Synthesis and in vitro evaluation of oxindole derivatives as potential radioligands for 5-HT(7) receptor imaging with PET

Matthias M Herth; Balázs Volk; Katalin Pallagi; Lasse Kofoed Bech; Ferenc A Antoni; Gitte M Knudsen; Jesper Langgaard Kristensen

doi:10.1021/cn3001137

Synthesis and in vitro evaluation of oxindole derivatives as potential radioligands for 5-HT(7) receptor imaging with PET

Matthias M Herth, Balázs Volk, Katalin Pallagi, Lasse Kofoed Bech, Ferenc A Antoni, Gitte M Knudsen, Jesper Langgaard Kristensen

Afdeling for Hjerne- og Nervesygdomme

27 Citationer (Scopus)

Abstract

The most recently discovered serotonin (5-HT) receptor subtype, 5-HT(7), is considered to be associated with several CNS disorders. Noninvasive in vivo positron emission tomography (PET) studies of cerebral 5-HT(7) receptors could provide a significant advance in the understanding of the neurobiology and eventual dysfunctions of the 5-HT(7) receptor. To date, no appropriate 5-HT(7) receptor PET ligand has been developed. Here, we modified known 5-HT(7) selective phenylpiperazinyl-butyloxindole derivatives so that they may be labeled either with carbon-11 or fluorine-18. A set of potential 5-HT(7) ligands for PET molecular imaging was successfully synthesized. Two compounds (10 and 14) were tested against a range of targets. Both compounds display a promising in vitro profile with respect to PET imaging of the 5-HT(7) receptor in thalamic regions.

Originalsprog	Engelsk
Tidsskrift	A C S Chemical Neuroscience
Vol/bind	3
Udgave nummer	12
Sider (fra-til)	1002-7
Antal sider	6
ISSN	1948-7193
DOI	https://doi.org/10.1021/cn3001137
Status	Udgivet - 2012

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10.1021/cn3001137

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title = "Synthesis and in vitro evaluation of oxindole derivatives as potential radioligands for 5-HT(7) receptor imaging with PET",

abstract = "The most recently discovered serotonin (5-HT) receptor subtype, 5-HT(7), is considered to be associated with several CNS disorders. Noninvasive in vivo positron emission tomography (PET) studies of cerebral 5-HT(7) receptors could provide a significant advance in the understanding of the neurobiology and eventual dysfunctions of the 5-HT(7) receptor. To date, no appropriate 5-HT(7) receptor PET ligand has been developed. Here, we modified known 5-HT(7) selective phenylpiperazinyl-butyloxindole derivatives so that they may be labeled either with carbon-11 or fluorine-18. A set of potential 5-HT(7) ligands for PET molecular imaging was successfully synthesized. Two compounds (10 and 14) were tested against a range of targets. Both compounds display a promising in vitro profile with respect to PET imaging of the 5-HT(7) receptor in thalamic regions.",

author = "Herth, {Matthias M} and Bal{\'a}zs Volk and Katalin Pallagi and {Kofoed Bech}, Lasse and Antoni, {Ferenc A} and Knudsen, {Gitte M} and Kristensen, {Jesper Langgaard}",

year = "2012",

doi = "10.1021/cn3001137",

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T1 - Synthesis and in vitro evaluation of oxindole derivatives as potential radioligands for 5-HT(7) receptor imaging with PET

AU - Herth, Matthias M

AU - Volk, Balázs

AU - Pallagi, Katalin

AU - Kofoed Bech, Lasse

AU - Antoni, Ferenc A

AU - Knudsen, Gitte M

AU - Kristensen, Jesper Langgaard

PY - 2012

Y1 - 2012

N2 - The most recently discovered serotonin (5-HT) receptor subtype, 5-HT(7), is considered to be associated with several CNS disorders. Noninvasive in vivo positron emission tomography (PET) studies of cerebral 5-HT(7) receptors could provide a significant advance in the understanding of the neurobiology and eventual dysfunctions of the 5-HT(7) receptor. To date, no appropriate 5-HT(7) receptor PET ligand has been developed. Here, we modified known 5-HT(7) selective phenylpiperazinyl-butyloxindole derivatives so that they may be labeled either with carbon-11 or fluorine-18. A set of potential 5-HT(7) ligands for PET molecular imaging was successfully synthesized. Two compounds (10 and 14) were tested against a range of targets. Both compounds display a promising in vitro profile with respect to PET imaging of the 5-HT(7) receptor in thalamic regions.

AB - The most recently discovered serotonin (5-HT) receptor subtype, 5-HT(7), is considered to be associated with several CNS disorders. Noninvasive in vivo positron emission tomography (PET) studies of cerebral 5-HT(7) receptors could provide a significant advance in the understanding of the neurobiology and eventual dysfunctions of the 5-HT(7) receptor. To date, no appropriate 5-HT(7) receptor PET ligand has been developed. Here, we modified known 5-HT(7) selective phenylpiperazinyl-butyloxindole derivatives so that they may be labeled either with carbon-11 or fluorine-18. A set of potential 5-HT(7) ligands for PET molecular imaging was successfully synthesized. Two compounds (10 and 14) were tested against a range of targets. Both compounds display a promising in vitro profile with respect to PET imaging of the 5-HT(7) receptor in thalamic regions.

U2 - 10.1021/cn3001137

DO - 10.1021/cn3001137

M3 - Journal article

C2 - 23259035

SN - 1948-7193

VL - 3

SP - 1002

EP - 1007

JO - A C S Chemical Neuroscience

JF - A C S Chemical Neuroscience

IS - 12

ER -

Synthesis and in vitro evaluation of oxindole derivatives as potential radioligands for 5-HT(7) receptor imaging with PET

Abstract

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