Radiosynthesis and in vivo evaluation of novel radioligands for PET imaging of cerebral 5-HT7 receptors
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Radiosynthesis and in vivo evaluation of novel radioligands for PET imaging of cerebral 5-HT7 receptors. / Hansen, Hanne D; Herth, Matthias M; Ettrup, Anders; Andersen, Valdemar L; Lehel, Szabolcs; Dyssegaard, Agnete; Kristensen, Jesper Langgaard; Knudsen, Gitte M.
In: Journal of Nuclear Medicine, Vol. 55, No. 4, 24.02.2014, p. 640-646.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Radiosynthesis and in vivo evaluation of novel radioligands for PET imaging of cerebral 5-HT7 receptors
AU - Hansen, Hanne D
AU - Herth, Matthias M
AU - Ettrup, Anders
AU - Andersen, Valdemar L
AU - Lehel, Szabolcs
AU - Dyssegaard, Agnete
AU - Kristensen, Jesper Langgaard
AU - Knudsen, Gitte M
PY - 2014/2/24
Y1 - 2014/2/24
N2 - The serotonin (5-hydroxytryptamine [5-ΗΤ]) 7 receptor (5-HT7R) is the most recently discovered 5-HT receptor, and its physiologic and possible pathophysiologic roles are not fully elucidated. So far, no suitable 5-HT7R PET radioligand is available, thus limiting the investigation of this receptor in the living brain. Here, we present the radiosynthesis and in vivo evaluation of Cimbi-712 (3-{4-[4-(4-methylphenyl)piperazine-1-yl]butyl}p-1,3-dihydro-2H-indol-2-one) and Cimbi-717 (3-{4-[4-(3-methoxyphenyl)piperazine-1-yl]butyl}-1,3-dihydro-2H-indol-2-one) as selective 5-HT7R PET radioligands in the pig brain. The 5-HT7R distribution in the postmortem pig brain is also assessed.
AB - The serotonin (5-hydroxytryptamine [5-ΗΤ]) 7 receptor (5-HT7R) is the most recently discovered 5-HT receptor, and its physiologic and possible pathophysiologic roles are not fully elucidated. So far, no suitable 5-HT7R PET radioligand is available, thus limiting the investigation of this receptor in the living brain. Here, we present the radiosynthesis and in vivo evaluation of Cimbi-712 (3-{4-[4-(4-methylphenyl)piperazine-1-yl]butyl}p-1,3-dihydro-2H-indol-2-one) and Cimbi-717 (3-{4-[4-(3-methoxyphenyl)piperazine-1-yl]butyl}-1,3-dihydro-2H-indol-2-one) as selective 5-HT7R PET radioligands in the pig brain. The 5-HT7R distribution in the postmortem pig brain is also assessed.
U2 - 10.2967/jnumed.113.128983
DO - 10.2967/jnumed.113.128983
M3 - Journal article
C2 - 24566002
VL - 55
SP - 640
EP - 646
JO - The Journal of Nuclear Medicine
JF - The Journal of Nuclear Medicine
SN - 0161-5505
IS - 4
ER -
ID: 103038632