DO - 10.1016/j.bmcl.2007.12.054

M3 - Journal article

C2 - 18187324

VL - 18

SP - 1515

EP - 1519

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

SN - 0960-894X

IS - 4

ER -

ID: 14248300